Activation of brain function by S-135, a benzodiazepine receptor inverse agonist

Add time:08/19/2019    Source:sciencedirect.com

1.1. S-135, 2-(5-methylthien-3-y1)-2,5-dihydro-3H-pyrazolo[4,3-c]quinolin-3-one, binds to benzodiazepine receptors with a high affinity and shows pharmacological actions opposite to those of conventional benzodiazepine drugs.2.2. S-135 induced no convulsion in mice by itself, but selectively potentiated the effect of subconvulsive dose of pentylenetetrazole.3.3. S-135 potentiated rat crossed extensor reflex and Ro 15-1788 completely antagonized this potentiation.4.4. S-135 antagonized pentobarbital-induced anesthesia, tetrabenazine-induced ptosis and reserpine-induced hypoactivity and shortened immobilization time in the despair test in mice, indicating that this compound possesses antidepressive properties.5.5. S-135 antagonized amnesia in mice and rats in passive avoidance tasks.6.6. Glucose utilization in brain areas relating to memory and arousal functions was enhanced following S-135 treatment.7.7. These results indicate that S-135 can be a useful drug for activating depressed brain function.

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