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GABAa Receptor Modulation

Meaning

GABA-A Receptor Modulation is the process of altering the functional activity of the Gamma-aminobutyric acid type A (GABA-A) receptor, which is the principal inhibitory receptor in the central nervous system. This modulation can be achieved by endogenous molecules, such as neurosteroids like Allopregnanolone, or by exogenous pharmacological agents. The effect is typically to enhance the receptor’s response to GABA, thereby increasing the influx of chloride ions and hyperpolarizing the neuron. This inhibitory action is crucial for controlling neuronal excitability and is the basis for anxiolytic, sedative, and anticonvulsant effects.