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PCP analogs (Cumulative) - Retrospective - Bioassays

blowjay

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Jan 7, 2010
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in vivo testing would have sufficed in the context i was discussing it in -- i'm pretty sure blowjay is just looking to trip out. :)
Sure... shift the blame... twist that knife... I am sure your interests in this thread are FAR different than mine...

(obvious sarcasm)

But I agree with you, bring on the 2-Fluoro-Deschloroketamine =D

In my opinion this thread is in the wrong forum, it def belongs in ADD of PD.
Agreed to the fullest with both, time to merge all of my posts of the day!
 
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blowjay

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Cooperation would be key in moving this thread forward, lets all try to get the seperate camps of differing thought and speculation helping each other out a bit more if we could.

It seems to me this thread is missing much information that is apparently easily accessed and it would be wonderful if we could compare literature on such topics to 'field' research and then maybe try to tackle the 'hunches' that posters have thrown out on here as likely active and interesting.

___________________~~~~~~~~~~__________________ Moving forward...

Is anyone going to tackle what an isoproyl sub on the nitrogen of any of the commonly mentioned arylcyclohexylamines such as PCP/Ketamine/MXE would likely do? I haven't seen any arylcyclohexylamines with said group and would love to know what that would theoretically or actually entail. I wouldn't be suprised if the PCI-Pr has been studied but how about the ketamine? Iso subs sure excite me!


Next order of business: Has anyone thought about ethoxy instead of methoxy on MXE? EXE has such a terrible ring to it, entertain this idea as well if you could.

And while I like the suggestion of moving the methoxy to a different position and think it would be interesting, at this point in time it may be useful to go towards things that won't be seen as positional analogs of MXE in a future where it is scheduled.

This is my reasoning behind furthering understanding of the potential changes brought upon by the Chloro sub and the ethoxy(or propoxy) and the Methyl/Propyl/Iso-Propyl sub's.

There is more magic out there and we will find it.
 

crOOk

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Adder mentions in his deleted recent post that he feels ketamine is opioidergic. Blowjay wants to get the hunches out of the way. So here is at least one bit of information...

Central antinociception induced by ketamine is mediated by endogenous opioids and μ- and δ-opioid receptors.
Abstract

It is generally believed that NMDA receptor antagonism accounts for most of the anesthetic and analgesic effects of ketamine, however, it interacts at multiple sites in the central nervous system, including NMDA and non-NMDA glutamate receptors, nicotinic and muscarinic cholinergic receptors, and adrenergic and opioid receptors. Interestingly, it was shown that at supraspinal sites, ketamine interacts with the μ-opioid system and causes supraspinal antinociception. In this study, we investigated the involvement of endogenous opioids in ketamine-induced central antinociception. The nociceptive threshold for thermal stimulation was measured in Swiss mice using the tail-flick test. The drugs were administered via the intracerebroventricular route. Our results demonstrated that the opioid receptor antagonist naloxone, the μ-opioid receptor antagonist clocinnamox and the δ-opioid receptor antagonist naltrindole, but not the κ-opioid receptor antagonist nor-binaltorphimine, antagonized ketamine-induced central antinociception in a dose-dependent manner. Additionally, the administration of the aminopeptidase inhibitor bestatin significantly enhanced low-dose ketamine-induced central antinociception. These data provide evidence for the involvement of endogenous opioids and μ- and δ-opioid receptors in ketamine-induced central antinociception. In contrast, κ-opioid receptors not appear to be involved in this effect.

Source: Brain Res. 2014 Mar 24. pii: S0006-8993(14)00374-6. doi: 10.1016/j.brainres.2014.03.026.
I've got the whole article. Just let me know if you want to read it.
 

crOOk

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And here is some countervailing data:

http://www.bluelight.org/vb/threads/649843-Binding-data-for-popular-arylcyclohexamines?p=10990521&viewfull=1#post10990521

The methodology of the study you cite above doesn't discriminate between downstream opioidergic effects and direct binding.

ebola
If ketamine exhibited opioidergic activity by directly binding to opioid receptors, shouldn't that have been worked out by now? I'd just assume it does not bind to them, otherwise I'm pretty sure it would'nt be worth publishing an article stating ketamine's antinociceptive effects are opioid receptor mediated. Catch my drift?

I personally haven't read the entire article, I just found it right before I posted it and only wanted to contribute. Therefore, I'm not sure whether it makes any claims as to what the opioidergic activity results from.
I was assuming it simply stated, that: YES! Ketamine does induce opioidergic activity (of course somewhere downstream of it's binding sites).

I personally have heard claims from users about various dissociatives' opioidergic effects many times, but have always been very sceptical about them. So for me, this is big news!

Btw are you sure the article "didn't discriminate between downstream opioidergic effects and direct binding" or did it just not even consider direct binding because it had been shown earlier that there is no direct binding to opioid receptors? If it actually didn't discriminate then it's one helluva shitty article and I might just as well delete my post lol.
 

adder

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Mar 28, 2006
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Adder mentions in his deleted recent post that he feels ketamine is opioidergic. Blowjay wants to get the hunches out of the way. So here is at least one bit of information...



I've got the whole article. Just let me know if you want to read it.
I've thought that I'd post a completely new thread in ADD, so more people can see it - here. I'm reasoning basing on the paper quoted there that ketamine is an opioid agonist superior both 2-methoxydeschloroketamine and ethylnorketamine. I'd gladly see an article with some numbers.

EDIT: I've read the article here before. I missed one part, but anyway I still think that there's possibly some indirect way of interaction with opioid receptors for ketamine.
 
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blowjay

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If ketamine exhibited opioidergic activity by directly binding to opioid receptors, shouldn't that have been worked out by now? I'd just assume it does not bind to them, otherwise I'm pretty sure it would'nt be worth publishing an article stating ketamine's antinociceptive effects are opioid receptor mediated. Catch my drift?

I personally haven't read the entire article, I just found it right before I posted it and only wanted to contribute. Therefore, I'm not sure whether it makes any claims as to what the opioidergic activity results from.
I was assuming it simply stated, that: YES! Ketamine does induce opioidergic activity (of course somewhere downstream of it's binding sites).

I personally have heard claims from users about various dissociatives' opioidergic effects many times, but have always been very sceptical about them. So for me, this is big news!

.
I want to also point out that methoxetamine has a kind of opioid effect on myself but I don't really get that from ketamine, if there is opioid related action that would certainly explain how the ketamine as a means to beat an addiction to opi's would be effective, I think others use methoxetamine in a similar application with good success stories.

So I guess the question now is why aren't there any people playing around and making some of these compounds we are discussing that are legal? I mean the ethyl to propyl really gets me, it isn't going to be hard to do swaps like that but nobody is even discussing that on methoxetamine. If NEK can be made and methoxetamine can be made then why can't the chloroxetamine (copy-righted by me) be made? Seems that if you can make the two of them it wouldn't be the hardest to do.

But in all seriousness, WHERE THE FUCK IS THE PROPYL OR ISOPROPYL VERSIONS OF METHOXETAMINE?!
 

crOOk

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All in time guys, all in time. We probably won't see new ones pop up before diphetidine and 2-meo-diphetidine have been outlawed.
 
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