Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues

A series of salvinorin A derivatives modified at the C(4) position were prepared and screened for binding and functional activities at the human κ-opioid receptor. Several selective κ-full agonists are reported. Salvinorin A, a compound isolated from the plant Salvia divinorum, is a potent and highl...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (21), p.5498-5502
Main Authors: Lee, David Y.W., He, Minsheng, Liu-Chen, Lee-Yuan, Wang, Yulin, Li, Jian-Guo, Xu, Wei, Ma, Zhongze, Carlezon, William A., Cohen, Bruce
Format: Article
Language:English
Subjects:
Agonist
Animals
Biological and medical sciences
CHO Cells
Cricetinae
Cricetulus
Diterpenes - chemical synthesis
Diterpenes - pharmacology
Diterpenes, Clerodane
Humans
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Noclerodane diterpene
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Receptors, Opioid, kappa - agonists
Receptors, Opioid, kappa - metabolism
Salvia
Salvinorin
κ-Opioid receptor
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Summary:A series of salvinorin A derivatives modified at the C(4) position were prepared and screened for binding and functional activities at the human κ-opioid receptor. Several selective κ-full agonists are reported. Salvinorin A, a compound isolated from the plant Salvia divinorum, is a potent and highly selective agonist for the κ opioid receptor. For exploration of its structure and activity relationships, further modifications, such as reduction at the C(4) position, have been studied and a series of salvinorin A derivatives were prepared. These C(4)-modified salvinorin A analogues were screened for binding and functional activities at the human κ-opioid receptor and several new full agonists have been identified.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.08.051