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CDPPB

MCE China：CDPPB

Brand：MedChemExpress (MCE)

Cat. No.HY-14569

CAS：781652-57-1

Purity：99.32%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease.

In Vitro：CDPPB (above 1 μM) exhibits agonist-like activity on CHO cells expressing mGluR5[1]. CDPPB (0.1 mM, 30 min) inhibits SO2-induced protein radical formation and mitochondrial dysfunction through activation of Akt in mouse hippocampal HT22 cells[2]. CDPPB (0.02-0.2 mM, 2 h before traumatic neuronal injury) suppresses the increase of LDH release and caspase-3 activation induced by traumatic neuronal injury in a dose-dependent manner[3].

In Vivo：CDPPB (1-30 mg/kg, s.c., 20 min prior to Amphetamine injection (locomotor test) or 20 min after Amphetamine injection (PPI test)) suppresses Amphetamine-induced locomotor activity without affecting spontaneous locomotor activity and reverses Amphetamine-induced deficits in PPI in rats[1]. CDPPB (10 mg/kg/day, i.p., 14 days) improves Phencyclidine-induced cognitive deficits in mice[4]. CDPPB (5 mg/kg, i.p., 14 days) improves cognitive impairment and partially reverses the lesion-induced changes in eNOS and nNOS expressions in olfactory bulbectomized rats[5]. CDPPB (1.5 mg/kg, s.c., 18 weeks) ameliorates pathology and phenotypic signs of Huntington's disease mice[6]. CDPPB (20 mg/kg, p.o., single) attenuates depressive-like behavior induced by repeated social defeat stress in mice[7]. CDPPB (10 mg/kg, i.p., adolescence) reverses MK-801 (HY-15084B)-induced locomotor hyperactivity and anhedonia in mice[8]. CDPPB (1-5 mg/kg, i.p., 8 days) improves neuronal survival and prevents memory deficits in C57BL/6 mice injected intrahippocampally with Aβ. [9].

IC50 & Target：mGluR5 27 nM (EC50)

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References：

[1]. Kinney GG, et, al. A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models. J Pharmacol Exp Ther. 2005 Apr; 313(1):199-206.  [Content Brief]

[2]. Guan DF, et al. The mGluR5 positive allosteric modulator CDPPB inhibits SO₂-induced protein radical formation and mitochondrial dysfunction through activation of Akt in mouse hippocampal HT22 cells. Cell Mol Neurobiol. 2015 May;35(4):573-83.  [Content Brief]

[3]. Chen T, et al. Protective effects of mGluR5 positive modulators against traumatic neuronal injury through PKC-dependent activation of MEK/ERK pathway. Neurochem Res. 2012 May;37(5):983-90.  [Content Brief]

[4]. Horio M, et al. Therapeutic effects of metabotropic glutamate receptor 5 positive allosteric modulator CDPPB on phencyclidine-induced cognitive deficits in mice. Fundam Clin Pharmacol. 2013 Oct;27(5):483-8.

[5]. Płoska A, et al. Neurochemical changes underlying cognitive impairment in olfactory bulbectomized rats and the impact of the mGlu5-positive allosteric modulator CDPPB. Brain Res. 2021 Oct 1;1768:147577.  [Content Brief]

[6]. Doria JG, et al. The mGluR5 positive allosteric modulator, CDPPB, ameliorates pathology and phenotypic signs of a mouse model of Huntington's disease. Neurobiol Dis. 2015 Jan;73:163-73.  [Content Brief]

[7]. Zhang L, et al. Post-stress Social Interaction and 3-Cyano-N-(1,3-Diphenyl-1H-Pyrazol-5-yl) Benzamide Treatment Attenuate Depressive-like Behavior Induced by Repeated Social Defeat Stress. Neuroscience. 2024 Feb 6;538:11-21.  [Content Brief]

[8]. Miller-Rhodes P, et al. Sex-specific behavioral impairments produced by neonatal exposure to MK-801 are partially reversed by adolescent CDPPB treatment. Neurotoxicology and Teratology, 2022, 89: 107053.

[9]. Bellozi PMQ, et al. A positive allosteric modulator of mGluR5 promotes neuroprotective effects in mouse models of Alzheimer's disease. Neuropharmacology. 2019 Dec 1;160:107785.  [Content Brief]