CGP 52432

Names

[ Name ]:
CGP 52432

[Synonym ]:
Tocris-1246
MFCD00041095
[3-[[(3,4-Dichlorophenyl)methyl]amino]propyl](diethoxymethyl)-phosphinic acid
CGP52432

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

Research Areas >> Neurological Disease

[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].

[Animal admin]

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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.258g/cm3

[ Boiling Point ]:
544.4ºC at 760mmHg

[ Molecular Formula ]:
C₁₅H₂₄Cl₂NO₄P

[ Molecular Weight ]:
384.23500

[ Flash Point ]:
283.1ºC

[ Exact Mass ]:
383.08200

[ PSA ]:
77.60000

[ LogP ]:
4.49100

[ Vapour Pressure ]:
1.1E-12mmHg at 25°C

[ Index of Refraction ]:
1.524

[ Storage condition ]:
2-8℃

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Correlated changes in NMDA receptor phosphorylation, functional activity, and sedation by chronic ethanol consumption.

J. Neurochem. 115(5) , 1112-22, (2010)

Alcohol abuse leads to tolerance, dependence, and memory impairments that involve excitatory glutamatergic NMDA synaptic transmission. The NMDA receptor (NMDAR) is known to undergo activity-dependent ...

Presynaptic mGlu7 receptors control GABA release in mouse hippocampus.

Neuropharmacology 66 , 215-24, (2013)

The functional role of presynaptic release-regulating metabotropic glutamate type 7 (mGlu7) receptors in hippocampal GABAergic terminals was investigated. Mouse hippocampal synaptosomes were preloaded...

Hippocampal Pyramidal Neurons Comprise Two Distinct Cell Types that Are Countermodulated by Metabotropic Receptors

Neuron 76(4) , 776-89, (2012)

Relating the function of neuronal cell types to information processing and behavior is a central goal of neuroscience. In the hippocampus, pyramidal cells in CA1 and the subiculum process sensory and ...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.