CTEP

Chemical compound
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
  • 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

  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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Metabotropic glutamate receptor modulators
Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR6Tooltip Metabotropic glutamate receptor 6
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR7Tooltip Metabotropic glutamate receptor 7
  • Antagonists: CPPG
  • MAP4
  • MMPIP
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
  • XAP044; Negative allosteric modulators: ADX71743
mGluR8Tooltip Metabotropic glutamate receptor 8
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators
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