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- W2071765304 abstract "5-Methyl,5-phenyl-2-pyrrolidinone (MPP) and 5-ethyl,5-phenyl-2-pyrrolidinone (EPP) were designed and synthesized to penetrate the blood-brain barrier and to be hydrolyzed there to yield γ-amino butyric acid analogs (GABA-analogs) that will inhibit γ-aminobutyric acid-α-ketoglutaric acid transaminase (GABA-T). Both EPP and MPP exhibited significant inhibiting action upon GABA-T activity of mouse and rat brain homogenates. This inhibition was markedly reduced or even disappeared when GABA concentration was doubled, indicating its competitive type. γ-Ethyl-γ-phenyl-γ-aminobutyric acid (EPGABA) caused a stronger inhibition of GABA-T activity of rat brain homogenates, which favors the idea that EPP is hydrolyzed by the homogenates to yield EPGABA, the active substance. The brain levels of glutamic acid, aspartic acid, glutamine, and GABA were not modified by intraperitoneal injection of 160 mg of either EPP or MPP/kg. EPP at doses of 80 and 120 mg/kg exhibited a strong protective action in mice against death caused by thiosemicarbazide: EPP at 80 mg/kg showed an even stronger protection against pentylenetetrazol. Doses of 25 and 50 mg of EPP/kg did not significantly impair a conditioned instrumental response in rats. A dose of 120 mg EPP/kg inhibited completely the conditioned response and also occasionally the unconditioned, but did not inhibit the patellar, flexor, palpebral, and pupillary reflexes. MPP did not affect the conditioned response at doses up to 200 mg/kg. Both EPP and MPP exhibited a powerful anticonvulsive action in rats against maximal electroshock, at doses from 25 to 200 mg/kg. Both the tonic and clonic phases were reduced by 50–98% and were sometimes completely abolished. Diphenylhydantoin produced similar effects in the same experimental conditions." @default.
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- W2071765304 date "1964-07-01" @default.
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- W2071765304 title "Anticonvulsive action of substances designed as inhibitors of γ-aminobutyric acid-α-ketoglutaric acid transaminase" @default.
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- W2071765304 doi "https://doi.org/10.1016/0006-2952(64)90102-9" @default.
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