Cat. No. 4458
Chemical Name: N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide
Biological ActivityPotent 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).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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.
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Keywords: VU 29, supplier, VU29, mGlu5, mGluR5, pams, positive, allosteric, potentiators, modulators, glutamate, receptors
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