Methoxetamine's Therapeutic Value

[PsychedelicPeptide]

This Glyx-13 peptide is pretty interesting. I'd be it is active via intranasal administration, given the small size and likely dual hydrophilic/hydrophobic properties it has (sequence Thr-Pro-Pro-Thr-amide). I wonder if they are pursuing additional structural work to find a better candidate to permit oral dosing and/or better potency...

 

[PsychedelicPeptide]

I'm amazed that a peptide drug like Glyx-13 is able to pass the blood-brain barrier.

You shouldn't be... for one, they give the stuff by IV in all the preclinical work and the running trials: http://www.clinicaltrials.gov/ct2/show/NCT01234558?term=glyx-13&rank=2

Actually there is one recruiting participants right now for drug-resistant depression (see above link, or if it doesn't work just search glyx-13 at clinicaltrials there is another study in healthy people too!) if anyone is interested. =)

But it has hydrophobic (Pro and Thr) and hydrophilic (Thr OH) qualities (sequence is short too: Thr-Pro-Pro-Thr-amide) and probably a rigid structure due to the Pros which are what you really want to be able to pass. And IV administration guaranteed helps ensure it gets up there effectively.

---------------------------------------------------------------------------------

On another note this peptide sounds a lot like that supposed nootropic peptide Semax (sequence Met-Glu-His-Phe-Pro-Gly-Pro-amide), which I found to be pretty lousy in my own trials. A few of the papers come to the conclusions about Glyx-13 having antinociceptive and neuroprotective properties, and that it may be useful for treating ischemia and stroke symptoms, just like they do in the Semax papers.

So I wonder how useful it will end up being. At least there is some evidence to support a known site of action for Glyx-13 though, whereas Semax no one has published any knowledge of it.

 

[AndroidsDreamofBTC]

To the OP:

Why not simply take small bumps (10mg<) of MXE throughout the day? I find that helps me with anxiety and motivation.

 

[fastandbulbous]

^ Because that's well down the road towards fucking with your short term memory etc. (10mg is an effective/active dose & repeated several times a day - say 50mg/day - is going to lead to tolerance).From what I've read in this thread, people referring to theraputic use seem to only want to dose a couple a times a month, so there isn't a constant plasma level of the drug ('cos that when the problems with side effects begin)

 

[ebola?]

Actually, and this is corroborated by some research, multi-daily, low dose dosing with dissociatives for ~2-4 days, and then cessation, appears dramatically effective (better than large, single doses taken more rarely). It seems that there is a chain of downstream effects (as of yet not entirely clear), including changes in AMPA receptor expression, hippocampal to PFC signalling, changes in levels of BDNF production, and who knows (my memory is failing on some of this).

When I gave this a try, the dosing schedule was on the order of 10-12 insufflated mg of K, every hour and fifteen minutes or so. It didn't resemble getting high AT ALL. In fact, i was really glad when I was done with my 2.5 days.

ebola

 

[ebola?]

Oh....anyone got a link to binding affinity screenings for methoxetamine? I've heard conflicting things re: DA and mu-opioid agonism .

 

[Limpet_Chicken]

I think it would be an excellent tool for those wishing to quit opioids.

I've started using it in cycles, periods on, and off, at low doses, maybe a match-head sized bump or so whenever I feel withdrawals, I'm on a rx, for chronic pain, and my use is to lower tolerance, I won't be quitting the pain meds any time soon, not unless my knee can be fixed at least, but it allows for my rapidly dropping down to a fraction of my normal opioid dose with no withdrawals, staying there, dropping it lower still, going off, for a very short time (as short as I can manage, without having to deal with the knee pain and being unable to get around)

No cravings, no nothing. I think this, is where MXE could shine, not as an antidepressant. And its definately a lesser evil than H addiction, for example.

 

[fastandbulbous]

Actually, and this is corroborated by some research, multi-daily, low dose dosing with dissociatives for ~2-4 days, and then cessation, appears dramatically effective (better than large, single doses taken more rarely). It seems that there is a chain of downstream effects (as of yet not entirely clear), including changes in AMPA receptor expression, hippocampal to PFC signalling, changes in levels of BDNF production, and who knows (my memory is failing on some of this).

When I gave this a try, the dosing schedule was on the order of 10-12 insufflated mg of K, every hour and fifteen minutes or so. It didn't resemble getting high AT ALL. In fact, i was really glad when I was done with my 2.5 days.

ebola

I've found (for me) a day of taking low doses once a month (say 40mg spread over 6 doses) pretty much halts depressive episodes of my bipolar illness. Have to be careful though as taking more or for longer increasses episodes of hypomania (which sometimes verge on full blown mania), which while they might feel good to me, puts an incredible strain on my family as megalomania begins to set in. Also, the day of taking the doses, if I do anything, I have crap recall of (which has lead to some things being misplaced for months)

It's definitely a blessing and a curse wrapped up in one molecule!

 

[Fried Man]

the antidepressant effect of NMDA channel blockers is complex, there is the short term mood lifting effect which is probably dopaminergic, there is the longer term more powerful AD effect which is mediated through some different mechanism (probably through growth factors) and this effect persists long after dosing and long after the drug is detectable.

http://archpsyc.ama-assn.org/cgi/content/extract/67/11/1110


Using regular doses of NMDA channel blockers as an antidepressant is not only pointless it is very unwise, these are not benign substances they disrupt a lot of important neurological functions including short term memory, they also seriously impair motor function, you should not drive or operate machinery under the influence of even a low dose.

MXE as a prescribed antidepressant?
There is next to no chance of any of these old style NMDA antagonists making it as antidepressants, the side effect profile is not acceptable, neither is the psychosis caused by acute overdose or chronic overdose (dosing at a rate that is higher than the clearance rate) or just at random. MXE appears to have significant dose to dose variability and be rather unpredictable, like PCP in its effects. There is also not a single reason to assume that chronic use of MXE is any safer than chronic Ketamine use, which leads to permanent physical and neurological changes.
Finally MXE or any of the related aryl cycloheyxlamines will not make it as medicines because they are tarnished. They were put out into the RC market without first having been put through the legitimate channels so irrespective of their purported medicinal benefits they will be labelled as first and foremost drugs of abuse drugs without any recognised medical utility. They will then be banned. Once they are banned they will never be investigated as potential therapeutics it is simply too risky too bureaucratic and too expensive to carry out clinical trials with Schedule 1 substances. By putting these substances out into the RC market to make a quick buck, the people behind MXE and similar, despite their high minded words to the contrary have killed these substances and destroyed any future they may have had. Slash and burn.

People seem to be confusing the dissociative and inhibition reducing acute effects with the true AD effects, they are not the same at all. People who justify regular use as somehow being antidepressant are unlikely to actually be depressed, rather they seek a continuous drug induced altered state of consciousness which is not achievable due to tolerance and is inadvisable. MXE appears to be rather less effective than ketamine as an antidepressant in the irregular shock dose (insult) regime.

until it is banned MXE is a semi-legal novelty. It is not likely to be a medicine in waiting.

Wow you completely brought me down. I totally feel the same way as the original poster. I thought mxe could be a better adhd drug than vyvanse if designed the same way.

But couldn't you argue the same about pharmaceutical medicinal/therapeutic amphetamines vs illicit crystal meth ?

 

[Fried Man]

Yeh my friend uses mxe for adhd and feels it's better than vyvanse, which is the 2nd best drug for his adhd.

He self medicates with cannabis and opiates for adhd symptoms as well and to use for motivation and creativity. He knows he gains lil from cannabis and opiates and that they do more harm for his adhd and overall happiness and productive lifestyle.

He found that Mxe helped opiate withdrawal more than any other substance (usually amphetamines and cannabis to combat opiate withdrawal & depression) and helped him not crave and stay off opiates. He talks about how he literally feels different when it comes to decision making. It's easier to not sink into junkie habits while using mxe therapeutically. The will power and control seem short lived though. Usually 1-3 small doses a day is needed to control will power & impulsiveness. Anti depressant and social anxiety effects are felt and valued as well. Feels extremely emphatic and in touch with people and feelings more too. Seems to feel extremely extroverted and gullible at times with people and friends. It seems like mxe is a wonderdrug for my friend. Improves life in almost all aspects. Just gotta keep the doses low . . .

It's like being a functional slightly autistic person with the dissociative aspects always in place he imagines. He thinks some people are born this way, have a more dissociated brain structure/personality/thought process. He prefers this lifestyle to his natural adhd state of mind and brain . . .

Non stop binges of mxe def send him into manic episodes and give him grand delusions / megalomania. But low doses can feel extremely therapeutic for him.