Pro- and anti-convulsant drug effects in combination with the convulsant benzodiazepine Ro 5–4864

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Abstract
The effects of several compounds believed to act at the GABA-benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol (leptazol, pentylenetetrazole) were investigated in combination with the convulsant benzodiazepine Ro 5–4864. Tracazolate (25–100 mg kg−1) failed to affect convulsions induced by Ro 5–4864; however, they were prevented by treatment with CL 218, 872 (20 mg kg−1). Compounds having proconvulsant activity in combination with a subthreshold dose of Ro 5–4864 were: CL 218,872 (5 mg kg−1), and CGS 8216 (20 mg kg−1) and FG 7142 (40 mg kg−1), two compounds characterized as ‘inverse agonists’; at benzodiazepine receptors. The phenylquinolines PK 8165 and PK 9084, originally believed to have anxiolytic properties, had no significant effect in combination with Ro 5–4864 (25–100 mg kg−1). The convulsant profile of Ro 5–4864 is compared with that of picrotoxin and pentetrazol.