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CTEP

Summary

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]

CTEP
Identifiers
  • 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
CAS Number
  • 871362-31-1 checkY
PubChem CID
  • 11646823
IUPHAR/BPS
  • 6409
ChemSpider
  • 9821562
UNII
  • E3BWG5775S
CompTox Dashboard (EPA)
  • DTXSID50469986 Edit this at Wikidata
Chemical and physical data
FormulaC19H13ClF3N3O
Molar mass391.78 g·mol−1
3D model (JSmol)
  • Interactive image
  • Interactive image
  • 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=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

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 (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.