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mGluR2 antagonist 1

Names

[ CAS No. ]:
1432728-49-8

[ Name ]:
mGluR2 antagonist 1

Biological Activity

[Description]:

mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> mGluR
Research Areas >> Neurological Disease

[Target]

mGluR2:9 nM (IC50)


[In Vivo]

In vivo, mGluR2 antagonist 1 (Compound 25) reverses the effect of mGluR2 agonist LY379268 in amphetamine-induced hyperlocomotion and shows good efficacy in the mouse delayed non-match to position assay at 10 mg/kg.

[References]

[1]. Youheng Shu,et al. Discovery of 4-arylquinoline-2-carboxamides, Highly Potent and Selective Class of mGluR2 Negative Allosteric Modulators: From HTS to Activity in Animal Models. Bioorg Med Chem Lett. 2020 May 1;30(9):127066.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H16FN3O3

[ Molecular Weight ]:
377.37

Related Compounds