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VU 29

Names

[ CAS No. ]:
890764-36-0

[ Name ]:
VU 29

[Synonym ]:
ABT 724 trihydrochloride
DPAP
VU-29

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H16N4O3

[ Molecular Weight ]:
384.38700

[ Exact Mass ]:
384.12200

[ PSA ]:
92.74000

[ LogP ]:
5.29600

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds