A naloxone-steroid hybrid azine with selective and long-acting opioid antagonism at delta receptors in vitro.

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Koman A, Kolb VM, Terenius L

A naloxone-steroid hybrid azine with selective and long-acting opioid antagonism at delta receptors in vitro.

Pharm Res. 1987 Apr;4(2):147-9.

PubMed ID

2855368 [ View in PubMed

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Abstract

The interaction of naloxone estrone azine (N-EH) with various opioid receptor types was studied in vitro. Its potency as an antagonist of opioid effects was compared to that of naloxone on the electrically evoked contractions of mouse vas deferens (Mvd) and guinea pig ileum myenteric plexus longitudinal muscle (Gpi) preparations. N-EH was found to be 9-fold more potent than naloxone in antagonizing the effects of D-Ala2-Leu5-enkephalin in the Mvd and 22-fold less potent in antagonizing normorphine in the Gpi. In the Mvd, the recovery half-time for N-EH was longer than 1000 min. Neither compound showed agonism. The two compounds were also compared for their capacity to displace the binding of 3H-D-Ala2-Leu5-enkephalin, 3H-dihydromorphine, and 3H-ethylketocyclazocine to rat brain membranes under conditions where delta, mu, and kappa sites were labeled. The relative affinities were 0.70, 0.16, and 0.14 for N-EH and 0.05, 0.87, and 0.08 for naloxone, respectively. Thus, compared to naloxone, which is mu selective, N-EH is a delta-selective antagonist.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dihydromorphine	E3 ubiquitin-protein ligase TRIM13	Protein	Humans	Unknown	Agonist	Details