Uses
GS 39783 is an allosteric positive modulator of GABAB receptors. GS 39783 attenuates acute cocaine-induced hyperlocomotion and blocks cocaine-induced Fos induction in the striatal complex.
Definition
ChEBI: N4,N6-dicyclopentyl-2-(methylthio)-5-nitropyrimidine-4,6-diamine is an aryl sulfide.
Biological Activity
Novel positive allosteric modulator of GABA B receptor function. Potentiates the effects of GABA on [ 35 S]GTP γ S binding at recombinant and native GABA B receptors (EC 50 values are 2.1 and 3.1 μ M respectively). Decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines.
