词条 | Barusiban |
释义 |
| IUPAC_name = (4S,7S,10S,13S,16R)-N-[(2S)-5-Amino-1-hydroxy-2-pentanyl]-7-(2-amino-2-oxoethyl)-10-[(2R)-2-butanyl]-13-sec-butyl-16-(1H-indol-3-ylmethyl)-N-methyl-6,9,12,15,18-pentaoxo-1-thia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide | image = Barusiban.svg | width = 250 | CAS_number = 285571-64-4 | ATC_prefix = None | ATC_suffix = | PubChem = 9832431 | DrugBank = | ChemSpiderID = 8008159 | chemical_formula = | C=40 | H=63 | N=9 | O=8 | S=1 | molecular_weight = 830.049 g/mol | smiles = CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCSCCC(=O)N[C@@H](C(=O)N1)CC2=CNC3=CC=CC=C32)C(=O)N(C)[C@@H](CCCN)CO)CC(=O)N)[C@H](C)CC | StdInChI = 1S/C40H63N9O8S/c1-6-23(3)34-38(55)46-31(20-32(42)51)36(53)45-29(40(57)49(5)26(22-50)11-10-16-41)14-17-58-18-15-33(52)44-30(19-25-21-43-28-13-9-8-12-27(25)28)37(54)47-35(24(4)7-2)39(56)48-34/h8-9,12-13,21,23-24,26,29-31,34-35,43,50H,6-7,10-11,14-20,22,41H2,1-5H3,(H2,42,51)(H,44,52)(H,45,53)(H,46,55)(H,47,54)(H,48,56)/t23-,24+,26+,29+,30-,31+,34+,35+/m1/s1 | StdInChIKey = UGNGRKKDUVKQDF-IHOMMZCZSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = }}Barusiban (INN) (code name FE-200440) is a non-peptide drug which is among the most potent and selective oxytocin receptor antagonists known.[1][2] It was trialed by Ferring Pharmaceuticals as a treatment of preterm labor but failed to demonstrate effectiveness and was not pursued any further.[1][3] See also
References1. ^1 {{cite book|author1=Rainer Landgraf|author2=Inga D. Neumann|title=Advances in Vasopressin and Oxytocin - From Genes to Behaviour to Disease|url=https://books.google.com/books?id=sDRBK1y7ObEC&pg=PA489|date=10 September 2008|publisher=Elsevier|isbn=978-0-08-093247-7|pages=194,489}} {{Oxytocin and vasopressin receptor modulators}}2. ^{{cite book|author1=Stefan Offermanns|author2=Walter Rosenthal|title=Encyclopedia of Molecular Pharmacology|url=https://books.google.com/books?id=iwwo5gx8aX8C&pg=PA1278|date=14 August 2008|publisher=Springer Science & Business Media|isbn=978-3-540-38916-3|pages=1278–}} 3. ^{{cite book|author1=Richard Ouellette|author2=Joseph Joyce|title=Pharmacology for Nurse Anesthesiology|url=https://books.google.com/books?id=7E1QfJSuppwC&pg=PA450|date=25 October 2010|publisher=Jones & Bartlett Publishers|isbn=978-0-7637-8607-6|pages=450–}} 6 : Abandoned drugs|Amines|Carboxamides|Indoles|Oxytocin receptor antagonists|Tocolytics |
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