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CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors (IC50: 43 μM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | Inquiry | 6-8 weeks | 6-8 weeks | |
| 50 mg | Inquiry | 6-8 weeks | 6-8 weeks | |
| 100 mg | Inquiry | 6-8 weeks | 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 |
| Smiles | P(CCCN)(CC)(=O)O |
| 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/Shipping at ambient temperature. |
| Solubility Information | H2O: <18.76 mg/mL, Sonication is recommended. DMSO: <18.76 mg/mL, Sonication is recommended. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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