VU-29| CAS 890764-36-0|DC Chemicals

Cas No.:	890764-36-0
Chemical Name:	N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
Synonyms:	ABT 724 trihydrochloride;VU 29;N-(1,3-Diphenyl-1H-pyrazol-5-yl)-4-nitrobenzamide;DNC013021;MolPort-020-313-399;CHEBI:448834;CHEMBL411221;SureCN1821818;AGN-PC-00CMDB;DPAP;VU-29;N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
SMILES:	C1(N2C(NC(=O)C3C=CC([N+]([O-])=O)=CC=3)=CC(C3C=CC=CC=3)=N2)C=CC=CC=1
Formula:	C₂₂H₁₆N₄O₃
M.Wt:	384.387444496155
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	VU-29 (DPAP)is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM)[1][2].
Target:	is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM)[1][2].
In Vivo:	VU-29 (500 nM) potentiates DHPG induced increases in phosphoinositide (PI) hydrolysis in rat hippocampal slices. VU-29 potentiates threshold TBS-induced long term potentiation (LTP) in rat hippocampal CA1 region. VU-29 (1 µM) potentiates chemically induced mGluR-long term depression (LTD) in area CA1 of the rat hippocampus. VU-29 (1 µM) potentiates stimulus-induced NMDA receptor-independent LTD[1].
References:	[1]. Ayala JE, et al. mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning. Neuropsychopharmacology. 2009;34(9):2057-2071. [2]. Chen Y, et al. 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. 2007;71(5):1389-1398.

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