Design, Synthesis and Pharmacological Evaluation of Α-substituted N-benzylamides of Γ-hydroxybutyric Acid with Potential Gaba-ergic Activity. Part 6. Search for New Anticonvulsant Compounds
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چکیده
In the recent study we have extended our investigations to the new anticonvulsant derivatives of αsubstituted N-benzylamides of γ-hydroxybutyric acid (GHB). Among the obtained compounds N-benzylamide of α-(1,2,3,4-tetrahydroisoquinoline)-GHB (9) has demonstrated activity against maximal electroshock (MES) induced seizures in mice (at 100 mg/kg ip) and in rats (at 30 mg/kg, po dose). Lactone 8 and amide 9 have possessed a weak effect on [H]-muscimol binding. Molecular modeling studies have revealed that anticonvulsant activity of the α-substituted amides of GHB might partially be explained by the orientation of the terminal ben-
منابع مشابه
Synthesis and pharmacological evaluation of new 4,4-diphenylbut-3-enyl derivatives of 4-hydroxybutanamides as GABA uptake inhibitors.
γ-Aminobutyric acid (GABA) is an inhibitory neurotransmitter concerned with the control of neuronal activity in the mammalian central nervous system (CNS). There is considerable direct and indirect evidence that impair activity of GABA-mediated inhibitory synapses may be an important causative factor in experimental and clinical seizure disorders (1, 2). Enhancement of GABA transmission by inhi...
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