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VU6005649 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 7 (mGluR7) and mGluR8.1 It enhances calcium mobilization induced by L-AP4 (Item No. 14538) in HEK cells expressing mGluR7 or mGluR8 (EC50s = 0.65 and 2.6 µM, respectively). It is selective for mGluR7 and mGluR8 over mGluR1-6, as well as a panel of 67 GPCRs, ion channels, transports, and nuclear hormone receptors, at 10 µM but does inhibit the neurokinin-1 (NK1) receptor (IC50 = 3.4 µM). In vivo, VU6005649 (50 mg/kg, i.p) increases the length of freezing time induced by contextual fear conditioning in mice.
WARNING This product is not for human or veterinary use.
1. Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-