:CTEP

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine

| image = CTEP.svg

| width = 250

| tradename =

| pregnancy_AU =

| pregnancy_US =

| legal_AU =

| legal_CA =

| legal_UK =

| legal_US =

| index_label =

| index2_label =

| IUPHAR_ligand = 6409

| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 871362-31-1

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = E3BWG5775S

| PubChem = 11646823

| DrugBank =

| ChemSpiderID = 9821562

| smiles2 = FC(F)(F)Oc3ccc(n2c(c(C#Cc1ccnc(Cl)c1)nc2C)C)cc3

| StdInChI = 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

| StdInChIKey = GOHCTCOGYKAJLZ-UHFFFAOYSA-N

| C=19 | H=13 | Cl=1 | F=3 | N=3 | O=1

| smiles = Clc2cc(ccn2)C#Cc1nc(C)n(c1C)-c(cc3)ccc3OC(F)(F)F

}}

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.{{cite journal | vauthors = 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 | title = CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 339 | issue = 2 | pages = 474–86 | date = November 2011 | pmid = 21849627 | doi = 10.1124/jpet.111.185660 | s2cid = 2554923 }}

References

{{Reflist|2}}

{{Metabotropic glutamate receptor modulators}}

Category:Alkyne derivatives

Category:Imidazoles

Category:MGlu5 receptor antagonists

Category:Pyridines

Category:Trifluoromethyl ethers

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