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ZAPA, (Z)‐3‐[(aminoiminomethyl)thio]‐2‐propenoic acid hydrochloride, a potent agonist at GABA‐receptors on the Ascaris muscle cell
Author(s) -
HoldenDye L.,
Walker R.J.
Publication year - 1988
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1988.tb16540.x
Subject(s) - gabaa receptor , receptor , ascaris , gabab receptor , agonist , gamma aminobutyric acid , gaba receptor , chemistry , pharmacology , inhibitory postsynaptic potential , muscle relaxation , biology , biochemistry , endocrinology , immunology , helminths
This study is the first report of a compound which is equal in efficacy to γ‐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 GABA A or GABA B ‐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.