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Intrinsic activity and effects of guanyl-5′-yl imidodiphosphate, Gpp(NH)p and sodium ion on the affinity of dynorphin 1–13, nalorphine and nalorphine-7,8-oxide to kappa-opioid receptor

Authors
Journal
General Pharmacology The Vascular System
0306-3623
Publisher
Elsevier
Publication Date
Volume
16
Issue
6
Identifiers
DOI: 10.1016/0306-3623(85)90153-3

Abstract

Abstract 1. 1. Nalorphine and nalorphine-7,8-oxide (nalorphine epoxide) behaved as partial agonists on the kappa-receptor in the electrically stimulated mouse vas deferens. 2. 2. The effects of a GTP-analogue, GppNHp and Na + on the inhibition of [ 3H]ethylketocyclazocine binding by dynorphin 1–13, nalorphine, its epoxide and naloxone (antagonist) were studied with a synaptosomal fraction of guinea pig brain (except a cerebellum) and compared with the intrinsic activity of the test drugs, which was estimated in the electrically stimulated mouse vas deferens. 3. 3. The effects of GppNHp and Na + on the affinity of the drugs to the kappa-receptor correlated with their intrinsic activities.

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