Some 14.beta.-substituted analogs of N-(cyclopropylmethyl)normorphine
| Autor: | Hans W. Kosterlitz, Maureen G. C. Gillan, Sydney Archer, Peter Osei-Gyimah |
|---|---|
| Rok vydání: | 1981 |
| Předmět: |
Male
Chemical Phenomena Stereochemistry Guinea Pigs Mouse Vas Deferens Nalorphine (+)-Naloxone In Vitro Techniques Mice Vas Deferens Ileum Drug Discovery medicine Animals Potency Guinea pig ileum Beta (finance) Normorphine Morphine Derivatives Morphine Chemistry Antagonist Muscle Smooth Molecular Medicine medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 24:212-214 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00134a018 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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