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VU 29Cat. No. 4458 |
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Chemical Name: N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide |
Biological 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).Certificate of Analysis / Safety Data Sheet
References
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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