VU 29 (N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide) | 890764-36-0

name

vu 29

chemical name

n-(1,3-diphenyl-1h-pyrazolo-5-yl)-4-nitrobenzamide

activity

potent allosteric potentiator at the rat mglu5 receptor (ec50 = 9 nm); binds to the mpep (cat. no. 1212) allosteric site (ki app = 244 nm). selective for mglu5 over mglu1 and mglu2 receptors (ec50 values are 557 nm and 1.51 μm for mglu1 and mglu2 respectively). potentiates both dhpg-induced ltp and threshold θ-burst stimulation (tbs)-induced ltp in rat hippocampal slices. analog of cdppb (cat. no. 3235).

MW

384.39

Formula:

c22h16n4o3

Solubility:

soluble to 100 mm in dmso

Purity:

>99 %

Storage:

store at rt

CAS No:

890764-36-0

de Paulis et al (2006) Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. J.Med.Chem. 49 3332. PMID: 16722652.

Chen et al (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol.Pharmacol. 71 1389. PMID: 17303702.

Ayala et al (2009) mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology 34 2057. PMID: 19295507.