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• W165720112 abstract "GABA is the major inhibitory neurotransmitter in the central nervous system (CNS). Virtually all neurons respond to GABA, while about 30% of them make and utilize it as a neurotransmitter. The GABAB receptors are defined as bicuculline-insensitive and baclofen-sensitive. They are members of the G protein-coupled, 7 membrane-spanning receptor family, and are associated with activation of K+ channels or inhibition of Ca’ channels; many times they are located on nerve endings and mediate presynaptic inhibition, including GABA autoreceptors (BOWERY 1993). The recent cloning of the GABAB receptor (KAUPMANN et al. 1997) raises hopes for the development of new drugs based on agonists or antagonists specific for GABAB receptor subtypes. GABAA receptors (GABAR) mediate rapid inhibitory synaptic transmission via chloride channel activation. They are defined by the antagonist bicuculline and the agonist muscimol. The GABA synapse is known to be site of action for many important clinical agents. GABAR appear to be modulated by several classes of CNS depressants, including benzodiazepines (BZ), barbiturates, neuroactive steroids, other general anesthetics including intravenous and volatile agents, and possibly ethanol. These drugs are used for anxiolytic, antiepileptic, sedative/hypnotic, and anesthetic applications. Antagonists of GABAR are generally convulsant, such as the competitive bicuculline and the noncompetitive picrotoxin, pentylenetetrazole, cage convulsants like TBPS, and benzyl penicillin. In addition, some agents acting at the BZ site on GABAR are antagonists of GABA function, and termed `inverse agonists’ (MACDONALD and OLSEN 1994; LUDDENS et al. 1995)." @default.
• W165720112 created "2016-06-24" @default.
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• W165720112 date "2000-01-01" @default.
• W165720112 modified "2023-09-27" @default.
• W165720112 title "GABAA Receptor Chloride Ion Channels" @default.
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• W165720112 doi "https://doi.org/10.1007/978-3-642-57083-4_19" @default.
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