| 词条 | Apararenone |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide | image = Apararenone.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 945966-46-1 | CAS_supplemental = | class = Antimineralocorticoid | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 24744336 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 28663572 | UNII = 832663U2NB | KEGG = | ChEBI = | ChEMBL = 2181929 | C=17 | H=17 | F=1 | N=2 | O=4 | S=1 | molecular_weight = 364.391 g/mol | SMILES = CC1(C(=O)N(C2=C(O1)C=C(C=C2)NS(=O)(=O)C)C3=CC=C(C=C3)F)C | StdInChI_Ref = | StdInChI = 1S/C17H17FN2O4S/c1-17(2)16(21)20(13-7-4-11(18)5-8-13)14-9-6-12(10-15(14)24-17)19-25(3,22)23/h4-10,19H,1-3H3 | StdInChIKey_Ref = | StdInChIKey = AZNHWXAFPBYFGH-UHFFFAOYSA-N | synonyms = MT-3995 }}Apararenone (INN) (developmental code name MT-3995) is a nonsteroidal antimineralocorticoid which is under development by Mitsubishi Tanabe Pharma for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.[1][2][3] It was also previously being developed for the treatment of hypertension, but development was discontinued for this indication.[1] Apararenone acts as a highly selective antagonist of the mineralocorticoid receptor (Ki < 50 nM), the receptor for aldosterone.[1][2][3] As of 2017, it is in phase II clinical trials.[1] See also
References1. ^1 2 3 http://adisinsight.springer.com/drugs/800032686 2. ^1 {{cite journal | vauthors = Yang J, Young MJ | title = Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences | journal = Curr Opin Pharmacol | volume = 27 | issue = | pages = 78–85 | year = 2016 | pmid = 26939027 | doi = 10.1016/j.coph.2016.02.005 | url = }} 3. ^1 {{cite journal | vauthors = Kolkhof P, Nowack C, Eitner F | title = Nonsteroidal antagonists of the mineralocorticoid receptor | journal = Curr. Opin. Nephrol. Hypertens. | volume = 24 | issue = 5 | pages = 417–24 | year = 2015 | pmid = 26083526 | doi = 10.1097/MNH.0000000000000147 | url = }} External links
6 : Antimineralocorticoids|Benzoxazines|Experimental drugs|Fluoroarenes|Ketones|Sulfonamides |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。