DMD Large equally mixed donor pool

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

Drug Metabolism and Disposition Fast Forward
First published on January 7, 2008; DOI: 10.1124/dmd.107.019240

0090-9556/08/3604-670-675$20.00
DMD 36:670-675, 2008

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow All Versions of this Article:
dmd.107.019240v1
36/4/670    most recent
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Chanda, S.
Right arrow Articles by Bley, K.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Chanda, S.
Right arrow Articles by Bley, K.

In Vitro Hepatic and Skin Metabolism of Capsaicin

Sanjay Chanda, Mohammad Bashir, Sunita Babbar, Aruna Koganti, and Keith Bley

NeurogesX, Inc., San Mateo, California (S.C., S.B., K.B.); Covance Laboratories, Madison, Wisconsin (M.B.); and In Vitro Technologies, Inc., Baltimore, Maryland (A.K.)

On the basis of the ability of capsaicin to activate the transient receptor potential vanilloid 1 receptor (TRPV1) expressed in nociceptive sensory neurons, topical and injectable high-concentration formulations are being developed as potential treatments for various pain syndromes. As much of the published literature on capsaicin is based on pepper extracts, which are typically a mixture of capsaicin and other capsaicinoids (including norhydrocapsaicin, dihydrocapsaicin, homocapsaicin and homodihydrocapsaicin), the purpose of this investigation was to study the in vitro metabolism of pure capsaicin. The metabolism of capsaicin was similar in human, rat, and dog microsomes and S9 fractions. In these assays, three major metabolites were detected and identified as 16-hydroxycapsaicin, 17-hydroxycapsaicin, and 16,17-dehydrocapsaicin. In addition to these three metabolites, rat microsomes and S9 fractions also produced vanillylamine and vanillin. Biotransformation of capsaicin was slow in human skin in vitro, with the majority of the applied capsaicin remaining unchanged and a small fraction being metabolized to vanillylamine and vanillic acid. These data suggest that the metabolism of capsaicin by cytochrome P450 enzymes in skin is minimal, relative to hepatic metabolism.

Address correspondence to: Dr. Sanjay Chanda, NeurogesX, Inc., 2215 Bridgepointe Parkway, Suite 200, San Carlos, CA 94404. E-mail: schanda{at}neurogesx.com




This article has been cited by other articles:


Home page
 Drug Metab. Dispos.Home page
C. K. Svensson
Biotransformation of Drugs in Human Skin
Drug Metab. Dispos., February 1, 2009; 37(2): 247 - 253.
[Abstract] [Full Text] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 2008 by the American Society for Pharmacology and Experimental Therapeutics.