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CGP36742 was the first orally active GABAB-selective antagonist. The IC50 for blocking GABAergic transmission is 36 μM. Oral administration of CGP36742 in rats blocks baclofen-induced neuronal depression, and reduces learning deficit and passive avoidance in an olfactory bulbectomy depression model.
| Molecular Weight | 179.2 |
| Formula | C7H18NO2P |
| CAS Number | 123690-78-8 |
| Solubility (25°C) | Water: 10 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Roger Bullock. SGS-742 Novartis
[2] Graham A R Johnston, et al. GABA(C) receptors as drug targets
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