A positive allosteric modulator of GABAB receptors; potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM

GS-39783 – 50 mg

Brand:
Cayman
CAS:
39069-52-8
Storage:
-20
UN-No:
Non-Hazardous - /

GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). 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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Description

A positive allosteric modulator of GABAB receptors; potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively); amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM); suppresses alcohol self-administration in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats from 25-100 mg/kg; reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice; reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg)

Formal name: N4,N6-dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine

Synonyms: 

Molecular weight: 337.4

CAS: 39069-52-8

Purity: ≥98%

Formulation: A crystalline solid

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