Article

Some 14 beta-substituted analogues of N-(cyclopropylmethyl)normorphine.

Journal of Medicinal Chemistry (impact factor: 5.25). 03/1981; 24(2):212-4. pp.212-4
Source: PubMed

ABSTRACT A series of N-(cyclopropylmethyl)-14 beta-substituted-normorphine analogues was synthesized and tested for opioid agonist and antagonist activity in the guinea pig ileum and mouse vas deferens preparations. The 14 beta-bromo compound proved to be a pure antagonist equal in potency to naloxone in the guinea pig ileum assay. In contrast to N-(cyclopropylmethyl)-14 beta-hydroxynormorphine which was a pure antagonist, the corresponding sulfur analogue was about equal to nalorphine in agonist and antagonist potency.

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Keywords

14 beta-bromo compound
 
antagonist potency
 
guinea pig ileum
 
guinea pig ileum assay
 
mouse vas deferens preparations
 
nalorphine
 
potency
 
pure antagonist
 
pure antagonist equal