Bicuculline blocks the response to acetylcholine and nicotine but not to muscarine or GABA in isolated insect neuronal somata.

The isolated somata of neurons from the thoracic ganglia of the locust, Locusta migratoria, respond to pressure microapplication of gamma-aminobutyric acid (GABA) and acetylcholine. The acetylcholine receptors fall into two groups. ACh1 (activated by nicotine) and ACh2 (activated by muscarine). The GABA receptor and the ACh1 receptor differ in pharmacology from the known vertebrate receptors. The GABA receptor is insensitive to bicuculline and its salts up to a concentration of 10(-4) M. In contrast, bicuculline is a moderately potent, at least partially competitive antagonist of the ACh1 receptor-mediated response in the thoracic neuronal somata. These observations suggest that classical diagnostic compounds such as bicuculline may show greater cross-reactivity than hitherto suspected among the members of the superfamily of ligand-activated channels.