CTEP

CTEP
Identifiers
	IUPAC name 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine;
CAS Number	871362-31-1 ;
PubChem CID	11646823;
IUPHAR/BPS	6409;
ChemSpider	9821562;
UNII	E3BWG5775S;
CompTox Dashboard (EPA)	DTXSID50469986 ;
Chemical and physical data
Formula	C19H13ClF3N3O
Molar mass	391.78 g·mol−1
3D model (JSmol)	Interactive image; Interactive image;
	SMILES Clc2cc(ccn2)C#Cc1nc(C)n(c1C)-c(cc3)ccc3OC(F)(F)F; ; FC(F)(F)Oc3ccc(n2c(c(C#Cc1ccnc(Cl)c1)nc2C)C)cc3;
	InChI 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; Key:GOHCTCOGYKAJLZ-UHFFFAOYSA-N;

CTEP (Ro4956371) 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

^ 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 (November 2011). "CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor". The Journal of Pharmacology and Experimental Therapeutics. 339 (2): 474–86. doi:10.1124/jpet.111.185660. PMID 21849627. S2CID 2554923.

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[pmid21849627-1] 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 (November 2011). "CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor". The Journal of Pharmacology and Experimental Therapeutics. 339 (2): 474–86. doi:10.1124/jpet.111.185660. PMID 21849627. S2CID 2554923.

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