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CGP 36216 hydrochloride Sale

目录号 : GC13676

Selective GABAB antagonist

CGP 36216 hydrochloride Chemical Structure

Cas No.:123691-29-2

规格 价格 库存 购买数量
1mg
¥682.00
现货
5mg
¥1,522.00
现货
10mg
¥2,364.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors with IC50 value of 43 µM.

GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) and are linked through G-proteins to potassium channels. Expression of GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system. GABAB receptors play a key role in regulating membrane excitability and synaptic transmission in the brain.

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 antagonising 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, that was reversed by baclofen. While CGP 36216 is ineffective at GABAB postsynaptic receptors, it is appreciably more active at presynaptic receptors1.

Reference:
1.   Ong J, Bexis S, Marino V, et al. CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain. European journal of pharmacology. 2001;415(2-3):191-195.

Chemical Properties

Cas No. 123691-29-2 SDF
化学名 (3-aminopropyl)(ethyl)phosphinic acid hydrochloride
Canonical SMILES CCP(CCCN)(O)=O.Cl
分子式 C5H14NO2P.HCl 分子量 187.6
溶解度 <18.76mg/ml in DMSO; <18.76mg/ml in Water 储存条件 Desiccate at RT
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1 mg 5 mg 10 mg
1 mM 5.3305 mL 26.6525 mL 53.3049 mL
5 mM 1.0661 mL 5.3305 mL 10.661 mL
10 mM 0.533 mL 2.6652 mL 5.3305 mL
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