CTEP

CTEP is an inverse agonist of metabotropic glutamate receptor 5 (mGluR5, K_is = 16.4, 12.6, and 9.5 nM for the human, rat, and mouse receptors, respectively, in a radioligand binding assay).¹ It is selective for mGluR5 over mGluR1, -2, -3, -4, -6, -7, and -8 (IC₅₀s = >10 µM for all) and the histamine H₁ and α₅β₃γ₂ subunit-containing GABA_A receptors (K_is = >4 and >3.2 µM, respectively), but does inhibit adenosine A₁, A₃, muscarinic, and kainate receptors (K_is = 6.2, 2.3, 5.3, and 7.9 µM, respectively), as well as L-type calcium and sodium channels (K_is = 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.

WARNING This product is not for human or veterinary use.

1. Lindemann, L., Jaeschke, G., Michalon, A., et al. CTEP: A novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J. Pharmacol. Exp. Ther. 339(2), 474-486 (2011).