A Novel Benzodiazepine Partial Inverse Agonist, S-8510, as a Cognitive Enhancer

Pharmacological actions of a novel benzodiazepine partial inverse agonist, S-8510 were examined. S-8510 ameriolated memory impairment induced by cholinergic deficit in rats in addition to augmentation of the LTP in hippocampal slice preparation. Furthermore, S-8510 increased in the extracellular level of acetylcholine in the hippocampus. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimum electrical shock- or strychnine-induced convulsion in mice. These results suggest that S-8510 is a therapeutic drug for senile dementia, including Alzheimer’s disease with little risk for inducing anxiety or convulsion.