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Recent Advances And Basis Of Drug Design In Gaba-Nergic Agonist

Author(s): Shashikant V.Bhandari | Mr. A.A.Patil | Dr.K.G.Bothara

Journal: Pharmaceutical Reviews
ISSN 1918-5561

Volume: 5;
Issue: 2;
Date: 2007;
Original page

ABA plays an important role in the arrest of convulsions. Many anticonvulsant drugs are reported to act by increasing the GABA level in the brain. Drug that enhance GABA-nergic transmission are anxiolytics, antiepileptics, muscle-relaxant and sedative hypnotics.GABA is the major inhibitory amino acid transmitter of the mammalian central nervous system and it is present in some 40% of all neurons. Iontophoretic application of GABA in CNS, indicating that it generally produced inhibitory hyperpolarizing responses on neurons, which were blocked competitively by the alkaloid bicuculline. The hyperpolarizing response is due to an increase in the chloride conductance of the neuronal membrane allowing chloride ions to flow down their electrochemical gradient into the cell.The benzodiazepines have an anticonvulsant action in addition to the anxiolytic activity. Recent work has helped distinguish between the two roles for the benzodiazepines. Picrotoxin is a convulsant, which interacts with the GABA receptor complex and blocks the Cl- ionophore. A variety of hypnotic, anesthetic and anticonvulsant drugs interact with a dihydropicrotoxin binding site, and may act as Cl- ionophore agonists. Barbiturates such as pentobarbital and phenobarbital enhance GABA binding in proportion to general anesthetic activity.
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