Add time:08/21/2019         Source:sciencedirect.com

The purpose of this study was to re-assess the classification in vivo of a series of (-)-normetazocine derivatives as κ-opioid agonists. From their ability to inhibit contractions of the electrically stimulated rabbit vas deferens, the (2″S)-N-(2″-methoxypropyl) and N-(2″-methoxyisobutyl) derivatives were identified as full agonists. Several partial agonists were discerned, including the (2″S)-N-tetrahydrofurfuryl derivative, Mr2034. (+)-tifluadom, (±)-bremazocine, (-)-ketazocine and (±)-U-50,488 were used as reference compounds. Structure-activity relationships are discussed.

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