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

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

Research output: Contribution to journalArticle

12 Citations (Scopus)

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 languageEnglish (US)
Pages (from-to)1051-1054
Number of pages4
JournalJournal of Medicinal Chemistry
Volume17
Issue number10
DOIs
StatePublished - Oct 1 1974

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Ileum
Analgesia
Morphine
Analgesics
Guinea Pigs

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Potential Nonequilibrium Analgetic Receptor inactIvators. Further Pharmacologic Studies of N-Acylanileridines. / Takemori, A. E.; Ward, Allen; Portoghese, Philip S; Telang, V. G.

In: Journal of Medicinal Chemistry, Vol. 17, No. 10, 01.10.1974, p. 1051-1054.

Research output: Contribution to journalArticle

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