CTEP

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
IUPAC name
  • 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H13ClF3N3O
Molar mass391.78 g·mol−1
3D model (JSmol)
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

References
  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.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.