Chemical Name:N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidin
ediamine
Biological Activity:
Novel positive allosteric modulator of GABAB
receptor function. Potentiates the effects of GABA on [35S]GTPγS binding at
recombinant and native GABAB receptors (EC50 values are
2.1 and 3.1μM
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.
Urwyler et al
(2003) N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine
(GS39783) and structurally related compounds: novel allosteric enhancers of γ-aminobutyric acidB
receptor function. J.Pharmacol.Exp.Ther. 307 322. Cryanet
al (2004) Behavioral characterization of the novel GABAB
receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine:
anxiolytic-like activity without side effects associated with baclofen or
benzodiazepines. J.Pharmacol.Exp.Ther. 310 952. Mombereauet
al (2007) GABAB receptor-positive modulation-induced blockade of
the rewarding effects of nicotine is associated with a reduction in nucleus
accumbens DFosB
accumulation. J.Pharmacol.Exp.Ther. 321 172.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.
