890764-36-0

890764-36-0 structure

Name: VU 29
Chemical Name: N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
CAS Number: 890764-36-0
Molecular Formula: C₂₂H₁₆N₄O₃
Molecular Weight: 384.38700
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2018-10-19 11:25:12
Modify Date: 2024-01-11 08:55:37
VU-29 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].

Name	N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
Synonyms	ABT 724 trihydrochloride DPAP VU-29

Description	VU-29 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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	rat mGluR5:9 nM (EC50) rat mGluR1:557 nM (EC50) rat mGluR2:1.5 μM (EC50) hmGluR4:154 nM (EC50) rat mGluR5:224 nM (Ki)
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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