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  • Trip Reports Moderator: Xorkoth

PCP analogs (Cumulative) - Retrospective - Bioassays

Closer to 5-MeO-DMT (but dark lol), I never liked that stuff either.

IM it gave me the most frightening psychedelic experience I've ever had. You couldn't pay me to take the stuff again


DPT+Ketamine always did that trick for me.

After that combo, I remember listening to the Robert Calvert track 'Ejection' and actually feeling like I was in an ejection seat, bursting up into the sky. With the right music, that combo is about as good as you can get


I'd be wary of conflating hypomania with antidepressant effect, but I still wouldn't completely doubt you just yet as you are far more experienced in these than I am.

You may well be right as I'm bipolar and always associate hypomania with feeling on top of the world (unlike full blown mania of which I've only ever progressed to a very few times, which is unpleasant due to pressure of thought and inability to concentrate or even think coherently)
 
You may well be right as I'm bipolar and always associate hypomania with feeling on top of the world (unlike full blown mania of which I've only ever progressed to a very few times, which is unpleasant due to pressure of thought and inability to concentrate or even think coherently)

Now that is interesting as I suffer from borderline personal disorder and I experience hypomania quite often but a full blown mania happened to me a few times (when I really didn't control my actions actually, I mean I wouldn't normally do things I did, from some episodes I don't even remember certain events). I know bipolar disorder is a different thing and I might get swaps from depression to mania more unexpectedly (not to mention other symptoms) but still with that said I see phencyclidine analogs with some action at opioid sites more antidepressant than straight dissociatives also.
 
I am Bipolar II as well, or at leasy according to my psychiatrist anyway. And yes, if I wanted a quick fix of hypomania, PCP analogues will work for me - but if it were hypomania that I wanted, I just skip all dissociatives and use the far more reliable amphetamines.

As with my previous posts, I am very careful to emphasize that the antidepressant action of ULD ketamine is absolutely NOTHING like the "antidepressant" jolt of PCP+co or even of a single dose of Ketamine.

It is more a feeling of balance and serenity - a sense of, "oh, so THIS is what normal people feel like when they're not in pain!"

I will keep vehemently disagreeing that the effect is a simple activation of some reward pathway in the brain. It seems to be far more involved than this and seems to have to do with a biological learning/rewiring process of some-sort.
 
I was very young (though I know people who got involved in this shit even at younger age) when I started taking opioids and got addicted to them. And my fascination with chemistry started even earlier. At the same time I started taking benzodiazepines every day, some 7 years ago it was very easy to get a prescription for anything, if not that even now a lot of people get whatever benzos they want without any help of some quack. I had some "on and offs" with mainly morphine at the beginning and later a shitload of semi-synthetic and fully synthetic opioids. Anyway, I never was a master in coping with withdrawals so my breaks were days, the longest - one and half a month...

Anyway, I also had some love for dissociatives from the beginning as well. They could unplug me from the world just like opioids, only in a different manner. I'm still a big fan of ketamine but I could also name a few of my favorites from PCP analogs I know of. Chemicals like PCP or PCE are ruthless, unforgiving but I've to say I never freaked out on those and similar, certainly they're the ones prone to cause (hypo)manic episodes. Those I find the best are either known as strong anesthetics or interact with opioid mechanisms in some way.

A lot of physicians don't even recognize anything like "Borderline Personality Disorder" so I was fed with lies for quite a long time going to private quacks and paying them a lot. I knew there was something wrong and it wasn't any straight depression. But it wasn't official until I met a very good doctor (not private) who did a good job with my diagnosis before prescribing meds. I also had a chance to get tested with a polygraph, I took an MMPI-2, and after the final talk with an analyst I got the letter and the number which meant BPD in short.

Well, whatever it is, you really need to work with yourself to overcome it. Actually, I find some symptoms of BPD as advantages when you train yourself. Yet going out of control still happens to me and during depressive episodes I think all my work went for nothing.
 
I know you'd rather not share, but can you elaborate on your IV experience with tiletamine? Dose? Duration? Onset?

I'd assume the ratio would be similar to that of Ketamine but one can never be too sure...
 
Right, I'd rather not share such precise information for a good reason. You're basically "out" after ketamine i.v. shot misdosed only a bit and if there's no one around, you can't even pray you wake up after an hour... And analogs with phenyl ring substituted by 2-thienyl are not to be messed up with really. I guess anyone who injected ketamine i.v. may report i.m. injection gives better effects in terms of "smooth" falling down the K-Hole. And some praise snorting it for other effects.

One thing I'm sure about my i.v. experience with tiletamine is that it was far from any research-like thing, it was simply abuse as I also used Telazol later and it didn't bother me there's 50mg of a crazy benzodiazepine analog in it (1:1 with tiletamine, for me zolazepam is only ~4 times weaker than clonazepam on a weight basis and articles say the same). Today's world and today's medicine show a finger to people like me. There's not a single person on Earth with any knowledge about medicine and pharmacology caring to help me. So I've "helped" myself numerous times in different ways. Not that I'm ashamed of it, it's not me to be ashamed. I just know this in no way helps people who apparently are in possession of some tiletamine (or in other cases other drugs, not only dissociatives) and want to use it recreationally or use as an aid for depression, for mania, for other problems. Intravenous usage is not the way and I totally disapprove of it.

And if you're still looking for an answer --
Read some posts about ketamine intravenous injection experiences and spice them up. Dose, duration, and onset are easy to deduce from what I wrote on i.m. injection of tiletamine. Still, I advise you to use it intramuscularly if you insist on injection. Tiletamine is harder to "co-operate with" than ketamine and as I'm totally against i.v. usage of any arylcyclohexylamines, I'm against i.v. usage of tiletamine, it doesn't go along with harm reduction.

I'll cut the long story short. I was tapering down with buprenorphine, it didn't work, I was getting more and more frustrated. I didn't use a needle since my last morphine shot in October '09. But then I did, several months later I broke through buprenorphine with 3-MF (~35mcg I guess) a few times. Then I stopped doing that and started using Telazol as it saved me time for obtaining ketamine. 2nd floor restroom, ~2ml of medicine from a 5ml vial preceded by 150mg of pure MDA snorted. Tick! And I was like in a situation balancing on a line over an abyss.
 
Despite your reports to the contrary, IV ketamine happens to be my most preferred ROA. After spending considerable time with the substance I've come to appreciate the efficient, intense experience offered by the needle.

Time is difficult to discern on Ketamine, especially in the more intense moments of an experience. One minute can feel like an hour--so why not shorten the duration so you can return to a workable state of sobrety with more haste? IME, the needle does not take away from the psychedelic and therapeutic effects of the drug in any way. The immediate integration into the k-space shatters my ego in the most beautiful way; that can be terrifying or unwelcome if the dose is too high or you're in the stall of a public restroom. Work up the dose slowly and respect the substance.

I'm not in it to win it, just trying to play the game. Thanks for the info friend.
 
I haven't written one can't use ketamine intravenously (and that being said - not for anesthetic purposes) safely when it's done responsibly etc.

I've injected ketamine along with morphine and snorted MDMA and I wasn't like dying. It's all about that simple phrase all should keep in their heads doing anything any route: "Know your body, know your substance, know your mind, know your source". There's a substantial difference between "T-Holing" or some strange elephant-flipping not caring about the dose and mixing even two potent depressant drugs with entheogen that is a stimulant rather with all doses measured properly and having taken each drug alone, right? Yet I don't find it in any way harm-reducing to report such experiences.

And you know what? There's nothing to win here, this game is really not about winning. I wish it were.:\ In sake of "it's better to show someone how to shoot up instead of watching how he/she is doing harm to himself/herself"... Tiletamine intravenously is slightly stronger than ketamine (judging only by the fact there's ethyl on nitrogen and 2-thienyl is a wilder solution than phenyl, right?). The onset and duration are very similar. I worked my dose of tiletamine i.v. myself basing everything on these facts as there's probably no source for dosing this drug in human. Also bear in mind that, although it doesn't have such a strong introxication feeling and bodyload like e.g. PCE, tiletamine thanks to 2-thienyl group behaves "wilder" than ketamine. Like there was this discussion about "ketamine's magic", well, this comes easily explained from how the drug works. After some short work-up ketamine is really appealing if someone's not afraid of dissociative experiences, moreover - this is what he/she aims for...
 
You make some good points. I'll make sure to start low with tilet when the time comes.

Got another question for you...how different are the experiences with Telazol and straight Tiletamine? Are the psychedelic effects negated by the benzos like I hear many people report?
 
Yes, Telazol feels different for me than tiletamine alone. Zolazepam is a nice sedative benzodiazepine analog for me and I also took it alone or with clonazepam when I had some (clonazepam alone became "shapeless" for me and it doesn't do its job like it used to). And it has an impact on general feeling of tiletamine. It's generally less "wild", I've never felt any fear after ketamine or tiletamine that the drug is going to act in a way I won't like. Are psychedelic effects negated? Well, I can't see it as a psychedelic. Dissociative effects aren't negated for sure, zolazepam potentiates anesthesia but if you mean a "ketamine-like" ride then zolazepam ruins it in some way. If one wanted to experience dissociative effects, ketamine is > Telazol.

Also it naturally depends on your tolerance to benzodiazepines. Mine is high. I take 6mg of clonazepam a day and that doesn't feel fine now anymore. I know I could eat the whole package (60mg) and I'd be fine, if you were sitting with me somewhere, you wouldn't have to call for ambulance. If you don't have any tolerance to benzodiazepines, Telazol with tiletamine:zolazepam 1:1 ratio is surely not a good source of tiletamine to get a good feel of it as active doses of tiletamine are much higher than active doses of zolazepam. It's a veterinary medication so for some bear or pets it's ideal to anesthetize them but as a drug of recreational use it might be dangerous with such a ratio of both drugs.

Articles state that 1-2mg zolazepam is equal to 0.5mg clonazepam. Like I wrote, for me it's more like 4 times weaker so 2mg makes more sense. So when I injected 2ml of Telazol, it was like I took 25mg clonazepam, that isn't much for me but it's good enough to tranquilize me. After 2ml injected i.v. I lost consciousness in like one minute so it's really no game. I believe I woke up after ~30 minutes and it took another 2-3 hours for me to recover totally. Total carefulness must be taken into account when trying this as ICP (pressure in skull), cerebral blood flow are raised and requirement for oxygen due to metabolism is increased as well (nothing new as this is common for all ketamine analogs). Zolazepam is there as tiletamine increases sympathetic tone and that stimulates heart (increased probability of tachycardia and arrhythmia).

It's also not to be done in places like men restroom at university because of ataxia so even if you don't lose your consciousness (but that's improbable in benzodiazepine-naive people and it may happen only with low doses and i.m. or s.c.)., your motor capabilities will be absent. It's best to have a place to lie after a shot or sit in a deep armchair.

BTW Telazol may be painful given i.m. or s.c.
 
^^^ wow just re-read this whole thread again, didn't realize i was the last one to post in it =p

just had one thought

3'-oh-pcp shows markedly increased analgesic effects, which is great, but it also makes it more potent as a dissociative so its hard to get to dosages where you're feeling strong opioid effects...

adding a paramethyl on the piperidine ring of PCP reduces potency by 3x while not altering effects too greatly you say

therefore i suspect that 4-methyl-1-[1-(3-hydroxyphenyl)cyclohexyl]piperidine could be a very interesting compound that produces both dissociative and opioidergic effects without either effect overpowering the other, no?

also i found this paper earlier tonight and wanted to share it somewhere on here. it claims that 3-amino-4-fluorophencyclidine is "biologically active"

http://books.google.com/books?id=mk...wAA#v=onepage&q="fluorophencyclidine"&f=false
 
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By p-methyl I figured out you mean placing methyl on position 3 of piperidine. 3-[1-(4-methylpiperidin-1-yl)cyclohexyl]phenol could be evaluated but I wonder what impact 3-methyl group would have on the potency on the 3'-HO-PCP.

3'-amino-PCP are similar compounds have this clearly distinctive sedative property present in 3-HO-PCP, amino group is a good replacer for hydroxy group.

4'-F-PCP was the only active derivative with a halogen on position 4 in phenyl group (also I counted in pseudohalogen groups4'-Br-PCP is inactive, 4'-nitro-PCP is inactive - I was like "what the heck?! I don't get SAR here" - and sadly I still don't). Nevertheless, if 4'-F-PCP is active and 3'-amino-PCP is definitely active, 3'-amino-4'-fluro-PCP may also be active however I have no idea to what extent and actually I would still prefer taking 3'-amino-PCP to 3'-amino-4'-fluro-PCP because I know that 3'-amino-PCP is along the lines of 3'-HO-PCP.

Note: It's 3'-amino-PCP, 4'-fluoro-PCP, 4'-HO-PCP instead of 3-amino-PCP, 4-fluoro-PCP, and 4-HO-PCP because when we (meaning my friend and I) started this project we started numbering piperidine ring first so phenyl ring has 2', 3', and 4' positions.
 
actually by "para-methyl" i meant where the additional methyl is in this compound from your original post... 4-methyl-1-(1-phenylcyclohexyl)piperidine. i've never taken o-chem so forgive me.

by adding that methyl group i'm hoping that 3'-OH-PCP's dissociative effects can be reduced without altering its potency as a mu-agonist.
 
I'm 99% sure what compound you had in mind. It's just that you use prefixes "ortho", "meta", and "para" only for substituents on different positions on aromatic ring. You can't use it for piperidine because it's not aromatic. Anyway, I'm guessing this is what you meant:

 
^^^ yup exactly what i meant. pure SARsturbation i know ;) haha. maybe someday i'll get to taste that stuff though and see if my theory is correct.
 
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This thread is still one of the best and deserves a bump. Out of plain curiosity, can anyone guesstimate what would happen if we placed a 3-Chloro-group on ketamine's phenylring instead of a 2-Chloro? Couldn't this theoretically increase potency? I'm really new to QSAR's and am studying medicine, not chemistry or pharmacology. So I might be totally off here. I drew a picture of what I'm thinkin of, not even sure if the isomers are correct...

My line of thought was this, not overly complex really...
If ketamine (2-(2-chlorophenyl)-2-(methylamino)cyclohexanone) and it's analogue with a methoxy in position two (2-(2-methoxyphenyl)-2-(methylamino)cyclohexanone) are showing the same activity, then both the 3-methoxy and 3-chloro substituted phenylring should provide an experience closer to MXE, but with a shorter duration (in theory anyway) because of a methyl, instead of an ethylgroup being attached to the amine, right?

Also, could a propylgroup on the amine further increase duration or is it more likely to show no activity at all??
The main problem with ketamine is it's high toxicity which is related to users constantly redosing massive amounts of substance, assuming the metabolic pathways of these analogues (ethyl/propyl) show comparable toxicity to ketamine per mol of metabolized substance.
So if either duration could be increased or dosage reduced, this could really do some good for the health of dissociative fans, right? I wonder if there is any way to increase ketamine's duration. Any input is much appreciated, I'm a total noob on this field.

Planning to play around with ACD/Labs in the near future and maybe deduct some qsar's through observation of known compounds as well. Is there anyway to get hold of a 3d template of the s1r and then perform in silico docking experiments with a selection of self-created structures? It really doesn't matter if it takes years for my pc to process the data, I love this shit. Any help is much appreciated. Gonna start reading into this soon...
 
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3-bromo-pcp is apparently inactive as i'm sure you saw. the 3-position doesn't seem to tolerate excessive bulk that well? chlorine could be active though, who knows... only one way to tell on this one IMO ;)

also, i would assume that someone had tested the n-propyls when they were testing the n-ethyls. either way your molecule above should probably have at least an n-ethyl on it, to increase potency and decrease risk of urinary problems for chronic users.
 
My first post answers your question. Halogens on 3. position of phenyl ring make compounds inactive (only 3-fluoro-PCP showed some very little activity in my wee research). The second structure you draw has carbonyl group placed differently. But still chlorine at 3C demolishes any activity.

The rule on the second amines is simple: ethyl > methyl ≈ n-propyl ≈ isopropyl > butyl > pentyl... Longer alkyl chain at the amine abolishes activity.

Ketamine's duration can be extended in a quite simple way - just get rid of chlorine. But then you end up with a dissociative that doesn't resemble ketamine at all. It's totally devoid of any ketamine "euphoria" and its "magic".
 
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