Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375987 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
Salvinorin A is the only known non-nitrogenous and specific κ-opioid agonist. A series of salvinorin A derivatives were prepared and tested for in vitro activity at the κ-opioid receptor. Unsubstituted carbamate 9 was a potent κ-agonist (EC50 = 6.2 nM) and should be more stable than salvinorin A toward metabolic transformations. Compound 10, containing an N-methyl carbamate at C(2), showed partial agonist activity with 81% efficacy when compared with the full agonist U50,488H. No antagonist ligands were observed.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Cécile Béguin, Michele R. Richards, Yulin Wang, Yong Chen, Lee-Yuan Liu-Chen, Zhongze Ma, David Y.W. Lee, William A. Carlezon Jr., Bruce M. Cohen,