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Opiate Dissociatives?

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thesomoan

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According to wikipedia the kappa opioid receptor " agonists have dissociative and deliriant effects" however strong k-opioid antagonists like buprenorphine do not appear to produce any dissociative effect that I know of, while some non opiates e.g. salvia antagonize the k-opioid receptor to great effect. Would it be theoretically possible to have a dissociative opiate, and if so any possible suggestions on the molecular structure?
 
I hate to be the first person to reply on my own post by I have sort of an addition to my original question. In researching this I came across the compound LPK-26 described by a pubmed article as " a derivate of ICI-199441, an analogue of (-)U50,488H, named (2-(3,4-dichloro)-phenyl)-N-methyl-N-[(1S)-1-(2-isopropyl)-2-(1-(3-pyrrolinyl))ethyl] acetamides (LPK-26). LPK-26 showed a high affinity to kappa-opioid receptor with the Ki value of 0.64 nM and the low affinities to micro-opioid receptor and delta-opioid receptor with the Ki values of 1170 nM and >10,000 nM, respectively. It stimulated [(35)S]GTPgammaS binding to G-proteins with an EC50 value of 0.0094 nM. In vivo, LPK-26 was more potent than (-)U50,488H and morphine in analgesia, with the ED50 values of 0.049 mg/kg and 0.0084 mg/kg in hot plat and acetic acid writhing tests, respectively. Moreover, LPK-26 failed to induce physical dependence, but it could suppress naloxone-precipitated jumping in mice when given simultaneously with morphine. Taken together, our results show that LPK-26 is a novel selective kappa-opioid receptor agonist with highly potent antinociception effects and low physical dependence potential." would a chemical like this have purely analgesic effects, or would it have dissociative/ recreational value?
 
Yeah, a lot of people say DXM is not an opioid because it is the inactive isomer but it does have an extremely weak affinity for the MOR. This would technically make it an opioid although too weak to have any noticeable subjective opioid effect or stop withdrawals in an addict. However, it's dissociative action is because it is an NMDA antagonist and not from KOR affinity. The opioid receptor affinity may add something to the effect, possibly but it is very weak in this respect.
 
OP: The "gold standard" (or whatever) k-agonist is Pentazocine. In my experience with it, it really has very little in common with classical dissociatives. It just feels weird, subtle, and borderline dysphoric (very uninteresting, for sure).

The new 3-Methoxylated PCP derivatives supposedly have some kind of powerful opioid action, and many seem to perceive them as such, but some do not (including yours truly).
 
what prevents opiates from acting as dissociatives? Do they not have enough k antagonism, or is it something in the way they antagonize the receptor? According to the (very short) wikipedia article on 3-meo-PCP it is primarily a NDMA antagonist, do u have any more information about its opiate action? Thanks for ur help guys
 
Well from what i understand the NMDA effects of lefetamine are fairly mild, and its more notable for acting like an opiate stimulant than a dissociative, however I have no experience whatsoever with the drug so if you have any more information i.e. first hand experience of dissociative effects that would certainly take precedence over what i have read on it, it is certainly an interesting compound tho because of it simultaneous opiate/stimulant effect.
 
why are u talking about ANTagonism of k/u-opiate receptors, they dont do anyhting, they're inactive unless yer high off opiates then they make u unhigh. Salvia is a kappa agonist. BTW i find it to b one of the most unpleasant highs but thats just me tho. The Benzorphans have alot of NMDA ANTagonism with kappa opiate AGONISM but are considered unpopular due to the kappa agonism(guess i'm not the only one who doesn't like k agonism)
 
Oh wow i just looked that up and ur right. It also looks like kappa agonism is inverse to mu agonism. But some opiates have characteristics of both, and so theoretically there could be an opiate hallucinogen that would have salvia characteristics but with opiate euphoria, i agree that salvia is not the greatest but something like that could definately be interesting
 
I personally for whatever reason(and I am very happy about this)don't get pleasurable fx from mu agonism either. But to combat the physical pain induced by kappa agonism, the only thing I can think of to go perfectly with it to combat that is a mu agonist. So yeah, k/mu agonist would b perfect in terms of having a trippy opiate. I'd b willing to try it if I wasn't worried about negative side fx I get from opiates
 
misinterpretted what u said, yes it would
 
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Swerlz said:
^yeah i was going to say 3-meo-PCP

have you had the chance to experiment more with it, Jam?
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Not since my report last year, no. I have, however, tasted Methoxetamine (2-Keto,3'-MeO-PCE), which (according to knowledgeable people on BL) has an even higher affinity for the opioid receptor by virtue of the 3'-MeO and 2-Keto substitutions. This indeed felt like an opioid to me - complete with itches - and did have some classic dissociative signatures.

I think Methoxetamine is the closest existing drug to the compound the OP asks about. To me, it is interesting - much more so than 3-MeO-PCP - but somehow I just don't find it being that useful as either opioid or dissociative, because it is sort of a half of each rather than both at once, not quite this but not quite that either. I would have mentioned it earlier but didn't want to publicize it, but now that I see it has been publicized in the last few days I thought I'd mention it here.
 
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thesomoan said:
Would it be theoretically possible to have a dissociative opiate
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I think meperidine is pretty amazing. Americans call it Demerol. On BL I've heard it referred to as pethidine (I don't know why it's such a shapeshifter). But now I'm wondering if others have experienced what I've experienced on Demerol: i.e. being able to watch yourself lose all decision-making power: having an alter ego take over but nevertheless remembering everything your body did while it was being piloted by the alter ego? Its no longer as if you're experiencing the high, but remembering the high in exquisite detail, while the high is taking place and sometimes even before it's taken place: an almost Billy-Pilgrim-like ability to become unstuck in time

Unfortunately my supply of Demerol ran dry several years ago and I haven't had any chance to experiment further with it

o-opioid antagonism
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This is the first time I've heard of the omicron opioid receptor. It sounds evil.
 
^ That's interesting, but no, I never experienced anything like that with pethidine. With low doses I get subtle but decent cocaine-like stimulation, but with higher doses, anticholinergic effects take over. Hardly any opioid euphoria. It makes me feel stupid and lethargic like nothing else, and for whatever reason it's also strongly amnesic. To me it feels quite a bit like tramadol, albeit much shorter acting and with a nasty anticholinergic twist. I used to enjoy it before, but now it just feels toxic.

Btw, Demerol is just a US brand name. The name meperidine is used in the US, while pethidine (INN nomenclature) is used here in Britain and, I believe, in mainland Europe. Very similar to the Tylenol vs acetaminophen vs paracetamol name confusion thing.
 
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