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GABA-A Receptor Negative Allosteric

Meaning

A pharmacological agent or endogenous neurosteroid that binds to an allosteric site on the GABA-A receptor, which is distinct from the primary GABA binding site, resulting in a conformational change that decreases the receptor’s sensitivity to GABA. This modulation effectively reduces the inhibitory current mediated by the receptor, thereby increasing neuronal excitability in the central nervous system. This specific action contrasts with positive allosteric modulators, which enhance GABA’s inhibitory effect.