JNJ-16259685

JNJ-16259685 is an antagonist of metabotropic glutamate receptor 1a (mGluR1a, Ki = 0.34 nM in CHO(dHFr-) cell membranes expressing the rat receptor). It is selective for mGluR1a over mGluR5, -2, -3, -4, and -6, as well as a panel of neurotransmitter receptors, ion channels, and transporters, at 10 µM. JNJ-16259685 inhibits glutamate-induced inositol phosphate accumulation in primary rat cerebellar neurons with an IC50 value of 1.73 nM. It increases drinking in the Vogel punished drinking task, indicating anxiolytic-like activity, when administered at doses of 2.5, 5, or 10 mg/kg.Formal Name: (3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl)(cis-4-methoxycyclohexyl)-methanone. CAS Number: 409345-29-5. Molecular Formula: C20H23NO3. Formula Weight: 325.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Chloroform: slightly soluble, DMSO: slightly soluble. SMILES: CO[C@@H]1CC[C@H](C(C2=CC(C=C(CCCO3)C3=N4)=C4C=C2)=O)CC1. InChi Code: InChI=1S/C20H23NO3/c1-23-17-7-4-13(5-8-17)19(22)14-6-9-18-16(11-14)12-15-3-2-10-24-20(15)21-18/h6,9,11-13,17H,2-5,7-8,10H2,1H3/t13-,17+. InChi Key: QOTAQTRFJWLFCR-XFHMXUHZSA-N.