befetupitant

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-morpholin-4-ylpyridin-3-yl]propanamide

| image = Befetupitant Structure.svg

| width = 220

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| CAS_number_Ref = {{cascite|correct|??}}

| CAS_number = 290296-68-3

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| PubChem = 6450815

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| UNII_Ref = {{fdacite|changed|FDA}}

| UNII = RSH7NDI7MI

| ChEMBL_Ref = {{ebicite|changed|EBI}}

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| ChemSpiderID = 4953365

| C=29 | H=29 | F=6 | N=3 | O=2

| smiles = CC1=CC=CC=C1C2=CC(=NC=C2N(C)C(=O)C(C)(C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCOCC4

| StdInChI = 1S/C29H29F6N3O2/c1-18-7-5-6-8-22(18)23-16-25(38-9-11-40-12-10-38)36-17-24(23)37(4)26(39)27(2,3)19-13-20(28(30,31)32)15-21(14-19)29(33,34)35/h5-8,13-17H,9-12H2,1-4H3

| StdInChIKey = ZGNPLCMMVKCTHM-UHFFFAOYSA-N

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Befetupitant (Ro67-5930) is a drug developed by Hoffmann-La Roche which acts as a potent and selective antagonist for the NK1 receptor.{{cite journal | vauthors = Hoffmann T, Bös M, Stadler H, Schnider P, Hunkeler W, Godel T, Galley G, Ballard TM, Higgins GA, Poli SM, Sleight AJ | display-authors = 6 | title = Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 16 | issue = 5 | pages = 1362–5 | date = March 2006 | pmid = 16332435 | doi = 10.1016/j.bmcl.2005.11.047 }} It was originally developed as a potential antiemetic drug, though development was ultimately discontinued after a related drug netupitant was deemed to be more suitable for clinical development. Befetupitant has however continued to be researched for other possible applications such as treatment of corneal neovascularization.{{cite journal | vauthors = Bignami F, Giacomini C, Lorusso A, Aramini A, Rama P, Ferrari G | title = NK1 receptor antagonists as a new treatment for corneal neovascularization | journal = Investigative Ophthalmology & Visual Science | volume = 55 | issue = 10 | pages = 6783–94 | date = September 2014 | pmid = 25228541 | doi = 10.1167/iovs.14-14553 | doi-access = }}

References

{{Reflist}}

{{Neurokinin receptor modulators}}

Category:NK1 receptor antagonists

Category:Trifluoromethyl compounds

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