CGP 36742

CGP 36742 (SGS-742) is an orally active and selective antagonist of GABA_B receptor (IC₅₀ = 36 µM). CGP 36742 is a brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study^[1][2][3][4]. IC50 & Target:IC50: 32 μM (GABA_B)^[1] In Vitro:CGP 36742 blocks the late inhibitory postsynaptic potential (i.p.s.p.) in CA1 pyramidal neurons^[2].
CGP 36742 (1 μM) prevents kynurenate from antagonizing N-methyl-d-aspartate (NMDA) (HY-17551)-induced release of noradrenaline from rat brain slices potently^[4].
CGP 36742 (1 μM) increases the somatostatin-like immunoreactivity (SRIF-LI) release from hippocampal slices exposed to NMDA^[4].
In Vivo:CGP 36742 (10-30 mg/kg; i.p.; 30 min before test) exhibits antidepressant-like activity in the forced swim test in mice^[1].
CGP 36742 (10 mg/kg; i.p.; once daily for 14 d) are effective in an olfactory bulbectomy (OB) model of depression in rats^[1].
CGP 36742 (30-200 mg/kg; p.o.; administered in a cumulative manner at intervals of 2.5-3 h) blocks the neuronal depression induced by iontophoretically applied baclofen in anaesthetized rats^[2].
CGP 36742 (1-10 mg/kg; i.v.; 25-30 min before test) dose dependently attenuates paired-pulse inhibition measured at latencies of > 100 ms^[2].
CGP 36742 (50-1000 mg/kg; i.v. or p.o.; once or twice) can penetrate the blood-brain barrier in male Sprague-Dawley rats ^[3].