Verlinde C, De Ranter C
Laboratorium voor Analytische Chemie en Medicinale Fysicochemie, Katholieke Universiteit Leuven, Belgium.
Eur J Pharmacol. 1988 Aug 9;153(1):83-7. doi: 10.1016/0014-2999(88)90590-0.
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.
本研究的目的是重新评估一系列（-）-去甲美沙酮衍生物作为κ-阿片受体激动剂在体内的分类。根据它们抑制电刺激兔输精管收缩的能力，鉴定出（2“S）-N-（2”-甲氧基丙基）和N-（2”-甲氧基异丁基）衍生物为完全激动剂。识别出了几种部分激动剂，包括（2“S）-N-四氢糠基衍生物Mr2034。（+）-替氟朵、（+/-）-布马佐辛、（-）-凯他佐辛和（+/-）-U-50,488用作参考化合物。讨论了构效关系。
