ZAPA, (Z)-3-[(aminoiminomethyl)thio]-2-propenoic acid hydrochloride, a potent agonist at GABA-receptors on the Ascaris muscle cell

  • Br J Pharmacol. 1988 Sep;95(1):3-5. doi: 10.1111/j.1476-5381.1988.tb16540.x.
L Holden-Dye  1 ,  R J Walker
Affiliations
  • 1. Department of Neurophysiology, University of Southampton.
PMID: 2851353 DOI: 10.1111/j.1476-5381.1988.tb16540.x
Abstract

This study is the first report of a compound which is equal in efficacy to gamma-aminobutyric acid (GABA) at the nematode Ascaris muscle GABA-receptor. The GABA-receptor at the Ascaris muscle cell which mediates a membrane hyperpolarization and muscle relaxation has eluded classification. The structure-activity profile of this receptor is not typical of GABAA or GABAB-receptors. Here we report that the isothiouronium compound ZAPA is as potent as GABA at this receptor. This finding has important implications for the characterization of the Ascaris GABA-receptor and the design of novel anthelmintics.

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