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Sunday, July 12, 2015

SFME-OX -A Ploy to Re-Engage the Efficiency of the Mu-Opioid System; Tolerance Uncovered! (Enhancing / Re-Sensitizing mu-Opioid Receptor System)

This article has been exclusively written for TrueLIFE Research - TeamTLR.com and to foster further progress within opioid system research and in reinforcing the significance of the system in current medical dilemmas


----------SFME-OX (Mu-Opioid Sensitizer/Tolerance Reversal) can be purchased of 99%  PURITY @TeamTLR below------------------------------------------------------------------------------------------------------



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Since the late 1990's to early 2000's a predictable problem in those needing strong pain medication has been the eventual tolerance(1)(2) and, when looking 'under the microscope' ; neural de-sensitization of the receptors was uncovered(3). This has provoked much research and has created a dilemma in the medical profession, forcing caregivers and Doctors alike, to adjust or augment the dose of opioid-like painkillers, often unexpectedly(4)(5)

In severe trauma and other debilitating conditions such as multiple sclerosis, cerebral palsy co-existing with injury, and in many other circumstances where severe , neurological or muscular pain endures, there aren't many alternatives to narcotics(at least equivalently effective ones)(6)(7). In dentistry, after a surgery or operation the same is true regarding alternatives, limited indeed(8)(9). The difference between dentistry and GP complaints?  : frequency. People usually go to their primary doc's more than their dentist, and more severe cases of pain are referred to specialists where much testing is completed. Still, in all of this, the pain has to be taken care of in order for the patient to fully cooperate with his/her medical advisory - one isn't likely going to be very motivated to go anywhere if they are in so much pain irrespective of tried remedies and such(10)(11).

Now imagine a scenario in which a severe sports complication or an elderly falls or has some other traumatic event causing injury, and their opioid pain medication which is supposed to do the trick - starts whittling down in effect, and to worsen the ordeal - higher doses are creating increased side-effects! Maybe even as intolerable as the pain itself...
Or consisting of increased pain due to the med losing it's effectiveness!!



What's the solution? Because the bridge certainly doesn't look too sturdy from here.



We need something that will allow victims of debilitating illness or severe injuries to utilize at maximum efficiency, the lowest possible therapeutic dose of their opioid pain medication...else , we are just lost and heavily restricted with worry , fear, and limited options. We need something that can act as a regulator of the entire system it works on, or at least the part that contracts to the alleviation of pain.

Now while some preliminary research was done a few years ago regarding re-sensitizing the responses to opioid pain medications, it was just that, very VERY preliminary..(12)(13).and probably not the best case made in favor of overall efficacy. However, new research is being presented by TeamTLR which aims to elucidate the root problem, and provide a potential solution that will provoke a new awakening in the pinnacle of medical research with regard to these issues.

The research compound is valuable and a huge step forward and goes by the name SFME-OX.
SFME-OX:Selective Filamin A MOR-System Enhancer Optimized Xtract binds Filamin A in a highly selective manner that demonstrates the effect of markedly reducing Mu-Opioid Receptor System (MOR-S) tolerance.  

SFME-OX further demonstrates a marked reduction in inflammatory cytokine production.

(
Cytokine's are small proteins involved in cell-signaling and a collection of them are involved in specific growth related processes as well as with inflammatory modulation. However, abundance of them relates to their significance and too many or too much production of them often leads to inflammatory responses which can lead to brain and joint inflammation.) 


Most NSAID's don't directly antagonize but indirectly reduce cytokine mediated responses and other pain relievers may offer some relative protection but usually do not go against the grain and reduce the source of the issue(!).

Source Plant:  Proprietary Lobelia species.


Animal Data:


In vitro data shows selective pM affinity binding at the Filamin A protein pocket that produces an marked enhancement MOR tone within an upregulation of MOR expression.  In vivo efficacy in murine models has been demonstrated eliciting a reversal of downregulation created via mu-opiate administration thus potently reducing tolerance to mu-opioid receptor agonist agents as demonstrated.

(This is revolutionary, by preventing or reversing the mu-opioid related downregulation, sensitivity to the medications are maintained or re-instated, and so by doing this, we have caught a major 'therapeutic break' - finally making our way into solutions that will lead to even more groundbreaking solutions for trauma, injury and autoimmune disease management.)


Future Human Clinical Trial Protocol and Projections:


SFME-OX is anticipated to provide potent upregulation of the Mu-Opioid Receptor sensitivity/expression at dose arms of 10mg and 20mg to be administered once daily.  Said administration is projected to provide a rapid restoration of sensitivity to opiate therapeutic agents and allowing a marked reduction in dosage to provide superior positive effects with reduced adverse effects.  An optimum course is anticipated to be via a 1 week of usage followed by 1 week of discontinuance alternating schedule. 


As you can see with the overview above, this is more than just evidence, but rather; an active trial that is long over-due - and the human trials will become the brew for the future insights and management of chronic pain and other disorders where opioid-systems or their malfunction plays a critical role. This may expand to even mental disorders such as depression and anxiety, to which mu-opioid receptors also play a huge role(14)(15)(16)(17).


Which brings me to my last point, because we have already seen the devil of de-sensitization with many anti-depressants (although in these cases, de-sensitizationd is often postulated to be beneficial) - the worry that would come with developing mu-agonists for depression or anxiety would stem from the possibility (or even probability) of fairly quick tolerance(18)...where most anti-depressants on the market now increase in effect the longer you take them (19) - an agonist at the mu-receptor would most likely be the opposite(20)..given they are a major GPCR (G-Protein-Coupled-Receptor).

So SFME-OX represents a future and present research tool for these dilemmas as well and the progress we make now will be as vast considerations for the future developments and even as a course of augmentation not prior seen...the unprecedented value in MU-SYSTEM SPECIFIC re-sensitization will parallel the benefits (but stand as the respective equivalent thereof) of 5-HT1AR desensitization in anti-depressant therapy(21)(22).

So both on a Central Nervous System and on a peripheral level, this critical method of re-sensitizing and enhancing the mu-opioid-complex function will prove to be a novel but long over due approach to the current treatment regimens or augmentation of current treatments in which will provide a better outcome for patients with a multitude of health complications sensitive to opioid-receptor function.



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