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CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors (IC50: 43 μM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | Inquiry | 6-8 weeks | |
50 mg | Inquiry | 6-8 weeks | |
100 mg | Inquiry | 6-8 weeks |
Description | CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors (IC50: 43 µM). |
In vitro | In rat neocortical preparations maintained in Mg2+-free Krebs medium, CGP 36216 acts as antagonism of baclofen-induced suppression of spontaneous discharges in a concentration-dependent manner. However, CGP 36216, up to 1 mM, was ineffective in antagonizing baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid (B) GABAB postsynaptic receptors 1. In electrically stimulated brain slices preloaded with [3H] GABA, CGP 36216 increased the release of [3H] GABA, which was reversed by baclofen. While CGP 36216 is ineffective at GABAB postsynaptic receptors, it is appreciably more active at presynaptic receptors1. |
Molecular Weight | 151.14 |
Formula | C5H14NO2P |
Cas No. | 123691-29-2 |
Relative Density. | 1.108 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O: <18.76 mg/mL DMSO: <18.76 mg/mL |
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