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Psychedelic Imidazolines

nuke

nuke

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Activities of novel aryloxyalkylimidazolines on rat 5-HT2A and 5-HT2C receptors

Barry W. Siegel, Jules Freedman, Mark J. Vaal and Bruce M. Baron
Marion Merrell Dow Research Institute, 2110 East Galbraith Road, Cincinnati, OH 45215, USA
Received 27 April 1995; revised 9 October 1995; accepted 20 October 1995. ; Available online 2 March 1999.

Abstract

Using transfected NIH 3T3 mouse fibroblast cell lines expressing the rat 5-HT2A and rat 5-HT2C receptor subtypes, and techniques of 2-[125I](+)-iodolysergic acid diethylamide ([125I]LSD) binding and serotonin (5-hydroxytryptamine, 5-HT)-stimulated phosphoinositide hydrolysis, we have characterized a new structural class of 5-HT receptor ligands, the aryloxyalkylimidazolines. These compounds were found to be potent competitors of [125I]LSD binding at both receptor subtypes (Ki 5–200 nM) and to have efficacy ranging from potent competitive antagonists (IC50 25 nM) to moderately potent full agonists (EC50 200 nM). Some of these compounds are agonists at both receptor subtypes, while others are 5-HT2C receptor agonists with 5-HT2A receptor antagonist activity. None of the aryloxyalkylimidazolines reported here have 5-HT2A or 5-HT2C receptor selective antagonist activity. Since these compounds are novel structures, we compared them with a variety of reference 5-HT receptor ligands selected from other chemical classes that have previously been studied at 5-HT2A and 5-HT2C receptors in native tissues.
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Strange I never heard anything about these before.. Full text would be awesome.

http://www.sciencedirect.com/scienc...serid=10&md5=4608c362ac3b0801aa4915e828f2fa86

Not only that, these would probably bypass the USA analogue act to a good extent because there aren't any other controlled imidazoline drugs.
 
I'm sure i'm just being stupid but don't those ki's also suggest mCPP would be a psychedelic? It seems to be a reasonably strong agonist too.

I thought that SKF83566 was interesting looking at the affinity then i noticed that its more of an antagonist! Not very good with this stuff!
 
This is super interesting, really. I can't believe it's taken 11 years to even be discussed at Bluelight.

What sort of side effects should be anticipated?
 
dorothyperkins said:
I'm sure i'm just being stupid but don't those ki's also suggest mCPP would be a psychedelic? It seems to be a reasonably strong agonist too.
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It is considered a sort of psychedelic, I think one of the big problems was that it was a 5HT1A antagonist and thus enabled things like panicking and other stimulatory weirdness.

Full agonists kind of scare me too, the higher the dose the more likely the effect won't saturate and will keep going higher (unlike LSD or 2c-b).
 
Reminds me, took a load of nefadozone in my more reckless days, caused some wierd hallucinations, the most persistent being an apparent snowstorm of black blobs. Also caused me to appear very drunk, never again!
 
nefadozone??? Wow- that's um.... eek!

I assume you're talking about more delirient-esque visuals, not serotonergic ones?
 
mCPP is clearly psychedelic at the right dose. Nowhere near the extent of tryptamines or phenethylamines, but you can definitely tell that the same sort of mechanism is probably going on, at least to some degree.
 
Yeah not serotonergic at all, and i've never tried mCPP so i can't say weather it was from the nefadozone itself or mCPP produced by its metabolism.

Edit: It doesn't sound like mCPP, the few reports i checked on erowid mentioned that it was kind of psychedelic.
 
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The interesting thing about compound 101156 is that it it impacts 5HT2C much more strongly than 5HT2A. This may actually be a really neat compound to assay because it would show what minor 5HT2A and strong 5HT2C action is like.
 
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