Synthesis and analgesic activity of stereoisomers of cis-fluoro-ohmefentanyl
Four stereoisomers 1a–d of cis-fluoro-ohmefentanyl have been synthesized. Their absolute configurations were determined by X-ray analysis of (3S,4R,2″S)-(—)-cis-I d. The analgesic activity (mice, sc, hot plate) revealed
extreme stereodifferences. The ED50 value of (3R,4S,2″S)-(+)-cis-I (1a) was 0.000774 mg/kg (17958 times more potent than that of morphine), while the corresponding antipode 1c was almost inactive.
Document Type: Research Article
Affiliations: 1: Guangzhou Institute of Chemistry, Chinese Academy of Sciences, 1122 Mailbox, Guangzhou/Guangdong, Postleitzahl, P.R. China, Email: [email protected] 2: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
Publication date: 01 May 2003
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