dissociatives of the future

[nativenick]

well since theres been psychedellics of the future entactogens, opiates, stimulants etc im curious about dissociatives

ive heard some interesting things about other pharmaceutical drugs already out or being researched that effect kappa opiod receptors to produce a dissociative high mind you the effects sounded very dysphoric from what i heard and very frightening like some overly intense salvia experiences. would a drug affecting kappa opiod receptor be recreational in any way or is that an oxymoron

also are there possibilites for future drugs that affect nmda receptors (ie something like ketamine, pcp and its analogues) as well as drugs hitting several receptors (nmda, pcp1 pcp2 sigma recpeptors something similar to dxm). im not gonna lie other drugs similar to dxm would be real neat

any other drugs that could affect other recptors to produce a dissociative mindstate

i find dissociatives very fascinating something enjoyable is not a requirement im really fascinated by there effects on the brain and the way they affect your perception of things ie the dreamy mindstate, revisiting past memories and visiting landscapes in vivid detail, dimensions, size, liliputian hallucinations, obe to just warping the way some one thinks of physics and such

 

[toxide]

pcp analogs seem like the most likely, kappa opiods are too different to considered typical dissociatives and most people hate them, they will never be "drugs of abuse" and most likely never schedueled, and mosdef never synthed to b sold to drug users, there's no $ in that type of chem.

As far as new types of classes of chem structures for dissociatives, theres obviously mk801 analogs, carboxylated phosphonic amines(the AP4/5 related, the piperidine and glycine and alanine ones will cross the BBB very potently), arylguanidines (my idea would be 1-benzylamino-3-naphthyleneguanidine>BANG< which is a cross between arginine/agmatine and aptiganel, and maybe spermine based chems like N-1,4,8-tribenzylspermine, dansylspermine analogs

What I really wanna see is a/b- endopsychosin , so little is known or available to know about it. It's been isolated from porcine brain and is an indiginous pcp/nmda dissociative of strong potency, dont know if it crosses bbb altho i think it does. I have not seen any info on its fx in human or animal or cells, no structure only a cas#, it's a peptide i think, that's the only info i could find

 

[delta_9]

...

 

[hussness]

I was wondering if anyone had access to the following article:


AU: Ferenc Zsila, András Gergely, György Szász
TI: Conformational study on ketamine by circular dichroism and ultraviolet spectroscopy
SO: Chirality
VL: 11
NO: 4
PG: 280-285
YR: 1999
CP: Copyright © 1999 Wiley-Liss, Inc.
ON: 1520-636X
PN: 0899-0042
AD: Institute of Pharmaceutical Chemistry, Semmelweis University of Medicine, Budapest, Hungary
DOI: 10.1002/(SICI)1520-636X(1999)11:4<280::AID-CHIR4>3.0.CO;2-E
US: http://dx.doi.org/10.1002/(SICI)1520-636X(1999)11:4<280::AID-CHIR4>3.0.CO;2-E
AB: Since the enantiomers of the N-methyl-D-aspartate (NMDA) receptors antagonist ketamine have different pharmacological profiles, CD and UV spectroscopy were applied for the study of conformer equilibrium and pH dependence in ketamine solutions. The assignment of the configurations and conformations was performed on the basis of the ?octant rule? and UV spectra. In accord with published data, it was established that, on protonation, the phenyl group of the ketamine molecule occupies an axial position, while for the base form, the ratio of conformers containing axial/equatorial aryl moieties is strongly solvent-dependent. The CD and UV spectra indicate the presence of an intramolecular H-bond C=O····H - N in the conformer with axial aryl moiety. Chirality 11:280-285, 1999. © 1999 Wiley-Liss, Inc.

I found the link on:
http://www3.interscience.wiley.com/cgi-bin/abstract/55003430/ABSTRACT?CRETRY=1&SRETRY=0

 

[Jamshyd]

There is a whole array of very interesting Ketamine and PCP analogues just WAITING to happen. Their SARs have actually been predicted by some very brilliant minds

But for some very stupid reason, it seems like people are more interested in crap like cathinone analogues (like seriously, wtf?).

Ask F&B. I'm sure he has some interesting opinions regarding this .

 

[egor]

Some tweaking of the tiletamine or memantine molecules could create some interesting compounds as well.

 

[toxide]

adding an aryl position to memantine seems like the most logical thing to do, maybe sumthing like... 1-theinylamino-3,5-dimethyl-adamantane, altho i don't understand y memantine is so expensive, it seems like such a simple structure, is it that hard to make?

 

[fastandbulbous]

I'd say avod the thienyl group for making arylcycloalkylamines... it has a greater effect on dopamine reuptake and the aftermath of PCP was unpleasant enough because a day afterwards I decided to have a small dose of desoxypipradrol (muscle tension throught my body). Much better staying with (ring substituted)phenyl groups IMO

 

[hussness]

^I'm not following what you just said. Could you explain further?

 

[nuke]

ideally i'd like something like ketamine but with a greater potency and shorter duration (the DMT of dissociatives!)

 

[Jamshyd]

^ Kinda like N2O?

 

[toxide]

I dont understand y anyone would want shorter duration than ketamine already has. Yeah i dont understand F&Bs statement either, pcp has a strong stimulating super euphoric (IMO) quality that lasts for days sumtimes, the after FX are a high unto itself,TCP just has greater potency and lasts much longer and is perhaps more stimulating, and i've never crashed off pcp. i can't see the negatives in that anywhere

 

[vecktor]

I dont understand y anyone would want shorter duration than ketamine already has. Yeah i dont understand F&Bs statement either, pcp has a strong stimulating super euphoric (IMO) quality that lasts for days sumtimes, the after FX are a high unto itself,TCP just has greater potency and lasts much longer and is perhaps more stimulating, and i've never crashed off pcp. i can't see the negatives in that anywhere

I fink dat FnB iz tryin 2 say dat he duzn't like the DAT reuptake FX and stimulation ov PCP urgo da more potent DARI's that R de thienyls will not B pleasant 4 him or sumthing.
Having tried tiletamine I wud agree dat sum thienyls are < pleasant. I don't know if it is the dat FX I dislike bout tiletamine but its a lot more disturbing than ketamine with low level wierdness persisting 4 a long time.
hope dis is wat F&B waz trying to say.

 

[haribo1]

TCP with a methyl in place of the cyclohexyl group? SHould lower the 1/2 life...

 

[vecktor]

^ or throw away the thienyl completely and replace it with a tetrazole ring. or maybe 5-oxo-1,4-dihydrotetrazol-1-yl moety. perhaps aromatic enough and certainly a short half life.

 

[toxide]

replace the cyclohex with methyl...

^and no dissociative fx?
I dunno, maybe americans r different but in all the many many people i know, they all love ketamine but pcp is by far the most sought after here, and not just cuz it's crazier and lasts longer but due to the longloasting stimulation of DA. 4 this reason PCP blows MDMA away in terms of u4ia. I'm quite familiar with "dust fiends" but K does not generate quite the same level of desire.

Anyway, I think if any new dissociatives were to surface the most likely would b aptiganel related diarylguanidines, some seem easy enuff to produce and quite potent with high affinity for blocking nmda,pcp receptors and stimulating sigma. Quite a bit of studies on the abolished anti-seizure/epilepsy drug aptiganel have determined it had very potent euphoric, hallucinogenic, and dissociative FX but no mention of any dopamine or 5HT FX for those who ^ dislike DA fx?
the synth is a bit more complex than the simpler DiPhenylGuanidines like DNG,Do/m/TG and the starting materials for sum maynot b as ez to find but they can all take a fairly wide degree of variation in structure an ez synth of an extremely active DPG is not too hard to come up with. sum hav a greater effect on pcp receptors than mk801/tcp

 

[hussness]

I fink dat FnB iz tryin 2 say dat he duzn't like the DAT reuptake FX and stimulation ov PCP urgo da more potent DARI's that R de thienyls will not B pleasant 4 him or sumthing.
Having tried tiletamine I wud agree dat sum thienyls are < pleasant. I don't know if it is the dat FX I dislike bout tiletamine but its a lot more disturbing than ketamine with low level wierdness persisting 4 a long time.
hope dis is wat F&B waz trying to say.

Pardon me if I'm wrong, but who hijacked your account? This isn't how you normally write.

 

[jasoncrest]

Are NDMA antagonists the only dissociatives?

Are sigma agonists and kappa agonists also considered dissociative?

----

About possible OTC dissociative of abuse of the future (if DXM is taken off the market):
there's an OTC medication called Carbetapentane (or Carbapentane or Pentoxyverine or Pentoxiverine)

Apparently it has DXM-like properties...

On the "dissociative analogues" thread, there was a list of dissociatives analogs, Carbetapentane was the first on the list:

carbetapentane(cough medicine)
Aptiganel(CNS-1102)(N-(3-Ethylphenyl)-N-methyl-N”-1-naphthalenylguanidine)
4ppbp(4-Phenyl-1-(4-phenylbutyl)piperidine)
pre084(2-(4-Morpholinethyl)-1-phenylcyclohexanecarboxylate)*
cis-(±)-N-Methyl-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexamine*
1-(4-Iodophenyl)-3-(1-adamantyl)-guanidine
bd1008(N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine)
arcaine(N,N'-1,4-Butanediyl-bis(guanidine)^
5,7-Dichlorokynurenic acid*^
U-54494A(cis(±)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzamide)
synthalin(1,10-Decanediyl-bis(guanidine)^
1-Benzyl-3,4-dihydrospiro[IH-indene-1,4'-piperidine
N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(1-azapinyl)ethylamine
L-701,252(7-Chloro-3-(cyclopropylcarbonyl)-4-hydroxy-2(1H)-quinoline)^
AP5(DL-2-Amino-5-phosphonovaleric acid)*
D-AP4(D(-)-2-Amino-4-phosphonobutanoic acid
SKF10047((+)-N-allylnormetazocine)10mg
dizocilpine("mk801"(5R,10S)+5Methyl10,11dihydro5H-dibenzo[a,d]cyclohepten5-10imine
PCPMP(1-(1-phenylcyclohexyl)-4-(phenylmethyl)piperazine)
memantine(3,5-dimethyl-1-aminoadamantane)
amantadine
4meopcpy(4methoxyphenylcyclohexylpyrrolidine)
2methylbenzyl(methylamino)cyclohexanone

 

[vecktor]

Pardon me if I'm wrong, but who hijacked your account? This isn't how you normally write.

no one
I thought I would try writing in the 'vectride' style but I don't think it works

I find toxides posts very hard to read. ho hum

 

[fastandbulbous]

Having tried tiletamine I wud agree dat sum thienyls are < pleasant. I don't know if it is the dat FX I dislike bout tiletamine but its a lot more disturbing than ketamine with low level wierdness persisting 4 a long time.
hope dis is wat F&B waz trying to say.

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? ), 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