• N&PD Moderators: Skorpio | thegreenhand

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

new cannabioids

L

Lombergerh

Bluelighter
Joined
Oct 1, 2010
Messages
65
I recently came across new range of cannabioids named:
STS-135
1-(5-fluoropentyl)-N-tricyclo[3.3.1.13,7]dec-1-yl)-1H-Indole-3-carboxamide

AKB48
H-Indazole-3-carboxamide, 1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl

And can't find any info about thier potency or even Ki valuves.
So any thoughts?
 
rvErO.gif


No idea how well they'd work though.
 
They look like structural analogues of AB-001

However, even the wikipedia page says that one is unknown, except in smoking blends, FWIW. Also checked pubmed and google real quick, and the only mention of AB-001, under the name 1-pentyl-3-(1-adamantoyl)indole, brings up a paper identifying it in a smoking blend in Hungary

I suspect that these, and several other cannabinoids are completely new, and not found in literature. I've found several mentions of synthetic cannabinoids that are 'like' other, known ones, but with 'something added' so that they skirt any existing laws. I would advise against. Even the common synthetics have little information published on them.
 
These I think resemble strong CB2 agonists with low-to-moderate CB1 activity, but I have no good data for that.
 
sekio said:
These I think resemble strong CB2 agonists with low-to-moderate CB1 activity, but I have no good data for that.
Click to expand...

And people should be very careful of these as upon ceasing heavy use all the OPPOSITE effects of CB2 agonists quickly manifest and they're rather nasty.
 
Does anyone know if these cannabinoids will metabolize into nasty metabolites?

hx_ said:
And people should be very careful of these as upon ceasing heavy use all the OPPOSITE effects of CB2 agonists quickly manifest and they're rather nasty.
Click to expand...

Never heard of this, can you elaborate?
 
sekio said:
These I think resemble strong CB2 agonists with low-to-moderate CB1 activity, but I have no good data for that.
Click to expand...
Does it means that they would have powerful cannabiod activity? I always think that CB2 was primary target for new psychedelic cannabioids.
 
Lombergerh said:
Does it means that they would have powerful cannabiod activity? I always think that CB2 was primary target for new psychedelic cannabioids.
Click to expand...

CB2 activation is not psychoactive.
 
Not in the same way as CB1 activation, but does it really have no psychoactive effects at all?

hx_ said:
And people should be very careful of these as upon ceasing heavy use all the OPPOSITE effects of CB2 agonists quickly manifest and they're rather nasty.
Click to expand...

Most of the JWH's etc. have pretty high affinity at CB2, it's probably already downregulated almost as much as possible in heavy users of these isn't it?
 
I swear there has got to be one rouge cannabioid out there with very similar to THC"s partial agonist unique profile. CB-1 and mixed CB-2 are good for your immunologist and the mind.
 
Are there thujone analogs which are active cannabinoids? or is thujone's molecular structure actually too far from the cannabinoid receptor conformation to truly dock? I know it was postulated to have cannabinoid properties itself which seem to be colloquially reported but experimentally rejected.
 
It's hightly unlikely, thujone is a very different structure from THC and freinds.

That said, if fenchyl/adamantyl groups work where the napthyl rings of JWH-018 fit, then I see no reason a substituent vaguely resembling the structure of thujone would not fit as well. Perhaps pinenyl-JWH even.

On a related note I have seen syntheses of 'cleassical' cannabinoids with terpenes such as e.g. verbenone, verbenol etc , that form the 1-methyl-4-isopropenyl-tetrahydrocyclohexane moiety to the resulting THC analog, similar to the actual enzymatic biosynthesis. I haven't seen or heard of (what would likely be) the C5-ring analogs of cannabinoids that you may get from running the synth with thujone or thujols. (Perhaps because they are ultimately inactive?)

But since they don't have recorded Ki values they are still legal, even in states where cannabinoid receptor agonists have been banned.
Click to expand...

This is exactly the kind of fucked up thinking that makes drugs dangerous... 'it's only legal if you know nothing about it...'

Do the states ban rancid peanut oil for its unusually high arachidonic acid content, too?
 
Security through obscurity simply doesn't work.

On another note: Actually, CB2 activation IS psychoactive. UR-144 is strong at a dose of 4mg, even though the CB1 Ki is ~150nM whereas the CB2 Ki is 1.8nM; 83x that of CB1). So that's that settled, I hope.
 
Nah I think UR-144 just demonstrates that low nanomolar Ki isn't required to produce decent effects, if the efficacy is high enough. After all, 150 nM isn't that weak, several of the 5HT2a agonist hallucinogens have Ki values in the hundreds of nM and are still effective. Show me psychoactive effects from one of those super selective CB2 agonists with CB1 Ki over 10,000 nM and I'll believe CB2 can be psychoactive by itself ;-)
 
Limpet_Chicken said:
http://en.wikipedia.org/wiki/JTE-907 This seems to contradict the theory of increased inflammatory procces on withdrawal of CB2 agonist cannabinoids,

It appears the CB2 receptor is somewhat complex in terms of pharmacology.
Click to expand...

Regardless, withdrawing from cannabinoids has various physical effects such as joint pain, cold sweats, diarrhoea, shakes, and disturbances in balance, sleep, speech and appeitite. I would be very surprised if none of these are mediated by CB2.


In other news, now (1-(5-fluoropentyl)-1H-indol-3-yl)(2,2,3,3-tetramethylcyclopropyl)methanone is coming to market, also with no ki or binding data.
 
Whats with the RC industry's fascination with 5-fluoroalkyl substitutions on the indolic nitrogen lately.....Its only a matters of time before they dream up some indole-based cannabinoid with an even-numbered alkyl chain and kill off a few users with fluoroacetate toxicity surely.
 
Limpet_Chicken said:
Whats with the RC industry's fascination with 5-fluoroalkyl substitutions on the indolic nitrogen lately.....Its only a matters of time before they dream up some indole-based cannabinoid with an even-numbered alkyl chain and kill off a few users with fluoroacetate toxicity surely.
Click to expand...

thats what i worry alot about all these new RC's with flourine in them, and the possibility of fluroacetate as a metabolite
 
Now I know it is not new but this seems a better place to post then the mega thread in CD so I am sorry if this annoys anyone by being here.

Does anyone have any info on the negative health impact from AM-2233? To me this feels the worst bodyload and lingers with you for the longest in the strangest way, very uncomftorable and the worst cannabinoid I have tried yet. I am not an ADD goer and would like some more info on this. I am just very interested as I was smoking a blend containing AM-2233 for a while and it fucked me up good and proper.
 
You must log in or register to reply here.
Top