Benzodiazepines do not alter the production, release, or metabolism of GABA but instead potentiates its inhibitory actions by augmenting or enhancing receptor binding. ![]() Benzodiazepines bind at the interface of the GABA-A receptor and subsequently lock the receptor into a configuration that increases its affinity for GABA. ![]() The GABA-A receptor, depending on various arrangements of its subunits, determines its affinity for various agents that bind to the receptor. Benzodiazepines exert their effect via modulation of the gamma-aminobutyric acid A (GABA-A) receptor, the primary inhibitory neurotransmitter in the central nervous system. Benzodiazepines are organic bases with a benzene ring and a 7-member diazepine moiety, with variable side chains that determine the potency, duration of action, metabolite activity, and rate of elimination.
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