| 词条 | Befetupitant |
| 释义 |
| 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.png | width = 220 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | bioavailability = | protein_bound = | metabolism = | excretion = | IUPHAR_ligand = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 290296-68-3 | CAS_supplemental = | ATC_prefix = none | ATC_suffix = | PubChem = 6450815 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|changed|FDA}} | UNII = | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = | ChemSpiderID = 4953365 | C=29 | H=29 | F=6 | N=3 | O=2 | molecular_weight = 565.550 g/mol | 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 }}Befetupitant (Ro67-5930) is a drug developed by Hoffmann-La Roche which acts as a potent and selective antagonist for the NK1 receptor.[1] 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.[2] References1. ^Hoffmann T, Bös M, Stadler H, Schnider P, Hunkeler W, Godel T, Galley G, Ballard TM, Higgins GA, Poli SM, Sleight AJ. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. {{PMID|16332435}} {{Neurokinin receptor modulators}}{{nervous-system-drug-stub}}2. ^Bignami F, Giacomini C, Lorusso A, Aramini A, Rama P, Ferrari G. NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest Ophthalmol Vis Sci. 2014 Sep 16;55(10):6783-94. doi: 10.1167/iovs.14-14553. {{PMID|25228541}} 2 : NK1 receptor antagonists|Trifluoromethyl compounds |
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