5-HT2A receptor agonist/antagonist extracted from Litsea sessilis

[BilZ0r]

Phytother Res. 2008 Oct 9. [Epub ahead of print]
5-Hydroxytryptamine(2A) receptor binding activity of compounds from Litsea sessilis.
Chung LY, Lo MW, Mustafa MR, Goh SH, Imiyabir Z.

Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.

A 96-well microplate filtration based 5-HT(2A) receptor-radioligand binding assay was optimized and adopted to carry out a bioassay-guided fractionation of the methanol extract of the leaves of Litsea sessilis. This purification led to the isolation of two compounds identified as (+)-boldine (1) and (+)-dehydrovomifoliol (2). (+)-Boldine binds to 5-HT(2A) receptors at high concentrations with a K(i) value of 2.16 microm. However, (+)-dehydrovomifoliol showed minimal competitive inhibition on the binding of [(3)H]ketanserin to the same receptor with a K(i) value of 2.06 mm. These results suggest that (+)-boldine influences the activity of 5-HT(2A) receptors through competitive binding as an agonist or antagonist. Copyright (c) 2008 John Wiley & Sons, Ltd.

 

[Hammilton]

I'm familiar with boldine, but not the other. this link is interesting:
http://www.ars-grin.gov/cgi-bin/duke/chemical.pl?BOLDINE

 

[LuxEtVeritas]

that it was boldine was quite disappointing from the title getting me a bit excited

 

[Riemann Zeta]

Yeah, the compound is clearly an antagonist at the 5-HT2A receptor. It is similar in structure to the compound nantenine, which is a natural 5-HT2A antagonist that was briefly studied as an "MDMA blocker."

 

[Hammilton]

too bad, there are too many 5HT2a antagonists that can't be modified to get an agonist.

 

[BilZ0r]

My bad.