VU6005649

VU6005649 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 7 (mGluR7) and mGluR8. It enhances calcium mobilization induced by L-AP4 (Cay-14538) in HEK cells expressing mGluR7 or mGluR8 (EC50s = 0. and 2. 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. µM). In vivo, VU6005649 (50 mg/kg, i.p) increases the length of freezing time induced by contextual fear conditioning in mice.. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml.