Behavioural actions of Ro 5-4864: a peripheral-type benzodiazepine?
Ro 5-4864 is a 1,4 benzodiazepine lacking typical benzodiazepine behavioural actions, and which has very low affinity for the "classical" CNS benzodiazepine binding sites. However, Ro 5-4864 has very high affinity for the peripheral type of binding site in the periphery and in the brain. Evidence is reviewed that Ro 5-4864 is sedative, convulsant and anxiogenic in rodents. We also describe the effects of combining Ro 5-4864 treatment with benzodiazepines (e.g. diazepam, chlordiazepoxide) and with other drugs that modify the activity of benzodiazepines (Ro 15-1788, CGS 8216, picrotoxin, PK 11195, phenytoin). The binding sites that might be mediating these behavioural actions of Ro 5-4864 are discussed.
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001570:Benzodiazepinones / Q000378:metabolism* / Q000494:pharmacology; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D003292:Convulsants / Q000378:metabolism* / Q000494:pharmacology; D004347:Drug Interactions; D005442:Flumazenil; D006801:Humans; D007546:Isoquinolines / Q000494:pharmacology; D007668:Kidney / Q000378:metabolism; D010672:Phenytoin / Q000494:pharmacology; D010852:Picrotoxin / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism; D011963:Receptors, GABA-A
D001570:Benzodiazepinones; D003292:Convulsants; D005442:Flumazenil; D007546:Isoquinolines; D010672:Phenytoin; D010852:Picrotoxin; D011720:Pyrazoles; D011956:Receptors, Cell Surface; D011963:Receptors, GABA-A; C028513:4'-chlorodiazepam; C033830:2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one; C037850:PK 11195