VU 29

• CAT Number: I010962
• CAS Number: 890764-36-0
• Molecular Formula: C22H16N4O3
• Molecular Weight: 384.395
• Purity: ≥95%
• Synonyms: N-(1,3-Diphenyl-1H-pyrazolo-5-yl)-4-nitrobenzamide
• Target: Neuronal Signaling
• Solubility: Soluble to 100 mM in DMSO
• Storage: Store at RT
• IUPAC Name: N-(2,5-diphenylpyrazol-3-yl)-4-nitrobenzamide
• InChI: InChI=1S/C22H16N4O3/c27-22(17-11-13-19(14-12-17)26(28)29)23-21-15-20(16-7-3-1-4-8-16)24-25(21)18-9-5-2-6-10-18/h1-15H,(H,23,27)
• InChIKey: KIALCSMRIHRFPL-UHFFFAOYSA-N
• SMILES: C1=CC=C(C=C1)C2=NN(C(=C2)NC(=O)C3=CC=C(C=C3)[N+](=O)[O-])C4=CC=CC=C4

VU 29 (CAT: I010962) is a potent allosteric potentiator that acts on the rat mGlu5 receptor. It exhibits a high affinity for the MPEP allosteric site, with an apparent Ki value of 244 nM. It demonstrates selectivity for the mGlu5 receptor over mGlu1 and mGlu2 receptors, with EC50 values of 557 nM and 1.51 μM, respectively. VU 29 has been found to enhance both DHPG-induced long-term potentiation (LTP) and threshold θ-burst stimulation (TBS)-induced LTP in rat hippocampal slices. These findings suggest that VU 29 has potential applications in the modulation of synaptic plasticity, which may have implications for various neurological conditions.

Reference

1.Chen, Yelin, 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." Molecular pharmacology 71.5 (2007): 1389-1398.
2.de Paulis, Tomas, et al. "Substituent effects of N-(1, 3-diphenyl-1 H-pyrazol-5-yl) benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes." Journal of medicinal chemistry 49.11 (2006): 3332-3344.
3.Ayala, Jennifer E., et al. "mGluR5 positive allosteric modulators facilitate both hippocampal LTP and LTD and enhance spatial learning." Neuropsychopharmacology 34.9 (2009): 2057-2071.