词条 | Pavinetant |
释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 3-(methanesulfonamido)-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide | image = MLE-4901.svg | width = 225px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = By mouth | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 941690-55-7 | CAS_supplemental = | class = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 23649245 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 28189763 | UNII = 3U471ZVC5K | KEGG = D11345 | ChEBI = 140478 | ChEMBL = 3545233 | synonyms = MLE-4901; AZD-4901; AZD-2624; AZ-12472520 | C=26 | H=25 | N=3 | O=3 | S=1 | molecular_weight = 459.564 g/mol | SMILES = CC[C@@H](C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)NS(=O)(=O)C | StdInChI_Ref = | StdInChI = 1S/C26H25N3O3S/c1-3-21(18-12-6-4-7-13-18)28-26(30)23-20-16-10-11-17-22(20)27-24(19-14-8-5-9-15-19)25(23)29-33(2,31)32/h4-17,21,29H,3H2,1-2H3,(H,28,30)/t21-/m0/s1 | StdInChIKey_Ref = | StdInChIKey = QYTBBBAHNIWFOD-NRFANRHFSA-N }}Pavinetant ({{abbrlink|INN|International Nonproprietary Name}}, {{abbrlink|USAN|United States Adopted Name}}; developmental code names MLE-4901, AZD-4901, AZ-12472520, AZD-2624), is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which was under development by AstraZeneca and Millendo Therapeutics for the treatment of hot flashes and polycystic ovary syndrome (PCOS).[1][2][3] It was also under investigation for the treatment of schizophrenia,[2] but development was discontinued for this indication due to lack of effectiveness.[1][4] In November 2017, development of the medication for hot flashes and PCOS was also terminated after its developer assessed the clinical risks and benefits.[1][3] See also
References1. ^1 2 http://adisinsight.springer.com/drugs/800038259 2. ^1 {{cite journal | vauthors = Malherbe P, Ballard TM, Ratni H | title = Tachykinin neurokinin 3 receptor antagonists: a patent review (2005 - 2010) | journal = Expert Opin Ther Pat | volume = 21 | issue = 5 | pages = 637–55 | year = 2011 | pmid = 21417773 | doi = 10.1517/13543776.2011.568482 | url = }} 3. ^1 {{cite journal | vauthors = Sassarini J, Anderson RA | title = New pathways in the treatment for menopausal hot flushes | journal = Lancet | volume = | issue = | pages = | year = 2017 | pmid = 28385351 | doi = 10.1016/S0140-6736(17)30886-3 | url = }} 4. ^{{cite journal | vauthors = Litman RE, Smith MA, Desai DG, Simpson T, Sweitzer D, Kanes SJ | title = The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study | journal = J Clin Psychopharmacol | volume = 34 | issue = 2 | pages = 199–204 | year = 2014 | pmid = 24525659 | doi = 10.1097/JCP.0000000000000071 | url = }} External links
5 : Abandoned drugs|Carboxamides|NK3 receptor antagonists|Quinolines|Sulfonamides |
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