CGP52432
CAS No. : 139667-74-6

CGP52432
Cat. No. : CS-0028031
M. Wt. : 384.24
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  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: CGP52432; 
Cat. No. : CS-0028031
CAS No. : 139667-74-6
Formula: C15H24Cl2NO4P
M. Wt. : 384.24
Solubility: DMSO: 5 mg/mL (Need ultrasonic and warming)

Activity:

CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM. IC50 & Target: IC50: 85 nM (GABAB receptor)[1] In Vitro: 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]. In Vivo: 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].

Protocol:

Animal Administration: CGP52432 is formulated in PBS[2].[2]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:

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.

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.

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.

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