ZAPA, (Z)-3-[(aminoiminomethyl)thio]-2-propenoic acid hydrochloride, a potent agonist at GABA-receptors on the Ascaris muscle cell.
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.
Holden-Dye
L
L
Department of Neurophysiology, University of Southampton.
Walker
R J
RJ
D000179:Acrylates / Q000494:pharmacology*; D000818:Animals; D001200:Ascaris / Q000378:metabolism*; D066298:In Vitro Techniques; D008564:Membrane Potentials / Q000187:drug effects; D008839:Microelectrodes; D009132:Muscles / Q000166:cytology / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism
D000179:Acrylates; D011963:Receptors, GABA-A; C058552:3-((aminoiminomethyl)thio)-2-propenoic acid