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CGP 36216 hydrochloride

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Catalog No. T22647Cas No. 123691-29-2

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

CGP 36216 hydrochloride

CGP 36216 hydrochloride

😃Good
Catalog No. T22647Cas No. 123691-29-2
CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors (IC50: 43 μM).
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50 mgInquiry6-8 weeks
100 mgInquiry6-8 weeks
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight151.14
FormulaC5H14NO2P
Cas No.123691-29-2
Relative Density.1.108 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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