| 词条 | Axelopran |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 3-[(1R,5S)-8-[2-[cyclohexylmethyl-[(2S)-2,3-dihydroxypropanoyl]amino]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]benzamide | image = Axelopran_structure.png | width = 240 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 949904-48-7 | CAS_supplemental = {{CAS|949904-50-1}} (sulfate) | ATC_prefix = none | ATC_suffix = | PubChem = 67156338 | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 31444004 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D10740 | C=26 | H=39 | N=3 | O=4 | molecular_weight = 457.60556 g/mol | smiles = C1CCC(CC1)CN(CCN2C3CCC2CC(C3)C4=CC=CC(=C4)C(=O)N)C(=O)C(CO)O | StdInChI =1S/C26H39N3O4/c27-25(32)20-8-4-7-19(13-20)21-14-22-9-10-23(15-21)29(22)12-11-28(26(33)24(31)17-30)16-18-5-2-1-3-6-18/h4,7-8,13,18,21-24,30-31H,1-3,5-6,9-12,14-17H2,(H2,27,32)/t21-,22+,23-,24-/m0/s1 | StdInChIKey = ATLYLVPZNWDJBW-KIHHCIJBSA-N | synonyms = }}Axelopran (INN, USAN) (developmental code name TD-1211) is a drug which is under development by Theravance Biopharma for the treatment of opioid-induced constipation. It acts as a potent, selective, and peripherally-restricted μ-, κ-, and δ-opioid receptor antagonist, with similar affinity for the μ- and κ-opioid receptors and about an order of magnitude lower affinity for the δ-opioid receptor. Axelopran has potent μ-opioid receptor antagonist activity on the gastrointestinal tract in vivo, and thus it produces a dose-dependent inhibition of opioid-induced delaying in gastric emptying in mice and rats following subcutaneous or oral administration.[1] See also
References1. ^ , Axelopran (td-1211) briefing document anesthetic and analgesic drug products advisory committee June 11 and 12, 2014. {{Laxatives}}{{Opioidergics}}{{gastrointestinal-drug-stub}} 4 : Drugs acting on the gastrointestinal system and metabolism|Kappa antagonists|Laxatives|Opioid antagonists |
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