GS-39783

GS-39783

CAT N°: 29482
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From 102.00 86.70

GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTP?S binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 ?M, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 ?M). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}

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