Assessment of the kappa-opioid activity of a series of 6,7-benzomorphans in the rabbit vas deferens.
The purpose of this study was to re-assess the classification in vivo of a series of (-)-normetazocine derivatives as kappa-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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Laboratorium voor Analytische Chemie en Medicinale Fysicochemie, Katholieke Universiteit Leuven, Belgium.
De Ranter
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D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology*; D004558:Electric Stimulation; D066298:In Vitro Techniques; D008297:Male; D009019:Morphinans / Q000494:pharmacology*; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000378:metabolism* / Q000502:physiology; D011817:Rabbits; D011957:Receptors, Opioid / Q000378:metabolism*; D017473:Receptors, Opioid, kappa; D014649:Vas Deferens / Q000378:metabolism / Q000502:physiology
D001575:Benzomorphans; D009019:Morphinans; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa