Analgesic activity and opiate receptor affinity of new derivatives of N-butylpiperidine

Piotr Janicki, A. Członkowski, B. Osipiak, U. Myszkowska, W. Gumułka, J. Libich, A. Chodkowski, B. Gutkowska

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

Abstract

The three newly synthesized derivatives of N-butylpiperidine 1-butyl-4-phenyl-4-isonicotinoylaminoethylpiperidine (BG 25), 1-butyl-isonicotinoylpiperidine (BG 26) and N-(1-butyl-4-phenyl-4-piperidinoyl) tetrahydropapaverine (BG 9) were evaluated for analgesic activity and opiate receptor affinity. All three compounds showed analgesic activity both in hot-plate and flinch-squeak-jump tests in mice, BG 9 being the most potent. The affinity of the compounds to opiate receptor was moderate (in comparison with pentazocine): the affinity of BG 9 was much greater than that of BG 25 and BG 26. The compounds showed a pronounced inhibitory action in stimulated guinea-pig ileum preparation; this was reversible by naloxone. As evaluated on pA basis, all three investigated compounds showed moderate antagonistic activity. Also in this respect BG 9 was more active than the other two compounds. Cholinolytic and strong spasmolytic properties were observed in isolated rat ileum preparation for BG 9 only.

Original languageEnglish (US)
Pages (from-to)141-148
Number of pages8
JournalPolish Journal of Pharmacology and Pharmacy
Volume32
Issue number2
StatePublished - Dec 1 1980

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science

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