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CGP 35348
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CAS NO:123690-79-9
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
CGP 35348 是一种选择性、脑渗透性、中枢活性 GABAB 受体拮抗剂，EC50 为 34 μM。
Cas No.123690-79-9
别名(3-氨丙基)(二乙氧基甲基)膦酸水合物
化学名(S)-(3-aminopropyl)(diethoxymethyl)phosphinic acid
Canonical SMILESO[P@@](CCCN)(C(OCC)OCC)=O
分子式C8H20NO4P
分子量225.22
溶解度DMSO: 0.1 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CGP 35348 is a selective antagonist of γ-aminobutyric acidB (GABAB) receptor with IC50 value of 34 μM [1].

The GABAB receptor is a metabotropic transmembrane receptors for GABA that is linked via G-protein to potassium channel. It stimulates the opening of K+ channel and hyperpolarize the neuron.

CGP 35348 is a selective GABAB receptor antagonist that can penetrate the blood-brain barrier. In rat cortex slices, CGP 35348 inhibited the potentiating effect of L-baclofen on adenylate cyclase stimulated by noradrenaline. In the hippocampal slice, CGP 35348 (10, 30, 100 μM) inhibited membrane hyperpolarization induced by L-baclofen (10 μM) and the inhibitory postsynaptic potential [1].

In the spinal cord of the rat, CGP 35348 (3-30 μg) inhibited L-baclofen-induced antinociception in a dose-dependent way [2]. In the rat, CGP 35348 induced pain-like response to mechanical stimulation in a dose-dependent way and reduced the paw withdrawal threshold to pressure [3]. In rats, CGP 35348(500 mg/kg) significantly reduced food consumption by the blockade of central GABAB receptors [4].

References:
[1].  Olpe HR, Karlsson G, Pozza MF, et al. CGP 35348: a centrally active blocker of GABAB receptors. Eur J Pharmacol, 1990, 187(1): 27-38.
[2].  Hammond DL, Washington JD. Antagonism of L-baclofen-induced antinociception by CGP 35348 in the spinal cord of the rat. Eur J Pharmacol, 1993, 234(2-3): 255-262.
[3].  Hao JX, Xu XJ, Wiesenfeld-Hallin Z. Intrathecal gamma-aminobutyric acidB (GABAB) receptor antagonist CGP 35348 induces hypersensitivity to mechanical stimuli in the rat. Neurosci Lett, 1994, 182(2): 299-302.
[4].  Patel SM, Ebenezer IS. The effects of intraperitoneal and intracerebroventricular administration of the GABAB receptor antagonist CGP 35348 on food intake in rats. Eur J Pharmacol, 2004, 503(1-3): 89-93.