词条 | Olorinab |
释义 |
| IUPAC_name = (4aS,5aS)-N-((2S)-1-hydroxy-3,3-dimethylbutan-2-yl)-1-(4-oxidopyrazin-2-yl)-4,4a,5,5a-tetrahydro-1H-cyclopropa(4,5)cyclopenta[1,2-c]pyrazole-3-carboxamide | image = Olorinab_structure.png | width = 200 | tradename = | legal_status = | routes_of_administration = Oral | metabolism = | elimination_half-life = | excretion = | CAS_number = 1268881-20-4 | PubChem = 60164925 | ChemSpiderID = | UNII_Ref = | UNII = | KEGG = D11429 | C=18 | H=24 | N=5 | O=3 | molecular_weight = 358.414 g/mol | smiles = CC(C)(C)[C@@H](CO)NC(=O)C1=NN(C2=C1C[C@H]3[C@@H]2C3)C4=NC=C[N+](=C4)[O-] | StdInChI = 1S/C18H23N5O3/c1-18(2,3)13(9-24)20-17(25)15-12-7-10-6-11(10)16(12)23(21-15)14-8-22(26)5-4-19-14/h4-5,8,10-11,13,24H,6-7,9H2,1-3H3,(H,20,25)/t10-,11-,13+/m0/s1 | StdInChIKey = ACSQLTBPYZSGBA-GMXVVIOVSA-N }}Olorinab (APD371) is a drug developed by Arena Pharmaceuticals for the treatment of pain associated with Crohn's disease. It acts as a potent and selective cannabinoid CB2 receptor agonist and is claimed to be orally active and peripherally selective, and has progressed to Phase II clinical trials.[1][2] See also
References1. ^{{cite journal | vauthors = Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J, Sadeque A, Usmani A, Chen C, Semple G, Grottick AJ, Al-Shamma H, Christopher R, Jones RM | display-authors = 6 | title = Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain | journal = ACS Medicinal Chemistry Letters | volume = 8 | issue = 12 | pages = 1309–1313 | date = December 2017 | pmid = 29259753 | doi = 10.1021/acsmedchemlett.7b00396 }} {{Cannabinoids}}{{Cannabinoid receptor modulators}}{{cannabinoid-stub}}2. ^{{cite web | title = Olorinab (APD371) | url = https://www.arenapharm.com/pipeline/apd371/ | publisher = Arena Pharmaceuticals, Inc. }} 1 : Cannabinoids |
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