Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect

Bioorg Med Chem Lett. 2009 Mar 17.
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect.
Srivastava BK, Soni R, Patel JZ, Joharapurkar A, Sadhwani N, Kshirsagar S, Mishra B, Takale V, Gupta S, Pandya P, Kapadnis P, Solanki M, Patel H, Mitra P, Jain MR, Patel PR.

Department of Medicinal Chemistry, Zydus Research Centre, Sarkhej-Bavla N. H. 8A, Moraiya, Ahmedabad 382 210, India.

A few thienyl substituted pyrazole derivatives were synthesized to aid in the characterization of the cannabinoid receptor antagonist and also to serve as potentially useful antiobesity agent. Structural requirements for selective CB1 receptor antagonistic activity of 5-thienyl pyrazole derivatives included the structural similarity with potent, specific antagonist rimonabant 1. Compound 3 has been identified as a hair growth stimulator and an antiobesity agent in animal models.

Capsaicin from Cayenne pepper does essentially the same thing.

CS -

you mentioned in another post that taking cayenne pepper along with other supplements may increase their bioavailability similar as bioperine does?
Is that true? Did I get it right?
If yes, does cayenne mess up with detoxification and removal of carcinogenic compounds similarly also?
How do you explain that some users had to stop taking cayenne pepper as it made them shed?

edony - This study may shed some light on this:

http://www.ncbi.nlm.nih.gov/pubmed/17487234

It's a bit technical, so the basically it says that Uridine dinucleotide phosphate (UDP)-glucuronyl transferase activity is decreased by a combination of curcumin & cayenne (not cayenne by itself). Uridine dinucleotide phosphate (UDP)-glucuronyl transferase activity is required for glucuronidation.

Be aware that Piperine and Cayenne have some similar actions, but not entirely the same. They are all, including curcumin, human vanilloid receptor agonists.

Piperline has some unknowns and not everything is clear. This is one study relating to Cayenne increasing the absorption of certain substances such as theophylline.

Was the shedding of cayenne from topical or internal use? I have not had that experience from either method, but if this is truly the case for them, it would buck the results of two studies which demonstrate cayenne to aid in hair growth.

I didn't see any increase in uptake from cayenne myself -- or if there was, it wasn't very noticeable.