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139667-74-6

139667-74-6 structure
139667-74-6 structure

Name 3-[(3,4-dichlorophenyl)methylamino]propyl-(diethoxymethyl)phosphinic acid
Synonyms Tocris-1246
MFCD00041095
[3-[[(3,4-Dichlorophenyl)methyl]amino]propyl](diethoxymethyl)-phosphinic acid
CGP52432
Description CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
Related Catalog
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.

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℃
RIDADR NONH for all modes of transport
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