JNJ-16259685 (JNJ16259685) is a highly potent, selective, non-competitive and centrally active mGluR1 antagonist with Ki of 0.34 nM.
JNJ-16259685 shows no agonist, antagonist or PAM activity toward rat mGlu2/3/4/6 receptors (IC50>10 uM) and does not bind to AMPA, NMDA receptor and other neurotransmitter receptors.
JNJ-16259685 inhibits glutamate-induced Ca2+ mobilization for rat and human mGluR1 with IC50 of 3.24 and 1.21 nM, inhibits glutamate-mediated inositol phosphate production with IC50 of 1.73 nM.
JNJ-16259685 attenuates drug context-induced reinstatement of cocaine seeking in rats.
