CTEP

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CTEP
CTEP.svg
Systematic (IUPAC) name
2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
Identifiers
PubChem CID 11646823
IUPHAR/BPS 6409
ChemSpider 9821562
Chemical data
Formula C19H13ClF3N3O
Molar mass 391.774 g/mol

CTEP is a research drug developed by Hoffmann-La Roche that acts as a selective allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5, binding with nanomolar affinity and over 1000 times selectivity over all other receptor targets tested. In animal studies it was found to have a high oral bioavailability and a long duration of action, lasting 18 hours after a single dose, giving it considerably improved properties over older mGluR5 antagonists such as MPEP and fenobam.[1]

References[edit]

  1. ^ Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. Journal of Pharmacology and Experimental Therapeutics. 2011 Nov;339(2):474-86. PMID 21849627