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CGP 52432 Sale

(Synonyms: 4-苄氧基苯基异硫氰酸酯) 目录号 : GC16947

A GABAB receptor antagonist

CGP 52432 Chemical Structure

Cas No.:139667-74-6

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10mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Mice[2]Two separate cohorts of male pups are used for the study. One cohort is treated with either R(+)baclofen HCl (2 mg/kg) or with vehicle (PBS). The second cohort is treated with the GABAB receptor antagonist CGP52342 (10, 30 mg/kg) or vehicle (PBS). Drugs are freshly prepared for injection each day, by dissolution in PBS with vortexing and brief sonication. Doses of R(+)baclofen and CGP52432 are chosen to be well tolerated in adult mice. All drug treatments are given via subcutaneous injection, once daily from P14-28 in a volume of 0.05 mL[2].

References:

[1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5.
[2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10.
[3]. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86.

产品描述

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM, 35- and 100-fold lower than at the receptors regulating somatostatin and glutamate overflow, respectively[1].

CGP52432 (10, 30 mg/kg) shows no effect on the total arm entries and total head dips of mice on the elevated-plus maze[2]. CGP52432 (100 nmol/kg, i.v., or 1 nmol/kg, i.c.v.) abolishes the suppressive effects of GABA ( 50 μmol/kg, i.v.) on enhanced renal sympathetic nerve activity (RSNA) during ischaemia, causeing elimination of the renoprotective effects of GABA in rats[3].

References:
[1]. Lanza M, et al. CGP 52432: a novel potent and selective GABAB autoreceptor antagonist in rat cerebral cortex. Eur J Pharmacol. 1993 Jun 24;237(2-3):191-5.
[2]. Sweeney FF, et al. Activation but not blockade of GABAB receptors during early-life alters anxiety in adulthood in BALB/c mice. Neuropharmacology. 2014 Jun;81:303-10.
[3]. Kobuchi S, et al. Mechanisms underlying the renoprotective effect of GABA against ischaemia/reperfusion-induced renal injury in rats. Clin Exp Pharmacol Physiol. 2015 Mar;42(3):278-86.

Chemical Properties

Cas No. 139667-74-6 SDF
别名 4-苄氧基苯基异硫氰酸酯
化学名 (S)-(3-((3,4-dichlorobenzyl)amino)propyl)(diethoxymethyl)phosphinic acid
Canonical SMILES ClC1=CC(CNCCC[P@](O)(C(OCC)OCC)=O)=CC=C1Cl
分子式 C15H24Cl2NO4P 分子量 384.24
溶解度 <3.84mg/ml in Water 储存条件 Store at -20°C
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1 mM 2.6025 mL 13.0127 mL 26.0254 mL
5 mM 0.5205 mL 2.6025 mL 5.2051 mL
10 mM 0.2603 mL 1.3013 mL 2.6025 mL
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