title: Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
abstract: Salvinorin A is the most potent naturally occurring opioid agonist with a high selectivity and affinity for kappa-opioid receptor. To explore its structure-activity relationships, modifications 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 kappa-opioid receptor and several potent new agonists have been identified.
authors.affiliation: Bioorganic and Natural Products Laboratory, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
authors.forename: David Y W
authors.initials: DY
authors.lastname: Lee
authors.forename: Minsheng
authors.initials: M
authors.lastname: He
authors.forename: Leelakrishna
authors.initials: L
authors.lastname: Kondaveti
authors.forename: Lee-Yuan
authors.initials: LY
authors.lastname: Liu-Chen
authors.forename: Zhongze
authors.initials: Z
authors.lastname: Ma
authors.forename: Yulin
authors.initials: Y
authors.lastname: Wang
authors.forename: Yong
authors.initials: Y
authors.lastname: Chen
authors.forename: Jian-Guo
authors.initials: JG
authors.lastname: Li
authors.forename: Cecile
authors.initials: C
authors.lastname: Beguin
authors.forename: William A
authors.initials: WA
authors.lastname: Carlezon
authors.forename: Bruce
authors.initials: B
authors.lastname: Cohen
mesh_terms: D000701:Analgesics, Opioid / Q000138:chemical synthesis* / Q000494:pharmacology; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045785:Diterpenes, Clerodane; D004353:Drug Evaluation, Preclinical; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000701:Analgesics, Opioid; D004224:Diterpenes; D045785:Diterpenes, Clerodane; D017473:Receptors, Opioid, kappa; D016244:Guanosine 5'-O-(3-Thiotriphosphate); C090499:salvinorin A