CAS 139667-74-6|CGP 52432
| Common Name | CGP 52432 | ||
|---|---|---|---|
| CAS Number | 139667-74-6 | Molecular Weight | 384.23500 |
| Density | 1.258g/cm3 | Boiling Point | 544.4ºC at 760mmHg |
| Molecular Formula | C15H24Cl2NO4P | Melting Point | / |
| MSDS | USA | Flash Point | 283.1ºC |
Names
| Name | 3-[(3,4-dichlorophenyl)methylamino]propyl-(diethoxymethyl)phosphinic acid |
|---|---|
| Synonym | More Synonyms |
CGP 52432 BiologicalActivity
| Description | CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM. |
|---|---|
| Related Catalog | Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch 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. |
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 |
| InChIKey | GJZVQXWEIYRHBE-UHFFFAOYSA-N |
| SMILES | CCOC(OCC)P(=O)(O)CCCNCc1ccc(Cl)c(Cl)c1 |
| Storage condition | 2-8℃ |
Safety Information
| RIDADR | NONH for all modes of transport |
|---|
Articles23
More 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 ... |
Synonyms
| Tocris-1246 |
| MFCD00041095 |
| [3-[[(3,4-Dichlorophenyl)methyl]amino]propyl](diethoxymethyl)-phosphinic acid |
| CGP52432 |
