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Discovery of Novel TRPV1 Ligands through Rational Approach Based on Its Putative Endogenous Ligand, 12(S)-HPETE
- Authors
- Min, Kyung Hoon; Lee, Seul; Kim, Hwa Soon; Suh, Young-Ger
- Issue Date
- 20-Jun-2010
- Publisher
- KOREAN CHEMICAL SOC
- Keywords
- TRPV1; 12(S)-HPETE; Vanilloid receptor; Antagonist
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.31, no.6, pp 1501 - 1505
- Pages
- 5
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 31
- Number
- 6
- Start Page
- 1501
- End Page
- 1505
- ISSN
- 0253-2964
1229-5949
- Abstract
- We report design and synthesis of the novel TRPV1 ligands through a rational approach. Simplified analogues of 12(S)-HPETE showing TRPV1 agonistic effect are disclosed. Biological evaluation revealed that substitution of functional groups without any change in conformation converted agonist into antagonist. Our work provided key information with regard to TRPV1 agonist/antagonist switching.
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