Chemical Name: 3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
Biological ActivityVU 6005649 is a positive allosteric modulator of mGlu7 and mGlu8 receptors (EC50 = 0.65 μM and 2.6 μM for mGlu7 and mGlu8, respectively). Displays >3.8 fold selectivity for mGlu7 and mGlu8 over other mGlu receptors (EC50 >10 μM for mGlu1,2,3,4,5,6). Also NK1 receptor antagonist (Ki= 650 nM, IC50 = 3.4 μM). Brain penetrant.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines.
Abe et al.
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