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Novel long‐acting benzodiazepine receptor ligands Ro 41‐7812 and Ro 42‐8773: Neurological and behavioral profile
Author(s) -
Moreau JeanLuc,
Jenck François,
Bonetti Erico P.,
Martin James R.,
Haefely Willy E.
Publication year - 1991
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430220409
Subject(s) - benzodiazepine , anticonvulsant , pharmacology , sedation , flumazenil , antagonist , gabaa receptor , receptor , motor activity , diazepam , chemistry , medicine , psychology , neuroscience , epilepsy
The pharmacological profiles of two novel benzodiazepine receptor ligands, Ro 41‐7812 and Ro 42‐8773, were assessed in various tests in mice, rats, and monkeys. Both compounds were orally active, exhibiting clear anticonvulsant activity within a dose range devoid of sedation or motor impairment, as well as effects in an operant conflict test and in a palatable food consumption paradigm. Furthermore, these two compounds attenuated, with a long duration of action, the sedation and motor impairment induced by classical benzodiazepine receptor full agonists but failed to exhibit proconvulsant activity even at high doses. Thus, despite a predominantly antagonist pharmacological profile, these two benzodiazepine receptor ligands appear to exhibit relatively clear anticonvulsant effects and might prove to be of value in the treatment of epilepsies.