Potential Nonequilibrium Analgetic Receptor inactIvators. Further Pharmacologic Studies of N-Acylanileridines

A. E. Takemori; Allen Ward; P. S. Portoghese; V. G. Telang

doi:10.1021/jm00256a004

Potential Nonequilibrium Analgetic Receptor inactIvators. Further Pharmacologic Studies of N-Acylanileridines

A. E. Takemori, Allen Ward, P. S. Portoghese, V. G. Telang

Medicinal Chemistry

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Abstract

The antagonistic property of ethyl p-(4-ethoxycarbonyl-4-phenyl-l-piperidinoethyl)fumaranilate (5) was investigated. Compound 5 was found to antagonize morphine analgesia in a complex manner which could not be described as a simple competitive or noncompetitive type. The antagonism, however, lasted for over 6 hr suggesting that 5 has a high affinity for the analgesic receptors. Compound 5 appeared to possess dependence liability in the single-dose suppression test. In the electrically stimulated isolated guinea pig ileum, 5 acted like an agonist. No antagonistic activity of 5 was apparent in the latter two tests.

Original language	English (US)
Pages (from-to)	1051-1054
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	17
Issue number	10
DOIs	https://doi.org/10.1021/jm00256a004
State	Published - Oct 1 1974

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AU - Telang, V. G.

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N2 - The antagonistic property of ethyl p-(4-ethoxycarbonyl-4-phenyl-l-piperidinoethyl)fumaranilate (5) was investigated. Compound 5 was found to antagonize morphine analgesia in a complex manner which could not be described as a simple competitive or noncompetitive type. The antagonism, however, lasted for over 6 hr suggesting that 5 has a high affinity for the analgesic receptors. Compound 5 appeared to possess dependence liability in the single-dose suppression test. In the electrically stimulated isolated guinea pig ileum, 5 acted like an agonist. No antagonistic activity of 5 was apparent in the latter two tests.

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Potential Nonequilibrium Analgetic Receptor inactIvators. Further Pharmacologic Studies of N-Acylanileridines

Abstract

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