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arylcyclohexamines

Phoenix_rising

Phoenix_rising

Bluelighter
Joined
Sep 22, 2010
Messages
592
Would it be possible to make a 3-hydroxy-pce and would it work? The hydroxy to replace the methoxy?
 
Sure, why would that be impossible?

3-HO-PCP isn't supposed to be very good though, so this likely applies to 3-HO-PCE as well.
 
roi said:
Sure, why would that be impossible?

3-HO-PCP isn't supposed to be very good though, so this likely applies to 3-HO-PCE as well.
Click to expand...

I remember reading 3-HO-PCP actually has affinity for the u-opioid receptor, not anecdotal bs, but I can't find it ATM. I may be wrong, someone may be to help one way or the other.

But to answer OP, yea, totally possible
 
Both 3-HO-PCE and 3-HO-PCP are known and active, both have been available shortly as well.

Just use google 8)
 
Gonna move this over to Neuroscience and Pharmacology Discussion :)
 
Swap the cyclohexyl ring, use a p-Tetrahydro-2H-thiopyran ring. Studied & works. Swapping ketone for methyl for more potent compound after seperation of isomers.
 
Oh yeah, just thought really weird but of course it is 3-ho-2'-oxo-pce. Will very probably have more or less the same opioid affinity, think MXE undoubtedly has such - not very strong and with a ceiling effect so no danger for overdose but for sure. And formation of this metabolite is done by CYP2D6, so individually dependent like DXM, not everyone gets it.
 
Strong as an opioid or in terms of general potency? Because I think there shouldn't be higher opioid to nmda ratio or you will head into tolerance and dependency.
 
I'd really like to see that evidence that 3-HO-PCX tend to be significant opioids, to ensure that this is not all originating from hearsay out of adder's assays and theories.

It's no surprise if 3-HO ACH's are generally pretty potent as NMDA antagonists - whatever the trapping - because it fits the pharmacophore best at that position having the acidic hydroxy of (N-methyl-)aspartic acid / glutamate.
Even if they aren't opioidergic, IIRC 3-HO-PCP sounded pretty narcotic.

I personally wonder about these + the K-like halo analogues and also whether they make for high-trapping NMDA antagonists and finally: whether high trapping ones imply big K-like magic potential.
 
I think there was someone here who sampled a bunch of related compounds two years or so ago and stated 3-HO-PCE to be a strong opioid at low dosages, but this is just anecdotal of course. Will look for the thread later. I have tried either 3-HO-PCP or PCE too, think it was PCE but unfortunately I don't remember it exactly. Had a distinct stoning quality that wasn't really dissociative, not typically opioid either but more of the latter, best comparison is AH-7921. Were quite low dosages though.

Would you mind to explain what the trapping means? Is it correct that memantine is a low-trapping one then, and that high-trapping means more pronounced dissociation and mental effects / magic?
 
Solipsis said:
I'd really like to see that evidence that 3-HO-PCX tend to be significant opioids, to ensure that this is not all originating from hearsay out of adder's assays and theories.
Click to expand...

The Ki of 3-HO-PCP for MOR is ~80 nM, whereas other PCP analogs bind with Ki values exceeding 10,000 nM. So addition of a 3-HO group does seem to increase MOR binding affinity to moderate levels.
 
Thanks ser2a

dopamimetic said:
Would you mind to explain what the trapping means? Is it correct that memantine is a low-trapping one then, and that high-trapping means more pronounced dissociation and mental effects / magic?
Click to expand...

Can't explain it better than this:

Another important reason for the variation in effect lies in the off-rate of the compound. This phenomenon has been termed “trapping block”.18, 19 Compounds with a slow off-rate such as ketamine (86% trapping) and MK-801 (almost 100% trapping) are examples of high-trapping antagonists. When the glutamate has dissociated from its binding site on the NMDA receptor, the ketamine remains trapped in the, now closed, ion channel thus causing a prolonged tonic blockade which disrupts both physiological and pathological function. In contrast low-trapping (fast off-rate) antagonists are able to escape from the channel before it closes, thus allowing some preservation of physiological NMDA function, and hence fewer side effects. For example the compound memantine (50–70% trapped) has minimal sedative or psychotomimetic effects. It is a low affinity open-channel blocker with a fast off-rate. It therefore only blocks NMDA channels which are open for a pathologically prolonged time, and has minimal effect when the NMDA channel is only transiently open, as occurs in most physiological states. In many ways this mechanism is analogous to the effect of persistent sodium channel blocking antiepileptic drugs.20 The net result is an NMDA blocker without appreciable anaesthetic effects.
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http://www.trendsanaesthesiacriticalcare.com/article/S2210-8440(14)20006-2/fulltext

But whether MK-801 qualifies as magical I couldn't say. Debilitating though apparently. :)

Seems worth evaluating off-rates for dissociatives being used and their likeability for each of us. Is isophenidine particularly high trapping for example?
Maybe one pharmacological property of a drug is not enough to correlate it with sought effects, esp with complex acting drugs like dissociatives but a 'profile' helps understand what people are looking for. Not saying that we all want the same, but some effects are popular.. ;)
 
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Solipsis said:
Maybe one pharmacological property of a drug is not enough to correlate it with sought effects, esp with complex acting drugs like dissociatives but a 'profile' helps understand what people are looking for. Not saying that we all want the same, but some effects are popular.. ;)
Click to expand...

I would guess that as you move across a single structural family of NMDA antagonists the %trapping probably stays fairly constant. In the 1980s-1990s, many PCP analogs were tested in rodents and significant correlations were found between behavioral potency and PCP site affinity. If there was wide variability in %trapping then it would be difficult to find a correlation between potency and affinity.
 
Going off memory here. 3-HO-PCE was available from a reputeable vendor once, turned out that it was a lot less potent than expected. I think that at least 50 mg was needed for just mediocre effects. It wasn't deemed bad per se, just very pricy per dose. The authenticity was questioned due to the low potency, but it turned out it was the real deal.

4-HO-PCP has a couple of reports here on bluelight, it's never been sold by vendors to my knowledge, so it's all probably been personal custom synth's. At least one or two of the reports were very negative, and reported physical malaise and dysphoria at pretty low doses. I might google when I have time so to supply links, if not for anything else, then just to see if my memory is correct ;)

Btw. We need more short acting arylcyclohexylamine RC's imo. Ketamine really has that perfect duration for a dissociative, if you ask me.
 
3-HO-PCP had much more opioidish activity in the few trials when I tried it. Yet had the same issue with random muscle tension on both that and 3-HO-PCE. Also if I'm not mistaken Incunabula, that was just a very poor synthesis (Please correct me if I'm wrong on this part). It'd be nice to know more about these compounds. I would /presume/ both of them have some opioid activity. Yet that's just me guessing. Also sense we're on the topic of 3-HO-PCX's. 3-HO-PCPy... would be interesting.
 
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