Abstract
In slices of rat cuneate nucleus, responses to the GABA-A receptor agonist muscimol were potentiated by flurazepam. The maximal potentiation by 1 μM flurazepam was antagonized by the neuronal benzodiazepine receptor ligand Ro15-1788 3 μM, by the quinoline derivative PK8165 0.1 μM and by the peripheral-type benzodiazepine receptor ligand Ro5-4864 0.1 μM. Another ligand for the peripheral-type benzodiazepine receptor, PK11195 10 μM, enhanced the potentiating effect of a submaximal concentration of flurazepam 0.1 μM and prevented the antagonism of flurazepam by Ro5-4864. At much higher concentrations of these drugs, additional effects were seen. Ro15-1788 30 μM and PK11195 30 μM each caused small potentiations of muscimol while Ro5-4864 30 μM caused a small antagonism. Ro15-1788 30 μM, PK8165 100 μM and Ro5-4864 30 μM all antagonized the potentiation of muscimol by pentobarbitone 10 μM; also, PK8165 and Ro5-4864 enhanced the potency of picrotoxin as an antagonist of muscimol. It is concluded that both Ro5-4864 and PK8165 have several distinct effects on the GABA-A receptor complex, all of which could result in reduced responses to muscimol.
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