VU6033685

VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 -induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%[1].

C20H19ClN4O

366.84

CC1=NC(C2CC2)=CC=C1CNC(C3=CC(N4C=CC=N4)=CC=C3Cl)=O

MGluR

Room temperature