ABSTRACT
The role of GABAergic mechanisms in realization of the effects of afobazole and picamilon on the cerebral circulation was studied in rats. It is found that the cerebrovascular effect of afobazole significantly decreases on the background of the GABA receptor antagonists bicuculline and picrotoxin. This is evidence of an important role of the GABA system in the its cerebrovascular and neuroprotective activity of afobazole. The results of experiments with picamilon showed that the cerebrovascular effect of this drug is not affected by receptor blocking with bicucullin. However, the blocking of chloride channels of the GABA receptors by picrotoxin significantly decreased the effect of picamilon on the cerebral blood flow.
Subject(s)
Analgesics/administration & dosage , Benzimidazoles/administration & dosage , Cerebellum/blood supply , Morpholines/administration & dosage , Receptors, GABA/metabolism , gamma-Aminobutyric Acid/analogs & derivatives , gamma-Aminobutyric Acid/administration & dosage , Animals , Bicuculline/administration & dosage , Cerebellum/metabolism , GABA Antagonists/administration & dosage , Picrotoxin , Rats , Regional Blood Flow/drug effectsABSTRACT
The selective anxiolytic drug afobazole administered in a dose of 5 mg/kg increased the cerebral blood flow in rats. The effect was more pronounced in rats with global reversible cerebral ischemia than in intact animals. The ischemia model was caused by occlusion of both common carotid arteries for 120 min with simultaneous reduction of the arterial pressure to 40-50 mm Hg through blood-letting. Afobazole also significantly increased the survival of rats with cerebral ischemia model caused by ligation of both common carotid arteries, which was evidence of the neuroprotector activity. Apparently, the ability of afobazole to improve the cerebral blood flow in ischemized rat brain is an important factor in realization of the neuroprotector activity.
