Pharmaceutisch Weekblad

, Volume 2, Issue 1, pp 1121–1127 | Cite as

The acetylcholinesterase inhibitory activity of metoclopramide and some of its biotransformation products

  • G. Huizing
  • A. H. Beckett
Original Article


Ki values were determined for thein vitro acetylcholinesterase inhibitory activity of the anti-emetic metoclopramide, some of its metabolic products and the newly synthesised N-(ethyl)-4-chlorobenzamide (1). Metoclopramide was a moderate inhibitor, 113 times more potent than 1 and 50 times less potent than physostigmine. Metabolic products of N-de-ethylation, N-di-de-ethylation, deamination followed by reduction and amide hydrolysis were increasingly less active as inhibitors. The implications of the present findings are briefly discussed.


Public Health Ethyl Internal Medicine Amide Inhibitory Activity 
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Copyright information

© Bohn, Scheltema & Holkema 1980

Authors and Affiliations

  • G. Huizing
    • 1
  • A. H. Beckett
    • 1
  1. 1.Department of Pharmacy, Chelsea CollegeUniversity of LondonLondonGreat Britain

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