CTEP

Chemical compound

Pharmaceutical compound

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 ^checkY
PubChem CID	11646823
IUPHAR/BPS	6409
ChemSpider	9821562
UNII	E3BWG5775S
CompTox Dashboard (EPA)	DTXSID50469986 Edit this at Wikidata
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

[edit ]

^ 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

mGluR₁ Tooltip Metabotropic glutamate receptor 1	Agonists: ACPD DHPG Glutamate Ibotenic acid Quisqualic acid Ro01-6128 Ro67-4853 Ro67-7476 VU-71 Theanine Antagonists: BAY 36-7620 CPCCOEt Cyclothiazide LY-367,385 LY-456,236 MCPG NPS-2390
mGluR₅ Tooltip Metabotropic glutamate receptor 5	Agonists: ACPD ADX-47273 CDPPB CHPG DFB DHPG Glutamate Ibotenic acid Quisqualic acid VU-1545; Positive allosteric modulators: LSN2463359 Antagonists: CTEP DMeOB LY-344,545 Mavoglurant MCPG NPS-2390 Remeglurant SIB-1757 SIB-1893; Negative allosteric modulators: AZD9272 Basimglurant Dipraglurant Fenobam GRN-529 MPEP MTEP Raseglurant

Group II

mGluR₂ Tooltip Metabotropic glutamate receptor 2

Agonists: BINA
CBiPES
DCG-IV
Eglumegad
Glutamate
Ibotenic acid
LY-379,268
LY-404,039 (pomaglumetad)
LY-487,379
LY-566,332
MGS-0028
Pomaglumetad methionil (LY-2140023)
Talaglumetad; Positive allosteric modulators: JNJ-40411813 (ADX-71149)

Antagonists: APICA
CECXG
EGLU
HYDIA
LY-307,452
LY-341,495
MCPG
MGS-0039
PCCG-4; Negative allosteric modulators: Decoglurant
RO4491533

mGluR₃ Tooltip Metabotropic glutamate receptor 3

Antagonists: APICA
CECXG
EGLU
HYDIA
LY-307,452
LY-341,495
MCPG
MGS-0039; Negative allosteric modulators: Decoglurant
RO4491533

Group III

mGluR₄ Tooltip Metabotropic glutamate receptor 4	Agonists: Glutamate L-AP4 LSP2-9166 PHCCC VU-001,171 VU-0155,041; Positive allosteric modulators: Foliglurax MPEP Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₆ Tooltip Metabotropic glutamate receptor 6	Agonists: Glutamate L-AP4 Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₇ Tooltip Metabotropic glutamate receptor 7	Agonists: AMN082 Glutamate L-AP4 LSP2-9166 Antagonists: CPPG MAP4 MMPIP MPPG MSOP MTPG UBP-1112 XAP044; Negative allosteric modulators: ADX71743
mGluR₈ Tooltip Metabotropic glutamate receptor 8	Agonists: DCPG Glutamate L-AP4; Positive allosteric modulators: AZ12216052 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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