Sunday, June 20, 2010

NAPTHALENE IS SO OVER

I'm seriously fucking peeved about how few synthetic cannabinoids incorporate a 2-methoxyphenyl moiety. Admittedly, JWH-250 is kind of boring but the same holds true for JWH-018, JWH-081, and JWH-200. JWH-073 is the only one of these compounds which warrants (calculatedly) risking ones health - as it is truly a powerful psychedelic catalyst which surpasses Δ9-THC in every possible way - if not for that pesky (putative) carcinogenic metabolite.

I have heard well informed people say that they think, in terms of carcinogenicity, the napthalene moiety is a red herring, but why? If napthalene is not to blame then what is? Regardless, when one exchanges a 2-methoxyphenyl for napthalene the decrease in potency and binding at CB1 is modest enough that there is really no reason to continue using and selling these naphthyl compounds. In terms of subjective effects the N-butyl compounds like JWH-073 are superior to the more potent N-pentyls - so what about N-butyl JWH-250? I'm sure Huffman has synthed it but I can't look up its numerical designation right now, what I do know is that it has never been sold. It would be only a hair less potent than JWH-073, the same goes for the WIN55212-x compounds which are unexplored and fertile territory and as far as I can tell have never undergone 3-methoxyphenyl substitution.

I wish there were more work done to elucidate the nuanced effects of these cannabinoids - sure affinity at CB1 is an important measure of potency but why are certain cannabinoids more colorful - or psychedelic - or stimulating? As technology stands such tests would require human consumption and a cannabinoid version of Pihkal would probably be very (very) redundant. But now that im getting really into the SAR of CB1 agonists I'm realizing what an insane ligand whore that receptor really is - there is no hope in creating tests to screen for them all - this is only the beginning!!!

Ah, so much work to be done...

7 comments:

Sq. Dave said...

I love your blog, and all your writing. But I wonder how many of your readers actually understand what your talking about. Can you dumb it down a little more? Speak more in terms of effects and side effects maybe? But then again, the esoteric nature of your scientific talk might be half of the charm.

plustaxsail said...

That's the best part. Looking up all these terms and fiuring out what it all means. Expand your mind with more than acid.

Hamilton Morris said...

yeah gonna have to side with plustaxsail, learning is fun. there are many great textbooks on CB receptor biochemistry at your local library - read them and feast on the knowledge!!!

like whats the deal with N-1,1-dimethylheptyl subs on AAIs - can we talk??

plustax said...

that makes it look like pot bro. shit's SORT of like a lock and key similar key hits a similar lock, but you know that. Sides, from what I've just read you want an oxygen on the 1 position and a alkyl group on the 3 position for any activity on the cannaboid receptors.

plustax said...

let me rephrase "shit's SORT of like a lock and key similar key hits a similar lock"

I meant that certain molecules fit into receptors. probably a very basic and crude form of what goes on...

Hamilton Morris said...

oxygen is not necessary for binding, check out JWH-171 the pure hydrocarbon analog of JWH-018, potency is reduced over oxygenated analogs though.

plustax said...

Just a quick question, you have any texts you'd (specifically on cannabinoid receptors) I know you say local library, but I'm not sure where I'd even start.