Saturday, May 24, 2014

{Area-1255} Official Review ::: ErgoGenix ::: ErgoBLAST {Area-1255}

Alright folks, brand new review here. This time it's from one of my favorite companies - ErgoGenix. I've used their cortisol control supplement (ErgoBolic) before and was very impressed with the results. It felt a little more than natural to me and was a very strong aid when doing a bulk last summer. I've also used ErgoShred and it gave me a very prominent buzz, but not even jittery in the least.  This time,. I'm reviewing ErgoBlast, A new Pre-Workout from them. 


I've only taken it a couple days now, and I can say energy boost from it is very noticeable. I've noticed very strong pumps before even getting into the second set of bench. 






I will be reviewing both flavors; Pineapple Mango and Strawberry Kiwi




Pineapple Mango
5/5
(Tastes like Powerade)


Was very Impressed with the taste, put a few ice cubes in with Fiji water - I gotta say, it's like Powerade or better!!!


Now today was a plain old bench press and chest press day.
About ten minutes after drinking it, the first thing I noticed was a very profound sense of focus; focused on the entire "to do list" of workouts. I was anxious to get to the Gym, and very amped to get going. I felt as if nothing mattered except the workout, now, normally it takes me a little while to get going and I need more of a warm up - not with this. I nearly blazed past the check in counter. I blasted out 50 military push-ups to get ready.

Started stacking the weights on bench press...this is where it gets good. Right in the middle of the first set, I got a crazy surge of focus. "Tunnel-Vision" my friends. Like nothing else mattered. 

Now before even getting to the second set, the pumps were already amazing. Vascularity is noticeable - though normally my veins are pretty prominent; they are especially engorged with this product.


Continuing on throughout the set, the Weights are actually feeling lighter, I did squeez out 4 extra reps even on the second set - though I am using high Repetition/moderate weight anyway.

I usually max out on the last set.

Third set - 5 extra reps, maybe today is a really good day, but I'm not distracted by anything....


DAY TWO (Logging)
Warmed up with Weighted Dips and Pull-ups. Strong, immediate, sense of motivation today as well, pumps are +++10. 
Did Squat's and Deadlifts today, no hesitation! Kept going finished and then even did a few reps on the bench (even though today is not bench day).
Did push-ups til failure last set and felt as though I could keep going! 
When I got home I did three more sets of push-ups (50x each) and that was it! (Normally wouldn't have)
Really liking this product!

Definitely no bloating to report, but that's typical with the Con-Cret. No other side-effects except a little facial flushing and something that kind of resembled a niacin flush (only lasted like 15 seconds). 
Tomorrow is a rest day so I will post again Thursday.

(Today I tried Strawberry Kiwi - and this is also an easy 5/5, very tasty!)




rest day


Day Three 
Kicked out 7 more reps than usual on the Pull-Up bar today, on the last set which usually drops!
Also did Legs today, both added 3 reps on set (4) and added weight as well. (!)
When I went for a run today, I got a bad headache and actually slowed down my pace halfway (ran 4 miles).. however allergies are kicking up around now as well. So it's too be expected.

All-round my strength has definitely been up and endurance as well. 
Differences are clear and noticeable.
No side-effects to report. Will keep logging.

_______________________________________________________________________________
(#8 Post) 
_______________________________________________________________________________
Stuff started to clump together today....



Anyhow, this is my Strawberry Kiwi review.


DAY FOUR

Once again, 5/5 taste. I'm not sure which one I like better as I like them both alot.

Did 4 sets of Barbell Squats (8 reps each) and 3 sets of Power Cleans today. (5 reps/= each)
Pump's are still great, focus in unreal. Aggression is "enhanced" on this due to the fact I am entirely focused on the workout, nothin else.
Also did roughly 600 push-ups today - military.

UPDATE : Strawberry Kiwi definitely leans on the sour bitter side - but dammit I love both of em!

When I got home, I did another 200 push-ups. That's 800. Goin for Chest again on Monday.



________________________________________________________________________

Today was supposed to be a rest day but I ended up doing some Squats and on the bench press once more. A masterful 15 reps at 250 - 4 more than usual for a first set. Strong ****.
________________________________________________________________________
MONDAY JUNE 2nd
________________________________________________________________
Chest workout today, Chest Press + Bench Press + Butterflies...!
Pump is unreal! Energy + Focus = Overdrive. 
Extra reps on all workouts; +5 on bench (set2/3) and + 6 on last set of chest press. 
Also ran 3 miles. No headache this time either.

________________________________________________________________________



DAY 6 + 7
Did a hella lot of Cardio these days - noticed Vascularity is insane lately.
This stuff is the ****!
I thought Assault was good, this is better!
Plus I don't get the tingling and histamine response with this one.
Folks, ergoBlast is where it's at!



_____________________________________________________________________________________


FINAL THOUGHTS AND REVIEW
1.) Both Flavors are Easy 5/5 - the Strawberry Kiwi is noticeably sour and the Pineapple Mango is extremely sweet. Mix with plenty of water and you've got yourself an energizing treat that tastes like Powerade or better!
2.) Tunnel-Vision focus is Unreal on this sup, I also noticed a little tingling on the last few days, during bench sets or any heavy work. Not in a bad way though.
3.) Strength and Reps both increased, refer to earlier part of log.
4.) Vascularity increased (even though I normally look cut up, veins became even more pronounced).
5.) No side-effects other than a headache on 1 day when going for a run.
6.) Mental Clarity and Focus for intellectual tasks was also increased on this. Probably due to the Huperzine-A compound, among others.

7.) Faster response time and reflexes during training were improved.








Wednesday, May 21, 2014

HypoProlactinaemia (Low Prolactin) in Men - A Cause for Concern or Ideal State?

Bodybuilders, Fitness Enthusiasts and ordinary men who have had elevated prolactin know firsthand the downsides of High Prolactin levels; it will ruin your sex drive, decrease testosterone production as well as dopamine and turn you into an Apathetic and passive zombie. In the meantime, you are gaining weight and suffering from insulin resistance. So we know for sure that high Prolactin is bad, but do we know the whole story behind prolactin's effects? Moreover, when people go on dopaminergics to lower prolactin back into the normal range, some actually end up nearly obliterating prolactin. As the level of prolactin fades into the deficient or even undetectable stage, should we be worried of possible side-effects? There is a condition describing this stage, it's called HypoProlactinaemia (as opposed to Hyperprolactinaemia which describes high prolactin), and it can also present serious side-effects.

Let's start by defining the effects of prolactin on the androgen receptor, according to PubMed - prolactin increases androgen uptake in the Prostate and also increases 5-Alpha-Reductase (the enzyme that converts testosterone into DHT).




Prostate. 1988;12(3):221-9.

Prolactin effect on the permeability of human benign hyperplastic prostate to testosterone.

Farnsworth WE.

                          Abstract

While it has been known for over 30 years that prolactin (Prl) synergizes with androgen in the support and stimulation of prostatic growth and metabolism, the evidence that this is accomplished through increasing access of the steroid to the cellular machinery of the gland has arisen only since about 1970. There is widespread uncertainty as to how the Prl effect takes place: by 1) increasing the free steroid concentration in the blood; 2) facilitating the uptake of protein-bound androgen; 3) increasing, by metabolism or receptor-binding, the concentration gradient that can support passive diffusion of the steroid across the plasma membrane; or 4) modification of the fluidity of the membrane itself to increase the solubility of the steroid in the lipoprotein and, thus, the ease of penetration of the cell. The present study attempted to learn if Prl is an effective stimulus of androgen uptake when the first three options are not operative. Using an equilibrium exchange procedure to track the uptake of [17 alpha-3H]-testosterone ([17 alpha-3H]-T) into minced benign hyperplastic human prostate tissue and the irreversible metabolism of the entering steroid to [17 alpha-3H]-dihydrotestosterone [17 alpha-3H]-DHT, it was found that the rate of production of the 5 alpha-reduced metabolite, during a 1-hr incubation in vitro, was directly proportional to the concentration of ovine Prl over the dose range of 0-160 ng/ml. The clinical significance of Prl mediation of steroid uptake is discussed, and suggestions are made as to how the Prl might alter the permeability of the plasma membrane.

PMID: 2453860 [PubMed - indexed for MEDLINE]
Prolactin also has a DIRECT effect on Adrenal Androgen release; being synergistic with ACTH in increasing androgen output (starting with DHEA).(1)

Therefore one would assume that by lowering prolactin excessively, one would then enter a Hypoandrogenic state or at the least a state of 5-alpha-reductase deficiency. This makes sense being that yet another study showed a group of males with induced low prolactin - were rendered infertile with oligozoospermia,  asthenospermia, and hypofunction of seminal vesicles(2). DHT has known effects on maintaining normal sperm motility and production as well as stimulating both seminal vesicles and allowing for normal ejaculation(3)(4)

Therefore, we are describing hypoprolactinaemia as a state similar to the 5-AR deficiency in users of the 5-AR inhibiting drug Finasteride.




Arch Androl. 1989;23(3):259-65.

Hypoprolactinemia as related to seminal quality and serum testosterone. Gonzales GF1, Velasquez G, Garcia-Hjarles M. Author information Abstract Semen quality and serum testosterone were studied in six men with hypoprolactinemia (less than or equal to 6 ng/ml) and in normoprolactinemic controls. The incidence of hypoprolactinemia in 92 men attending an infertility clinic was 7.5%. Males with hypoprolactinemia showed in high percentage of disorders (oligozoospermia, 50%; asthenospermia, 75%; hypofunction of seminal vesicles, 67%; and hypoandrogenism, 67%). Hypoprolactinemia is a clinical disorder associated mainly with poor sperm motility.



PMID:

2619414

[PubMed - indexed for MEDLINE]





One other study also described the side-effects of low prolactin in men even better; men presented with Metabolic Syndrome, Premature Ejaculation, Anxiety and Ateriogenic Erectile Dysfunction(5). With this picture, it is looking like low prolactin is causing not only androgen deficiency (or at least low DHT) but also some sort of haywire nervous system....anxiety and premature ejaculation both are associated with elevated glutamate and possibly norpinephrine.

So I went even further and found these studies.

 The effect of prolactin on glutamate decarboxylase activity and GABA concentration in hypothalamic slices.

B H Duvilanski, A Seilicovich, M C Diaz, M Lasaga, L Debeljuk Centro de Investigaciones en Reproduction, Facultad de Medicina, Universidad de Buenos Aires, 1121 Buenos Aires, Argentina Psychoneuroendocrinology

(Impact Factor: 5.14). 02/1987; 12(2):107-16. DOI:10.1016/0306-4530(87)90041-2 

PubMed ABSTRACT

The effect of prolactin on the activity of GABA-related enzymes and GABA concentrations were studied in hypothalamic slices incubated in vitro. After short periods of incubation (up to 40 min), prolactin (0.25 micrograms/ml) added to the incubation medium produced a significant increase (21% at 20 min of incubation) in glutamic acid decarboxylase (GAD) activity in the hypothalamic slices. A higher concentration of prolactin (1.0 micrograms/ml) produced a slight but significant decrease (8% at 20 min of incubation) in hypothalamic GAD activity. However, after longer periods of incubation (over 8 hr), both doses of prolactin induced a sustained increase in hypothalmic GAD activity, a response which depends upon protein synthesis. No changes were observed in GABA-transaminase (GABA-T) activity of hypothalamic slices incubated in the presence of prolactin. Prolactin decreased GABA concentration in the hypothalami incubated for 10 hr and, at the same time, increased GABA release into the medium. These results indicate that prolactin modifies the synthesis and release of hypothalmic GABA and suggest the existence of a feedback mechanism that prolactin may exert directly at the hypothalamic level.


                                                              ARTICLE 2 



 2002;114(1):229-38.

Prolactin-releasing peptide (PrRP) promotes awakening and suppresses absence seizures.



Lin SH1, Arai AC, España RA, Berridge CW, Leslie FM, Huguenard JR, Vergnes M, Civelli O.



Abstract

Prolactin releasing peptide (PrRP) is a recently identified neuropeptide that stimulates prolactin release from pituitary cells. The presence of its receptor outside the hypothalamic-pituitary axis suggests that it may have other functions. We present here evidence that PrRP can modulate the activity of the reticular thalamic nucleus, a brain region with prominent PrRP receptor expression that is critical for sleep regulation and the formation of non-convulsive absence seizures. Intracerebroventricular injection of PrRP (1-10 nmol) into sleeping animals significantly suppresses sleep oscillations and promotes rapid and prolonged awakening. Higher concentrations of PrRP (10-100 nmol) similarly suppress spike wave discharges seen during absence seizures in genetic absence epilepsy rats from Strasbourg, an animal model for this disorder. In concordance with these findings, PrRP suppressed evoked oscillatory burst activity in reticular thalamic slices in vitro. These results indicate that PrRP modulates reticular thalamic function and that activation of its receptor provides a new target for therapies directed at sleep disorders and absence seizures.

Copyright 2002 IBRO PMID: 12207968 [PubMed - indexed for MEDLINE]


Given both of these studies dictate prolactin as inhibitory, we can conclude that prolactin may be protective against excessive glutamate by increasing the enzymes that Convert glutamate into GABA (the brains primary inhibitory or "calming" neurotransmitter). Then this makes sense as well, since glutamate generally increases prolactin, whereas GABA inhibits prolactin, low prolactin then increases glutamate in order to try and raise prolactin up to the norm - by negative feedback. Unfortunately, in many cases this particular adaptation response fails, because the low prolactin state is often induced by drugs or bulimia. 

This also makes sense going back to the other study showing hypoprolactinaemia as causing anxiety and premature ejactulation, as said before (and my theory was correct), glutamate excess or deficiency of GABA becomes apparent when prolactin drops too low. Therefore seizure disorders, anxiety, OCD and other similar disorders may also appear in the presence of low prolactin.  

Considering Androgens such as DHT also increase GABA release while decreasing glutamate, and that low prolactin levels lead to low androgen or at least low DHT - this represents another mechanism by which hypoprolactinaemia (low prolactin) causes anxiety and restlessness. 





Therefore in Summary, HypoProlactinaemia (though decreasing or eliminating the refractory period) may be outweighed by the other side-effects of low prolactin and so I advise caution against reducing prolactin to a deficient or undetectable state, especially in those particularly susceptible to anxiety, E.D, or any like conditions.



  • Deficient Prolactin in men induces low DHT levels and lower Androgen levels.
  • Low Prolactin may cause anxiety; by decreasing GABA synthesis and increasing glutamate activity.
  • Low Prolactin may cause Calcium Channel overload and increased noradrenaline.
  • Low Prolactin may cause male infertility; oligozoospermia and asthenospermia.
  • Hypoprolactinaemia also leads to premature ejaculation and anxiety induced and / or arteriogenic E.D.


Sunday, May 18, 2014

Born to be Relentless

I have witnessed throughout my life, multiple great atrocities; I've witnessed the failure and regression of people born capable, but taught otherwise nearly since birth. I've witnessed indiscretion upon trainers, teachers, parents, politicians, spokesman, Leaders, sports players, veteran's, corporation's and virtually every significant entity that exists in America. I've witnessed times of good judgement as well - but the consistency is appalling. I've witnessed intolerance by young and old, and I've witnessed arrogance by all. There's a movement towards egotism, and there's a new trend that's been brewing, and has manifested - the trend of total narcissism both in those who didn't make it and in those who did.  Even so, those who have climbed the steps to the top now carry with them arrogance in fear of losing what they have gained.



All who gain significant power are afraid to lose it

Why are people so filled with strife that one's success in the world has to be paralleled by an equivalent sense of paranoia!!!? Why is this necessary? The colliding of forces perhaps, an enigma on one end can never be trusted, out of the ordinary is deemed insane! Do any of you ever stop to look at ANY of this. People must grab a hold of their conscience before it slips away completely - into the black hole of this infected and ever-primal world. 

Now it was once said that if you become all instinct, and know not love or peace that this would happen. 


There's unnecessary heartache in the world because people only have the shield of arrogance in defense to the first attack, instead of dissolving this with peace, or forgive and forget, people rage back. People, need to move on and find a new path. If more did this, then they wouldn't be so focused on an unnecessary battle, with incalculable ends, and with treacherous consequences. Besides, if there is one thing we should be focusing our anger on, it's the state of economy and government that sweeps most of us into misery every day, that precedes daily conflict amongst normal humans.


Therefore, to keep what you have gained (it is not easy to not be paranoid), you must keep the people's hearts who have supported you....who knows when you may fall incapable of dealing with a circumstance..or two. If you underestimate what can happen, it is a problem, but this should then apply to everything. Therefore, territorial and rude to underlings and subordinates at work or in an organization, because things *can* fall apart, this....this is the manifestation, of your fear, and this is why FEAR CORRUPTS.


Yes, fear is one of the most (if not the most) corrupt emotions in many circumstances, it is a dark emotion that leads to violence, hatred and unending peril and suffering amongst men. When you fear excessively, this spreads like wildfire to those who know you well, and if they get wind of this, now hostility is present, but if you can rid that fear, or remove it with logic, now you have the capability to put others at ease as well!


In a work environment, this applies, in a home environment, this applies, in a school or college, this applies. If positivity doesn't exist and everyone surrounded themselves with fear, who would trust each other? No one. Why ? Fight or Flight. A constant adrenaline rush upon humanity? No one can get along this way. This is where it is getting towards, more and more people and groups of people are so isolated, even when being right next to each other, people are afraid to talk because when a persons attitude carries with them a constant sense of fear and aversion, it makes others wonder, and get nervous.


One person can change an entire room, town, city, country, or even the world, simply by letting his aura be made so strongly manifest, and having a relentless desire for change, that it creates a "charge" in the atmosphere of energies we live in.




This is the philosophy I take with me today... 


It is the philosophy of better days, the philosophy of a better future; or at least a future where some are worthy to be among the reformers who rejuvenate honesty, respect, and a more traditional image of power. 

I will continue to write, because with me is a relentless spirit, who sets goals and accomplishes them, and with every set back is the desire to push forward two times stronger, this has been true since I was 5 years old, and will continue to be. I may be on the brink of madness at times, but I surely will maintain sanity when needed, and whatever else is necessary. I will take every tool needed for every journey, and endure. 

I am more than a strong and courageous spirit, I am one divinely inspired, motivated to obtain, and motivated to inform. Motivated to inspire, and motivated to Lead, strength in battle, strength in the mind, and the strength to move forward. 

Relentless then, relentless now. Born to be Relentless.

Thursday, May 15, 2014

Overpowering Adversity and Utilizing Your Environment in a Closed Minded Society (Freely)

I was born not under the chains of constraint, nor into the lines of fault; I was born a free human with the ability to be aware, the ability to be productive and the ability to eventually influence - thought at first I did not see it this way. Because I emphasized these trait's as something either unimportant, or the ability to influence, though felt and heard, was a difficult task according to my own definition! In my younger days at least....but for any like person, who was not born amidst a highly intelligent and rich family....who was not born out of furiously unfortunate circumstances either - I say to you, the only battle that is going to hold you back consistently throughout life - is the battle in your mind. The conflict of perceptions; the reality you hold dear, you have to ask yourself .... is this reality formed because of your own pessimistic ideation?  Is it formed from what another person is telling you? The thing is, no one has the right to judge you, and your capabilities,

Albert Einstein wrote..


Everybody is a Genius. But If You Judge a Fish by Its Ability to Climb a Tree, It Will Live Its Whole Life Believing that It is Stupid.

What this means is... other people's expectations are often wrongly timed, misplaced, and distorted, and this is also evident in the education system  today - a system built out of lies, inspiring not awareness, but comprised of a will favoring the strong suppression of the mind; by enclosing a wretched "Common Core" curriculum upon those who attend and entertain it. As I said before, influencing others was a difficult task according to my own definition, but the reality is - it wasn't my own definition was it? No. It was the definition, and lack of expectation, generated from a false education system; a GOVERNMENT run education system,.. now day by day more people are wondering why they send their kids to a school that hardly teaches communication skills, that hardly ever teaches anyone to think for themselves, to think "outside the box", I'm sure people scratch their heads wondering - why does everything seem so robotic, void and "standardized"....the answer to me is clear.

The people who put these standards out, the People who enforce this agenda - are set to destroy the old mind, and replace it with a programmed mind; one who is taught to only believe - if from the origin's of vastly exaggerated textbooks and unreliable criteria, one set upon the pendulum of disinformation, modification of reality and one that strategically does NOT want a Smart population; who can have any possibility of creating real change in the living "atmosphere". This is a system that favor's conflict, condemns people who are spiritually Just, condemns progress, and allows for compensatory and hostile mindsets, by taking away the reality from their own minds. I have no doubt that people often search their own heart's, knowing they are right, but because of this terrible system, they are thrown backwards, criticized and made to be persecuted.

Ignorance and stupidity spread like a wildfire, but in this system, the most pathetic thing, is ignorance and stupidity have become Popular, and adored.

Even so, ignorance has been made to sound like humility, and wisdom - the inverse upon which was intended for mankind, and for the concept of freedom, a concept being destroyed at an accelerated pace in the last decade.

We've been plagued by ignorance and a society that labels people based on their differences, as if Science can determine everything...and perhaps it can determine most things, but it is not an omnipotent tool of greatness and more often this same science is used to control population, perhaps the accuracy in technology is the downfall in society; for when technology becomes accurate and is used as an identification tool - for all the smart ones; the Indigo Children; Prodigy's, it is then used as a tool to single out those same people who refuse to live by the structure given to us. It is used as a tool to single out freedom and to amplify the power's of a corrupt government by not only diverting, but extracting the multitude's who have potential, throwing them into an institution, or throwing them into some "Mental Clinic".

They'll be damned when people adapt to the system and simultaneously display and project emphatically the ideas of their mind, the system will be damned when people become visual, and step out of their delirium, a delirium created by the conflict of human will's.


 That's the funny thing in all this, sometimes the human will - those who really have it, are able to surpass their ancestor's and also prevail in a modern, "pre-set" society, and when this happens, this system is also persecuted, but not in great enough numbers to succeed. No. If we want a free and just society; one where we overpower adversity, and teach our kids valuable "old-school" traits like courage, and never giving up; one where we teach our kids INSIGHT, and the ability to think for themselves.....then we must re-group, we must take these traits and utilize them x100 - we should expect adversity, from all ends, even our own family at times, but be not confined or disarmed by this; realize it is a manifestation of the "mainstay virus" - the virus of closed-mindedness, the one we must defeat at all costs.


Anyone can be a part of this - and for those who don't agree, or for the typical un-awake american population, I'm going to ask you to think about this - just a few sentences is all you have to utter in your brain, how does one or many go about controlling large groups of people? How in the past have tyrannical rulers taken control, moreover; what do you see in movies, video games and every day in your lives as it relates?

I ask you to ask yourself, are we really free? What would be the best way to control population..?
If you were to be insightful, you would understand - set yourself in the real shoes of the corrupt Politicians, this Corrupt Government, and ask yourselves - how would they operate? You can even make it sound theoretical in your mind, and when you ask yourself that also ask yourself - "why does everyone with my belief  (who you most likely have come across at least once, some point in your life) believe so strongly in such"?

Surely, knowing how belief works..there must be something to this and so ask yourself - are you believing what you believe because of fear? Are you believing what you believe because it is an inconvenience to your own lifestyle? Should this be allowed to substitute the truth - when the truth can make you a STRONGER person? Should you and your whole generation be condemned by the **possibility** that we are right, me and everyone who speaks like me...? Is that the chance you want to take? If so, read one last line...what then is the reason for failure in this society? What then is the reason for belligerence and pessimism ? What has happened every time you have "gone mad", what have YOU been conflicting with? I'm betting that there is somewhere down the line, a conflict of thought and perception, brought about at least in part - from the contributions of this corrupt system. It's a heir to the old roman empire is what this is. That's what America is now, and that's what we must defeat, instead of looking the other way.

When you realize the sacrifices that need to be made, and start to stand up for them - but on your own will, not by feeling like people are pushing them on you...after all - who wants to follow a message that has been Pressured upon people?

No, I encourage people to search on their own, and with their own sense, find the truth as they see it but considering what I have said - if it comes after your finding of the truth, or during, that you then begin to apply your own sense of criticism - because you have been deceived by this system as well, and you will see I have built this writing not upon hypocrisy; but in support of your will and freedomin support of your personal strength, and I sincerely hope you all find your place in life, and do not let any of Society's  "standards" limit you in any way. Find your own path, but let the elements of freedom merge you with your destiny.

Find your own path, but let the elements of freedom merge you with your destiny.


With all of this utilized, we can overcome adversity, and using the same traits to re-create our individualization, we can also change the environment, and create a new one even; except with the arrow of persecution upon the Corrupt minds who try to control all of us.

Tuesday, May 13, 2014

Re-Igniting and (Possibly) Finishing the Search for the "Dopaminergic Pot of Gold"




WARNING : Everything you read here is theoretical and for educational purposes, you may read and absorb, but do not take the methods literally. If you happen to do this, you should understand the potential side effects (behavioral changes, blood pressure elevation and delirium). I do not recommend anyone try this concept in it's entirety until you know how each bit and part will affect YOU. Just because the concept may work for me or someone else, doesn't mean it will benefit YOU. 



:::::Maximizing GABA is ESSENTIAL to this, you will get anxiety if you don't keep your Adrenaline in Check::::

!!! This does not mean take massive doses of KLONOPINE or XANAX !!!

It means, naturally do everything to keep your GABA levels elevated, or do what it takes to keep GABA elevated. Otherwise these methods will not work properly.

One more thing, it is absolutely essential that you keep an Anti-Nausea drug - namely ZOFRAN on hand while experimenting. 
In fact DO NOT even BEGIN the application of ANY of this without that drug, you might want to take Zofran before even using the first compound. 




The GOAL of the Dopaminergic Pot of Gold, is to create a Euphoric and Intelligent state, resembling that of a Amphetamine Rush perhaps, but while maintaining BP and a healthy heart. This state of mind may rapidly increase feelings of Unlimited Power, and Invincibility, and will enhance your body and mind to a state - unprecedented. It represents one part of a "Perfect Chemistry". 


Read the WHOLE ARTICLE, and the Citations. 




I was reading through a topic on "Dr.Bob" one day ; a long discussion about the recreational/intentional enhancement of dopamine levels, it was interesting to find they had referred to this premise as "The Dopaminergic Pot of Gold". This isn't the first time it has been brought up either - people seem to see Dopamine as being an all-powerful neurohormone that transforms your conscience into that of a deity. Bluelight and psychedelic forums are two other notable discussion area's where I've seen this brought up.
I don't disagree. People have been trying to dig up this kind of information for a long ass time.

IN FACT, I am one of them, you might even say I've gone "above and beyond", being a natural perfectionist - I've longed to see the results of dopaminergic enhancement through every possible mechanism.


One is described below.
5-HT2A antagonism, now what does this do?
Well 5-HT receptors are SEROTONIN receptors, the 5-HT2A/2C are inhibitory upon dopaminergic neurotransmission - "notably in reward area's such as the Ventral Tagament (VTA) and Hypothalamus". The activation of these receptors are associated with increases in cortisol and prolactin - which also lower dopamine levels.

Besides enhancing dopamine, 5-HT2A/2C blockade is useful for another reason. Lowering Blood Pressure.
You see, when you activate 5-HT2A/2C - this in turn activates Phospholipase C and Protein Kinase C - both of these are vasoconstricting enzymes. (2)(3)(4)

We wouldn't want to have High Dopamine and high blood pressure anyway - would we? Depending on your Dopamine > Norepinephrine (NORadrenaline) conversion, this might under normal "dopamine enhancing circumstances" become a reality.





Posted by Brainbeard on July 2, 2009, at 16:14:09
 At the end of the rainbow? Perhaps. It has only lately occurred to me that, in my desperate and frantic searching for a way to enhance dopaminergic functioning, I have overlooked or at least wasn't aware of a particular way of raising dopamine (DA) (and noradrenaline (NA)) levels and/or firing, namely 5HT2A/C-antagonism. Stephen Stahl opened my eyes. I knew that a low dose of Prozac raises DA (and NA) levels in crucial parts of the brain, but I didn't know it did that because of 5HT2C-antagonism. I've experienced that low dose Risperdal, which I thought was supposed to help with anxiety, turned me into a social superman besides boosting my 'mental libido' (the part between the ears as opposed to what's going on below the belt) - without doing much for anxiety. I now understand that because of Risperdal's 5HT2A-antagonism, it indeed elevates dopamine levels, resulting in mentioned phenomena. There is a nice presentation by Stahl on the web where he explains how 5HT2A and -C-antagonism result in increased dopamine release. I can't give a direct link because it seems to be a subscription page; nevertheless, when you follow the following link and click on the first search result, you do end up in the presentation: http://www.google.nl/search?hl=nl&safe=active&rlz=1B3GGGL_nlNL255NL258&q=Schizophrenia%3A+From+Circuits+to+Symptoms+Presented+by+Stephen+M.+Stahl&btnG=Zoeken&meta= Quoting from the presentation: 'What receptor properties can enhance the ability of an atypical to improve mood and cognition? What does the 5HT2A antagonist property have to do with that? Normally, the serotonin neuron (...) talks to the dopamine and norepinephrine neurons and tells them to be quiet, to step on the brake. If you interfere with that, you don't inhibit anymore; and, if you don't inhibit anymore, you disinhibit, which is a fancy way of saying, "turning it on." So, to disinhibit means not another way to do it, but rather to turn things on. If you block the natural ability of serotonin to stop norepinephrine and dopamine release, you enable the dopamine and the norepinephrine to be released. So blocking this causes release.' And: 'What other receptor binding properties might enhance this ability, besides those of 5HT2A? We get into some speculation, but useful speculation. The 5HT2C receptor is also connected to the dopamine and to the norepinephrine neurons, and it also reduces those through gamma-aminobutyric acid (GABA) interneurons; if you block them, it also increases dopamine and norepinephrine.' For this reason, Stahl explains, low doses of both Prozac (fluoxetine) and ziprasidone (Geodon) can be activating, because they block 5HT2C and/or 5HT2A without much (or any) serotonergic (Prozac) or antidopaminergic (Geodon) action going on. Furthermore, 5HT1A-agonism seems to be essential to complete the trick: 'Any other properties? The 5HT1A agonist properties could be useful. Presynaptic actions could help antidepressant effects, and postsynaptic actions could help cognitive effects. Dr. Meltzer has done seminal work showing that you don't get these increases -- of the good, smart neurotransmitters of dopamine and norepinephrine, particularly dopamine -- unless you work through a 5HT1A receptor.' Stahl gives extensive descriptions of these phenomena in his Essential Psychopharmacology, fragments of which can be read on the web, for instance here: http://books.google.nl/books?id=cWbYxSfKN3cC&pg=PA351&dq=Stephen+Stahl+5HT2A-antagonism+dopamine+5HT1A+serotonin In Depression And Bipolar Disorder, he explains the link between 5HT1A-agonism and 5HT2A/C mediated DA release: http://books.google.nl/books?id=zqvVZOea2JAC&pg=PA120&dq=Stahl++stimulation+of+serotonin+1A+receptors+acutely+reduces+the+serotonergic+inhibition+of+DA (read the text UNDER the small text belonging to the picture). Here's a research abstract that shows that 5HT2A-antagonism revives SSRI-decreased noradrenergic firing: http://www.journals.elsevierhealth.com/periodicals/bps/article/PIIS0006322306006597/abstract So, all the moaning and whining about SSRI-induced apathy could once and for all be abolished if SSRIs would standardly get served with 5HT2A/C blockade plus 5HT1A-agonism. And this is where things get dirty. There ARE pure 5HT2A and/or -C antagonists, but they don't have enough marketing potential since as stand-alone's they're not very impressive. So they are only known under desperately unimaginative names like SR46349-B. The 5HT2A/C-blockers that HAVE been marketed are for the bigger part pretty dirty drugs, which is to day, they have affinity for a range of receptors and do a dozen of things simultaneously, often in a dose-related manner. The atypical antipsychotics (AAP's) are almost all characterized by 5HT2A-blockade. See this table for a comparison of antipsychotic beinding data: http://www.nature.com/npp/journal/v28/n3/fig_tab/1300027t1.html Risperdal, mentioned earlier, is a potent 5HT2A-blocker, but because it crosses the blood-brain-barrier, even at low doses it raises prolactin levels wildly. Let me assure you, hyperprolactinemia is not something to take lightly. 


It can cause tumors or make your bones brittle. In my case, it leads to gynecomastia, which isn't fun when you're not a travestite with Pamela Anderson as your role model. Zyprexa is an excellent 5HT2A and -C-blocker, but it's a much too strong antihistaminergic - what use is extra DA and NA when you're sleeping all day - and strongly diabetogenic on top of that. Geodon (ziprasidone) is an interesting candidate since it's a strong 5HT2A-blocker, a relatively strong 5HT2C-blocker, a weaker 5HT1A-agonist, AND its antagonistic touch of D2 is soft enough not to raise prolactin levels much or cause extrapyramidal symptoms even at therapeutic doses. Geodon is also a moderately strong serotonin and noadrenaline reuptake blocker. Stahl refers to it as sort of a mini-Effexor. Its withdrawal syndrome, though, doesn't seem to be very mini if you may believe the anecdotal evidence. Anyway, Geodon (ziprasidone) is an interesting candidate for augmenting SSRI-therapy in a low dose - perhaps less than 20mg would already be enough? At such a dose, the whole cascade of the drug's other actions would hardly yet be put into motion. An even more interesting candidate, in my opinion, would be sertindole, which is a potent 5HT2A/C-blocker that touches D2 only lightly in comparison. In contrast to Geodon, that has a very short half-life, sertindole has a long half-life and it's blocking effects on 5HT2A are reported to be long-lasting. Sertindole was temporarily withdrawn from the market after reports of sudden death and the like because of its tendency to prolong QT-interval; later studies revealed, however, that this tendency wasn't any greater than that of most other AAP's; Risperdal, for instance, is a worse offender when it comes to QT-interval-prolonging. Anyhow, the QT-interval-prolonging is dose related, and I think that even a 4mg dose (therapeutic dosage for schizofrenia is >20mg) would be enough for the goal I have in mind. Sertindole, sadly, is considered a second-line treatment and hasn't even been investigated, it seems, as an augmentation strategy for SSRI-treatment. So who will ever prescribe it for me?! Then you have the good ol' TCA's, of course, most of which throw in a bit of 5HT2A or -C antagonism among all the other stuff they're doing. You can see and compare their 5HT2A-antagonistic properties in this table: http://www3.interscience.wiley.com/cgi-bin/fulltext/121665024/main.html,ftx_abs#t3 When you remember the (A)AP-table, you will realize that the 5HT2A or -C antagonism of the TCA's is rather weak and will probably only come into full play at therapeutic rather than low doses. That's a pity, because at such doses the side-effects of TCA's are so severe that only the truly heroic stand their ground. Which leaves the rest tantalized. Amitriptyline, for instance, has perhaps the best ratio of SRI versus NRI versus 5HT2A (and -C)-blockade. But it's a stronger antihistaminergic than Zyprexa (see there), and it's a very strong anticholinergic, and a very dirty drug overall, so though certainly undeserved, it IS imaginable that some doctor's have called the drug 'rat poison'. To draw towards the end. My personal suggestion (towards myself, that is) for a fine antidepressant cocktail with both anxiolytic and stimulating and motivating qualities would be: sertraline (Zoloft) + sertindole or ziprasidone (Geodon) or, if those aren't available, Risperdal + Buspar (buspirone), the 5HT1A-agonist. On paper, it looks good. What do you think?

Trazodone or Remeron <-- both are POTENT 5-HT2A antagonists, only Remeron has affinity for 2C.


I think you are correct you insightful poster. Good to see kids are still learning!
Now to dig a little further.
The research on autoreceptors.

Dopamine auto-receptors, that is.




                                      2008 Oct;28(8):1480-90. doi: 10.1111/j.1460-9568.2008.06450.x. 
Chronic activation of the D2 dopamine autoreceptor inhibits synaptogenesis in mesencephalic dopaminergic neurons in vitro.

Fasano C1, Poirier A, DesGroseillers L, Trudeau LE.

 Abstract

Chronic blockade or activation of dopamine receptors is critical for the pharmacological treatment of diseases like schizophrenia, Parkinson's or attention deficit and hyperactivity disorder. However, the long-term impact of such treatments on dopamine neurons is unclear. Chronic blockade of the dopamine D2 receptor in vivo triggers an increase in the axonal arborization of dopamine neurons [European Journal of Neuroscience, 2002, 16, 787-794]. However, the specific involvement of presynaptic (autoreceptors) vs. postsynaptic D2 receptors as well as the molecular mechanisms involved have not been determined. Here, we examined the role of D2 autoreceptors in regulating the ability of mouse dopamine neurons to establish axon terminals. Chronic activation of this receptor with quinpirole, a specific agonist, decreased the number of axon terminals established by isolated dopamine neurons. This effect was accompanied by a decrease in dopamine release and was mediated through inhibition of protein kinase A. The decrease in axon terminal number induced by D2 receptor activation was also occluded when the mammalian Target of Rapamycin pathway of mRNA translation was blocked. Our results suggest that chronic activation of the D2 autoreceptor inhibits synaptogenesis by mesencephalic dopamine neurons through translational regulation of the synthesis of proteins required for synapse formation. This study provides a better understanding of the impact of long-term pharmacological interventions acting through the D2 receptor.

PMID: 18973573 [PubMed - indexed for MEDLINE]


What does this all mean...?
Well basically autoreceptors are the brain's own receptor based negative feedback system for dopamine; telling the brain "we are having too much dopamine activation, let's decrease and / or moderate the release of by this receptor). It's a built in wiring "insurance policy" ensuring that dopamine increases will always be associated or followed by a decrease.






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Point is. Dopamine D2 has two receptor subtypes, pre-synaptic D(2) Short (S) - "D2S" - receptors which INHIBIT dopamine - and Dopamine D(2) Long - "D2L" which activate their own actions. 



In light of this - there aren't many compounds that actually block dopamine auto-receptors besides Amisulpride, and only at lower doses, at higher doses it acts as an AntiPsychotic drug and blocks them all. Point being - Dopamine D2 has two receptor subtypes, pre-synaptic D(2) Short (S) - "D2S" - receptors which INHIBIT dopamine - and Dopamine D(2) Long - "D2L". Blocking ONLY D2S's - due to the fact that there aren't many compounds AVAILABLE - you would certainly need to experiment with low dose Amisulpride. However there are "pathways" that need to be ensured before we even get to that.


Also - IN ORDER TO UNDERSTAND DOPAMINE PRODUCTION AND FEEDBACK - we need to understand the CENTRAL MECHANISM and following effects of D(2) like RECEPTORS. 

SPECIFICALLY, Dopamine D(2) receptors INHIBIT adenlyl cyclase - which then INHIBITS - CYCLIC ADENOSINE MONOPHOSPHATE (cAMP) - which then the decrease of this (since cAMP normally stimulates the Enzyme TYROSINE HYDROYXLASE) decreases TYROSINE hydroxylase ; the enzyme by which dopamine is produced from the amino acid TYROSINE. Cyclic AMP is positively correlated with Protein Kinase A activation.

Thus - CYCLIC AMP is KEY to activating dopamine activity, and since Cyclc AMP is related to THYROID function, there is a STRONG link between associated thyroid hormones (such as T4 and T3) and dopamine synthesis.






Brain Res. 1988 Jul 26;456(2):302-9.

Evidence that adenosine A2 and dopamine autoreceptors antagonistically regulate tyrosine hydroxylase activity in rat striatal synaptosomes.

Onali P1, Olianas MC, Bunse B.

Abstract

Incubation of rat striatal synaptosomes with the adenosine receptor agonist 2-chloroadenosine (2-CADO) produced a concentration-dependent increase of dopamine (DA) synthesis (about 50% of control value). The effect was not additive with the stimulation produced by either 10 microM forskolin or 2 mM dibutyryl cyclic AMP. Pretreatment of striatal synaptosomes with 2-CADO produced an activation of tyrosine hydroxylase (TH) which withstood washing and lysing of the tissue. This activation was largely independent of the presence of Ca2+ ion in the preincubation medium and, when analyzed as a function of different concentrations of the pterin cofactor 6-methyl-5,6,7,8-tetrahydropterin (0.08-0.4 mM), it was associated with an apparent increase in the Vmax of the enzyme. Quinpirole, a selective D2 DA receptor agonist, reduced control synaptosomal DA synthesis and caused a persistent inhibition of TH activity. When added together with 2-CADO, quinpirole depressed the stimulation of DA synthesis and TH activity produced by the adenosine analog. The effect of quinpirole was stereospecifically antagonized by the D2 DA antagonist sulpiride. Quinpirole also inhibited the activation of TH elicited by a submaximal concentration of forskolin, but not that produced by dibutyryl cyclic AMP. The inhibitory effect of quinpirole on basal and 2-CADO-stimulated TH activities was mimicked by DA. These results indicate that presynaptic DA autoreceptors and adenosine A2 receptors interact antagonistically in controlling DA synthesis in rat striatal synaptosomes presumably by exerting opposite inputs on a presynaptic adenylate cyclase system. PMID: 2905190 [PubMed - indexed for MEDLINE]


Now there are many ways to increase Cyclic AMP.
One of those is by supplementing with a compound called "Forskolin" - a direct adenylyl cyclase ACTIVATOR. As one of the supplements that activate adenylyl cyclase - we will expect as seen above, an INCREASE in cyclic AMP. Now we have more tyrosine hydroxylase - and thus more DOPAMINE.

As another big note ::: None of this will apply if you aren't getting the necessary amino acids in your diet!!!! 
Therefore, if you attempt to apply any information in this article, remember that PROTEIN intake is ESSENTIAL! I suggest eating a handfull of peanuts and getting the rest of your protein from lean meat.


Let's review so far.

Methods of increasing dopamine activity.

  • Blocking/Antagonizing 5-HT2A / 2C receptor activity.
  • Blocking auto-receptors using low - dose amisulpride.
  • Increasing Protein Intake
  • Supplementing with Forskolin.

The next one is kinda like hitting two birds and a squirrel with one jagged stone.



Why Yohimbine...?

For good reason - it blocks many serotonin receptor subtypes that have detrimental effects on dopamine synthesis and also cause vasoconstriction. Some of these are the serotonin 5-H1(B) receptor, 5-HT1(D) receptor and 5-HT2(B) receptor. That means that by blocking serotonin's effect on these receptors, Yohimbine allows for both vasodilation and dopamine release.


Second to all of this - Yohimbine blocks Central Alpha-2-receptor's VERY POTENTLY.
By blocking Alpha-2-Receptors, dopamine release is enhanced.





So just with the triple triple cocktail of Yohimbine, Trazodone (or Remeron) and Forskolin we have a super boost in dopamine. Add in ami sulpride at very low dose - and we've enhanced it even more.


Now let's move to other aspects of dopamine's breakdown.



MONOAMINE OXIDASE ACTIVITY

Monoamine Oxidase type A - is an enzyme that breaks down Catecholamines/Monoamine's; dopamine, epinephrine, norepinephrine and serotonin. Monoamine Oxidase also has a type B ; and this breaks down Dopamine and Phenylethylamine ONLY.

To maximize dopamine, both of these enzymes should be inhibited.
However, we are starting to cross the red river here as far as side-effects.
Always keep an alpha-blocker on hand, no-one should be applying any of these concepts without having an anti-nausea/sympatholytic drug on hand.

VERY IMPORTANT : Wiping out MAO-A and MAO-B does NOT require drugs AT ALL. 
They are ANTIOXIDANT based enzymes, the more antioxidants you have in your blood, the less of these enzymes that break down dopamine and EPI etc.


To inhibit MAO-A and MAO-B ...you only need two products.
Syrian RUE and KAVA KAVA.

Syrian Rue can be found here ---> Herbs of the Gods
KAVA KAVA can be found ---> HERE









NEXT ASPECT OF DOPAMINE BREAKDOWN...



DAT (Dopamine Transporter)
To inhibit this transporter which will then allow for more dopamine to stay active (and not get used up quickly) - we need transporter inhibitors (specifically DAT and NET inhibitors).

NET is norepinephrine transporter...why inhibit this? Because dopamine is INACTIVATED by NET in certain area's of the brain...very important area's in cognitive processing and emotions such as Prefrontal Cortex. So to REALLY maximize dopamine...we would have to block both DAT and NET...which locks both dopamine and norepinephrine into the synapse. ALWAYS KEEP AN ALPHA BLOCKER ON HAND. So you don't get high BP....you should be only the HEALTHIEST of an individual to try these methods out. 


To inhibit both DAT and NET...

We only need one or two HERBS.


Kava inhibits both NET and MAO-B, while Catuaba inhibits DAT.


Now with all the methods listed so far.

We only have ONE method left..one little trick left in maximizing dopamine to absolutely SUPRAPHYSIOLOGICAL concentrations.

A transporter called "VMAT".


VMAT is what Amphetamines bind to. But we don't need amphetamines.
We only need one substance. The natural form of amphetamine already present in our body.

PEA - Phenylethylamine. If we take this orally, while inhibiting MAO-B...then we have already done our deal with the devil..because MAO-B inhibition ensures PEA stays around...which means we ENSURE VMAT Inhibition!


There is one little feeback mechanism NOT mentioned yet...


NMDA-receptors. When you interfere with NMDA glutamate receptors, you will actually indirectly block the reuptake of dopamine, leading to enhanced dopamine Activity.






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