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Thursday, February 12, 2015

5-HT1A Antagonists; Their Function, Benefits and Where to Buy Them Online

UPDATE: WAY 100 635 is now available.

  • This is a 5-HT1A antagonist known as the "gold-standard", chemically unique, and also has dopamine D4 agonist properties with no affinity for D2 autoreceptors.
  • Studies show 10 mg minimum as a dose for humans and up to 45 mg at the maximum, effects may very per person.
  • Provides cognition enhancing and may substantially increase nervous system strength and workout motivation.
Certainly, besides the histamine H(3) autoreceptor/heteroreceptor - there is not one other G-protein coupled receptor, that has fascinated me quite like the serotonin 5-HT(1)A receptor.

This receptor is extensively studied because of it's well-known role as a central regulator across many neuronal networks - it is heavily intertwined with neuro-endocrine networks and plays a central role in the pathophysiology of depressive disorders as well as anxiety disorders and addiction(1) (2).

Particular interest in it's neuro-endocrine roles began in the late 80's to early 90's , with agonists such as 8-OH-DPAT and flesinoxan showing to release cortisol , prolactin, beta-endorphin and oxytocin(3) (4).

Since these neuro-hormones and peptides are distinctly involved in the regulation of GnRH (GonadoTropinReleasingHormone) neuron activity, it seems reasonable to consider the use of antagonists to increase testosterone levels(5)

Additionally, 5-HT(1)A antagonists have shown to be useful in alleviating SSRI-induced sexual dysfunction ; and the studies display a primary role of this receptor in inhibiting the process of penile erection {SEE HERE}.
This includes the erectile responses induced by dopamine agonists(!)


Interactions with specific hormones such as cortisol and estrogen have been documented. On the inverse, cortisol seems to regulate the amount of 5-HT1A activity (6) , estrogen seems to downregulate both synaptic forms of this receptor  (7)(PRE-SYNAPTIC & POST-SYNAPTIC). Testosterone and Androgens on the other hand, seem to enable 5-HT1A receptor function and / or normalize them during times of stress(8) (9) (10).

Before we get any further, you have to understand the difference between pre-synaptic and post-synaptic receptors.


Pre-synaptic serotonin 5-HT1A's are strictly AUTORECEPTORS (11) - that means they decrease the release of their given neurotransmitter or act on nerve terminals to inhibit the release of separate neurotransmitters.

In the 5-HT1A receptor terminals, they tell the brain to decrease serotonin release - acting as a sort of homeostatic feedback so that when the brain has too much serotonin - it can moderate/reduce it by these receptors.

Additionally, these 5-HT1A receptors are also somewhat intertangled with GABA networks...GABA is the primary inhibitory, and very calming neurotransmitter in mammals and humans. Serotonin specifically inhibits GABA - and especially does so in the PVN; Paraventrical Nucleus of the hypothalamus(12).....this effect likely accounts for some of the dopaminergic enhancement that may occur by stimulating the pre-synaptic receptors.  Conversely, antagonizing or blocking the pre-synaptic 1A receptors would enhance both GABA and serotonin..

                  POST-SYNAPTIC  5-HT1A RECEPTORS 

Post-Synaptic 1A receptors on the other hand - are expressed ubiquitously in the hypothalamus and hippocampus (rather than broadly distributed), their role seems to be a major focus for depression and anxiety. Post-Synaptic receptors (5-HT1A) tend to be anxiogenic (anxiety provoking) ( 13 ) and to inhibit male sexual responses to the presence of a female and thus inhibiting sexual behavior(14). Additionally, the activation of these receptors may have anti-depressant effects or paradoxically, hastening depression. An article by the scientific american states that blocking the 5-HT1A is the next phase in development of novel anti-depressant compounds or synergists for current anti-depressants(15).

{Analogy with 5-HT1A Antagonists}

With these receptors, an increasing large barrier between becoming the ultimate male can be seen - additionally, aggression is usually REDUCED by 5-HT1A activation(16). However, these acts of aggression are also prominently dependent on psychology and social status.

The reasons we want to target and block 5-HT1A receptors are not just to alleviate depression or help prevent it from occurring , but also to disable negative feedback from corticosteroids, and yet to enable what I refer as the front-flipping, "keep going" cyclical gonadotropin continuance signal.

In simple terms, it means to enhance pulsatile secretion of both nitric oxide testosterone and to make one more immune to negative feedback and yet a better responder to things like hCG or other natural "testosterone boosters"(17) (18).

Because these receptors are heavily involved in both "regulating" dopamine, glutamate and testosterone output - the benefits of blocking them would include alleviating central nervous system depression, enhancing hormone production, and especially improving cognitive and intellectual functioning.



  • Alleviate depression(!).
  • Boost testosterone(!) (!).
  • Increase glutamatergic / NMDA mediated neurotransmission(!).
  • Increase nitric oxide (!).
  • Help to cure stimulant dependence.
  • Reduce anxiety(!).
  • Improve memory and some signs of dementia(!).
  • Increase strength and aggression(!).
  • Increase self-grooming / alleviate laziness(!).

UPDATE : WAY 100 635 is now available HERE. This compound is known as the "gold-standard" of 1A antagonists. It also has dopaminergic effects.

Your ideal candidates would be LECOZOTAN & WAY 100 635, I have not found a retail source yet...but when I do - I will update this article.

Additionally, way 100 635 functions as a dopamine agonist at the D(4) receptor - so that would be ideal for enhancing hormone function / libido aswell increasing oxytocin by modulating the serotonergic systems.

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