Potential Nonequilibrium Analgetic Receptor Inactivators. Synthesis and Biological Activities of N-Acylanileridines

P. S. Portoghese, V. G. Telang, A. E. Takemoei, G. Hayashi

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

In a effort to prepare nonequilibrium analgetic receptor inactivators, a variety of Ar-acylanileridines having alkylating capacity were synthesized. The analgetic potencies of this series are reported together with experiments designed to detect receptor blockade. Ethyl p-(4-ethoxycarbonyl-4-phenyl-1-piperidinoethyr, fumaranilate (5) caused significant blockade of analgetic activity 2 hr after ip administration. Pretreatment with naloxone, a narcotic antagonist, blocked completely the analgetic activity of 5. Naloxone also protected the analgetic receptors against inactivation. The data suggest that 5 has the capacity to alkylate analgetic receptors selectively.

Original languageEnglish (US)
Pages (from-to)144-148
Number of pages5
JournalJournal of medicinal chemistry
Volume14
Issue number2
DOIs
StatePublished - Feb 1 1971

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