Leelamine

[Ham-milton]

Leelamine is a diterpene molecule whose name derives from the Sanskrit word leela which means “play”. It has weak affinity for the human central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors, exhibiting 20% displacement of [3H]-CP55940 at a concentration of 10 µM.1 Leelamine inhibits pyruvate dehydrogenase kinase (PDK) with an IC50 value of 9.5 µM.2 Derivatives of leelamine exhibit anti-inflammatory activity and show moderate inhibition of phospholipase A2 activity from a variety of sources.3
1 Martin, B.R. Leelamine. (6 Apr 27).
2 Aicher, T.D., Damon, R.E., Koletar, J., et al. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK). Biooganic & Medicinal Chemistry Letters 9 2223-2228 (1999).
3 Wilkerson, W., DeLucca, I., Galbraith, W., et al. Antiinflammatory phospholipase-A2 inhibitors. I. Eur J Med Chem 26 667-676 (1991).

I was wondering what sort of recreational effects this might have? I can't provide a link to the source of that quote because it's from a vendor, but I found it quite interesting.

As many people have found with high-affinity CB1 agonists, they're just not very good recreationally, and since scientists are more interested in creating the most potent, strongest binding, bestest whatever, substance, low affinity cb1 agonists like THC are kinda falling by the wayside.

So, aside from the unusual peripheral effects (I assume they're unusual and peripheral side effects not from the CB1 agonism).

---

I just watched the Episode of Family Guy where Peter and Lois get stoned and reform a band- and they have a big concert and everyone gets pissed because they suck.

Later Chris explains that they were so baked they only sounded good to themselves.

Lois says, "And we thought the weed was inspiring us."

Chris replies, " Actually Mom, Dad, that's a popular misconception. The active ingredient in Marijuana is THC, a psychedelic that's a mild form of Acid. It has many adverse effects, including loss of sexual potency, major damage to the brain, central nervous system, and [I forget]. In short, there's a reason they call it 'dope.'"

I found that hilarious- but c'mon- they should really have done more research about it before saying retarded shit like that.

 

[dorothyperkins]

I like the name! Do you have the structure?

Wierd with family guy, i like the drug references in some of them, like peter takes e and starts smoking crack! hehe

 

[LuxEtVeritas]

i think family guy must have been being tongue and cheek all the ay withth at as they seem to be VERY liberal guys in most regards --- the show is one of the best irreverent comedies on TV

anyway this is i guess OT , LOL

 

[LuxEtVeritas]

i believe this barely would do anything even if you could shoot it icv

 

[Pomzazed]

Leelamine Structure :

 

[Riemann Zeta]

Looks like a cannabinoid alright. I don't think it would be orally active (but I see no reason why it a priori wouldn't be), but that's not the real problem. The real problem is the super-weak receptor affinity. I realize that CP-55960 is a super-high potency agonist, but still, a 10uM EC20? I don't like the sound of the pyruvate dehydrogenase inhibitor concentration being equal. Don't I use that enzyme for all sorts of things, like living, for example?

I remember that Family Guy, I couldn't believe that they threw that DARE horseshit into the episode. It's like someone got ahold of the script and just snuck that in. I remember the Family Guy where Peter asked: "where did you get that tattoo?" and Lois replies: "I'm not really sure--meth is a hell of a drug."