Effects of phencyclidine and its derivatives on enteric neurones

A. R. Gintzler, R. S. Zukin, S. R. Zukin

Research output: Contribution to journalArticle


The effects of N-(1-phenylcyclohexyl)piperidine (PCP) and related drugs on isolated intact segments of the guinea-pig ileum were determined. 1-1-(2-Thienyl) cyclohexylpiperidine (TCP), PCP and ketamine decreased the height of electrically induced contractions (0.1 Hz) of intact segments of isolated guinea-pig ileum. Thirty to forty percent of the inhibition of contraction height (0.1 Hz) was reversed by pretreatment with the pure narcotic antagonist, naloxone. This naloxone-reversible component showed cross-tolerance with morphine. PCP pretreatment caused a shift to the right in the dose-response curve to acetylcholine (ACh) that was not parallel with the control dose-response curve. Thus PCP does not interact with the muscarinic cholinoceptor in a strictly atropine-like competitive fashion. Binding sites for [3H]-PCP were detected in homogenates of the guinea-pig longitudinal muscle-myenteric plexus preparation. The affinity constants and the rank order of potencies of various PCP derivatives competing with [3H]-PCP for binding suggest that these binding sites are very similar to those found in the central nervous system. These data suggest that the guinea-pig isolated ileum may be used as an in vitro system for studying the mechanism of action of phencyclidines.

Original languageEnglish (US)
Pages (from-to)261-267
Number of pages7
JournalBritish Journal of Pharmacology
Issue number2
StatePublished - 1982
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology

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    Gintzler, A. R., Zukin, R. S., & Zukin, S. R. (1982). Effects of phencyclidine and its derivatives on enteric neurones. British Journal of Pharmacology, 75(2), 261-267.