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Antipentylenetetrazole activity of diazepam a site of action


, : Antipentylenetetrazole activity of diazepam a site of action. Drug Development Research 9(4): 259-266

The site at which pentylenetetrazol (PTZ) and diazepam interact was explored. Neither Ro 15-1788, a benzodiazepine (DZ) receptor antagonist, nor 4,5,6,7-tetrahydroisoxazolo (5,4-c) pyridin-3-ol, (THIP) a .gamma.-aminobutyric acid (GABAA) receptor ligand, alone had any effect on the incidence of PTZ-induced seizures. Ro 15-1788 inhibited the anti-PTZ activity of diazepam but not that of pentobarbital. THIP had no effect on the anti-PTZ activity of diazepam even after toxic doses. Combination studies with diazepam and progabide (GABAA receptor ligand) or diazepam and pentobarbital demonstrate that the anti-PTZ activity of the individual components interact additively. These results imply that GABA-independent BDZ receptors contribute to the anti-PTZ action of BDZs.

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