• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

dissociatives of the future

Well yes you have something there.
Do you know what happens with substitution of various functional groups elsewhere on that cyclohexyl ring, their activities? :)
 
According to the arylcyclohexylamine SAR on rhodium the cyclohexane ring can be substituted with either methyl or ketone groups, at either the 2 or 4 positions, so you could play around with various combinations.

A ketone at the 4-position of the cyclohexane ring is supposed to boost opioid activity, so maybe PCP substuituted with a ketone at the 4-position of the cyclohexane ring and a chlorine at the 2-position of the phenyl ring might be good, should be a strong analgesic at any rate but whether that would make for a superior recreational drug is hard to say.

Really some inspired chemist who really likes these kind of drugs needs to do a PIHKAL type project with all the PCP/ketamine analogues, there are far too many possibilities and factors involved to easily predict which ones might be better as recreational drugs. Although I'm sure whoever did the research at Parke Davis back in the 60s would have an idea or two about what ones might have the most "abuse potential"....
 
can ketamine have a ketone or ketone replacement at the 2 position? like...
2-(2chlorophenyl)-methylamino-2-cyclohexan-2-one OR 2-cyclohexan-2-ol
 
Last edited:
mad_scientist said:
Really some inspired chemist who really likes these kind of drugs needs to do a PIHKAL type project with all the PCP/ketamine analogues, there are far too many possibilities and factors involved to easily predict which ones might be better as recreational drugs. Although I'm sure whoever did the research at Parke Davis back in the 60s would have an idea or two about what ones might have the most "abuse potential"....
Click to expand...
Exactly what I'm thinking! There might be a lot of potential in the ketamine anlogs.
As I already wrote, Deschloroketamine (MPCH) is very different in its action than ketamine: doubled potency, but nearly ten times longer duration and less desirable effects.
But all that research on ketamine analogs has already been done, at least in animals, in the research that led to the development of ketamine.
It would be prudent to first obtain all available data on the known and tested compounds before starting such a project, in order to see which ones are worth testing by an experimenter and which ones are inactive or dangerous.
No one would make a dozen of analogs only to find out that most of them are inactive, or worse, toxic.

Please, if someone here has access to papers on ketamine analogs, consider sharing them, I am sure a lot of people are as interested in them as me.
I know that somebody posted about how removal of the chlorine atom and replacement of N-CH3 by N-C2H5 quadruples potency, so some papers must be out there...
 
Last edited:
Phencyclidine (``Angel Dust'') Analogs and Opiate Benzomorphans Cause Cerebral Arterial Spasm

Bella T. Altura, Remi Quirion, Candace B. Pert, and Burton M. Altura



Several psychotomimetic phencyclidine (PCP) analogs--N-ethyl-1-phenylcyclohexylamine (PCE), N-[1-(2-thienyl)cyclohexyl]piperidine (TCP), N-[1-(thienyl)cyclohexyl]pyrrolidine (THP), ketamine, and N,N-dimethyl-1-phenylcyclohexylamine (PCDEA)--were tested on basilar and middle cerebral arteries of the dog in vitro and found to induce contraction in these blood vessels with a maximal contractile activity (i.e., intrinsic activity) similar to that of PCP. The concentration-effect curves of these compounds were found to be parallel to the curve of PCP (P < 0.01). The relative potency was PCE > TCP > PCP > THP > PCDEA > ketamine. A PCP analog with no psychotomimetic activity, 1-piperidinocyclohexanecarbonitrile (PCC), did not induce the blood vessels to contract, nor did the opiate morphine. Three psychotomimetic benzomorphans--pentazocine, cyclazocine, and N-allylnorcyclazocine--were found to: (i) also produce contraction; and (ii) have concentration-effect curves parallel to the curve of PCP, but with reduced intrinsic activities (i.e., maximal tensions were lowered) compared to PCP. A opiate, ethylketocyclazocine, relaxed the blood vessels in a dose-dependent manner. This study provides direct evidence for a distinct PCP receptor on cerebral blood vessels and suggests that certain benzomorphans may produce cerebral vasospasm via PCP-receptor interactions.
Click to expand...

Does this mean we've got to be really careful with PCP analogues? Strokes etc sound kind of dangerous
 
ok, how about... 3,4-methylenedioxy-n-methyl-1-phenylcyclohexyl-dl-methorphanyl-lysergic acid-diethyl-amphetamide freebase

how bout that dooode, duz that sound kool...put that in yer pipe and smoke it:)
 
Dissociatives are like a magic trick in terms of the chemistry involved:

a) PCP, involves "non classical" displacement of cyanide by PhMgBr from PCC.

b) The rearrangement in the last step of forming ketamine is completely mind boggling to the untrained eye.

My friend showed me a german opioid which looks like a cross between PCC and the precursor to methadone. I cant remember its name though, pipramide or something. Its on wikipedia, uh, i'll edit this later.
 
Guess he's gonna change his mind on PCP,wasn't that the 3-HO-PCP you actually tried?

And btw,is that alledged hangover from PCP mostly caused by the PCC impurity which is present to quite a degree (50% ) in cheap samples? A reasonable dose of PCP lasts only 4 hours,this is comparable to those simple tryptamine psychedelics which we label "short acting" for some reason ;) Hangover is more a pleasant afterglow in my view and hey,I have it with K as well at least when doing >60mg i.m.! Though when doing higher doses PCP (above 8mg) the picture is changing.

Stop bad mouthing Phencyclidin.Every drug has its optimal dose and targeted effect.A P-hole is it probably not. A K-hole is.


fastandbulbous said:
It was just the general 'too much dopamine' after effects of PCP that I didn't like (had several days of muscle tension) and replacing the phenyl group with a 2-thienyl group only makes it more active as a dopamine reuptake inhibitor. I like stimulants (you'd never guess eh? =D), but the dopaminergic activity after PCP was somewhat unpleasant as far as I was concerned.

I agree with vecktor that tiletamine is a somewhat less than pleasant drug with it's after-effects (my experience with it was just too weird to be comfortable with) and after reading about the pharmacology of TCP (I always think of the antiseptic product sold in Britain when I hear TCP - trichlorophenol - too much experience with the smelly stuff from falling off bicycles etc when I was a kid!) I thought that it comes under the category of 'thanks, but no thanks'. I like dissociatives to be short(ish) acting and not leave you the day after with excessive dopaminergic activity and a quick tour of 'the world of schizophrenia'; Tweaking ketamine so that you end up with say a 2 hour experience would be the best way to go in my book
Click to expand...
 
hugo24 said:
Guess he's gonna change his mind on PCP,wasn't that the 3-HO-PCP you actually tried?

And btw,is that alledged hangover from PCP mostly caused by the PCC impurity which is present to quite a degree (50% ) in cheap samples? A reasonable dose of PCP lasts only 4 hours,this is comparable to those simple tryptamine psychedelics which we label "short acting" for some reason ;) Hangover is more a pleasant afterglow in my view and hey,I have it with K as well at least when doing >60mg i.m.! Though when doing higher doses PCP (above 8mg) the picture is changing.

Stop bad mouthing Phencyclidin.Every drug has its optimal dose and targeted effect.A P-hole is it probably not. A K-hole is.
Click to expand...
Gawd the afterglow of pcp is supernatural. I used to feel like that for months and the only thing bringing me off it were a few bowls of the very same substance at night time till I'd find myself jumping out of bed in the morning feeling like superman on coke. I'm not really sure about the role of dopamine in these after effects. They might be due to the nmda antagonism as well. We can see antidepressant effects in various nmda antagonists. Maybe pcp is just decreasing nr2b receptor activity moreso than the other recreational non selective NMDA antagonists and the dopamine reuptake inhibition just tops it off... Either way, the afterglow of pcp is fucking amazing and for me there's never been any euphoria close to that of a phencyclidine afterglow in combination with a low dose of psilocin.

Ham-milton said:
Do you mean Piritramide? I think so.

that's an opioid I'd love to taste!
Click to expand...
I got that IV in hospital each time before they started removing the dead tissue from my burns and it was fucking amazing!!!


EDIT: Btw watch out for those pcp analogues out there. Some of them are utter crap. I got something which was supposed to be 3-OH-PCP and all I experienced was a massive increase in muscle tension coupled with waves of intense clonic muscle activity induced by voluntary contractions of muscles. NOT pleasant and possibly (just a vague uneducated guess here!) due to massive serotonine agonism.
 
Last edited:
^ Encouraging words for the 3-MeO. I'm looking forward to seeing what it can do.

One thing that worries me though is the (reported) lack of Anaesthesia. While this is not a problem if we're talking about small, therapeutic doses, it is a problem for entheogenic use (for me). See, I consider the anaesthesia to be a key part of all the mystical experiences I had with my beloved Ketamine.

And yes, I agree with you about PCP - the "time shuffle" is a rather disheartening effect of angel dust.
 
@fastandbulbous
Unfortunately, on the mentioned substance I acquired I experienced no effects like that at all. In fact, no psychological, emotional, or perceptive changes at all. Just the muscle tension and clonus. Total failure. I upped the dosage to 20mg over the course of my experiments, driven by the curiosity about pcp analogues. That's when it became apparent there wouldn't be anything to gain from it.
Btw the person who gave me this made the same disappointing observations upon ingesting the substance and so did his friends. Supposedly it was 3-OH-PCP, but I'm guessing it an entirely different pcp analogue.
 
Unfortunately, on the mentioned substance I acquired I experienced no effects like that at all. In fact, no psychological, emotional, or perceptive changes at all. Just the muscle tension and clonus. Total failure.
Click to expand...


Yep I had some of that - not at all nice, muscles tennse like a kangaroo, but fuck all psychologically. Yeah, 3-hydroxys are write offs. The 3-methoxys on the other hand have no muscle tension and very exceptional psychological effects excellent potential theraputic tools. Soooo nice...


Still reckon 2-(3-methoxy)-2-(N-ethylamino)cyclohexanone and N-ethylnorketamine are potential winners
 
Last edited:
Can someone post pictures of the molecules of these new (or newly made, I guess) PCP analogues, with comparison to plain old PCP and Ketamine?
 
I can... just a sec

pcpandfriends.png
 
fastandbulbous said:
Yep I had some of that - not at all nice, muscles tennse like a kangaroo, but fuck all psychologically. Yeah, 3-hydroxys are write offs. The 3-methoxys on the other hand have no muscle tension and very exceptional psychological effects excellent potential theraputic tools. Soooo nice...
Click to expand...
Oh how very tempting.
 
You must log in or register to reply here.
Top