CTEP

CTEP is an inverse agonist of metabotropic glutamate receptor 5 (mGluR5, Kis = 16.4, 12.6, and 9.5 nM for the human, rat, and mouse receptors, respectively, in a radioligand binding assay). It is selective for mGluR5 over mGluR1, -2, -3, -4, -6, -7, and -8 (IC50s = >10 µM for all) and the histamine H1 and alpha5beta3gamma2 subunit-containing GABAA receptors (Kis = >4 and >3.2 µM, respectively), but does inhibit adenosine A1, A3, muscarinic, and kainate receptors (Kis = 6.2, 2.3, 5.3, and 7.9 µM, respectively), as well as L-type calcium and sodium channels (Kis = 2.7 and 5 µM, respectively) in a panel of 103 receptors, enzymes, and ion channels at 10 µM. CTEP inhibits inositol phosphate accumulation and quisqualate-induced calcium mobilization in HEK293 cells expressing human recombinant mGluR5 (IC50s = 6.4 and 11.4 nM, respectively). It reduces stress-induced hyperthermia in mice and increases drinking in the Vogel conflict test in rats, indicating anxiolytic-like activity, when administered at a dose of 0.3 mg/kg.Formal Name: 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]-pyridine. CAS Number: 871362-31-1. Molecular Formula: C19H13ClF3N3O. Formula Weight: 391.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 25 mg/ml. lambdamax: 240, 330 nm. SMILES: FC(F)(F)OC1=CC=C(N2C(C)=C(C#CC3=CC(Cl)=NC=C3)N=C2C)C=C1. InChi Code: InChI=1S/C19H13ClF3N3O/c1-12-17(8-3-14-9-10-24-18(20)11-14)25-13(2)26(12)15-4-6-16(7-5-15)27-19(21,22)23/h4-7,9-11H,1-2H3. InChi Key: GOHCTCOGYKAJLZ-UHFFFAOYSA-N.