An Opioid Agonist with Preference for κ‐Opioid Receptors: (−)‐N‐Cyclopropylmethylmorphinan‐6‐one
1990
N-Cyclopropylmethyl- and N-cyclobutylmethylmorphinan-6-one (3 and 4, respectively) were prepared from N-methylmorphinan-6-one (1). The pharmacological studies showed 3 and 4 to be potent opioid agonists. Compound 3 was found to have preference for κ rather than μ opioid receptors.
Ein Opiatagonist mit Praferenz fur κ-Opiatrezeptoren: (−)-N-Cyclopropylmethylmorphinan-6-on
N-Cyclopropylmethyl- und N-Cyclobutylmethylmorphinan-6-on wurden ausgehend von N-Methylmorphinan-6-on (1) hergestellt. Die pharmakologischen Studien zeigen, das 3 und 4 hoch wirksame Opiatagonisten sind. Verbindung 3 hat hohere Affinitat zu κ-Opiatrezeptoren als zu μ-Opiatrezeptoren.
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