| 词条 | S-444,823 |
| 释义 |
| IUPAC_name = 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid | image = S-444,823_structure.png | width = 260 | drug_name = | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 885490-15-3 | ATC_prefix = none | ATC_suffix = | ChemSpiderID = 28501432 | C=25 | H=33 | N=3 | O=4 | S=1 | molecular_weight = 471.61 g/mol | smiles = O=C(C(C(NC1=NC(CCC(O)=O)=CS1)=O)=C2)N(CC3CCCCC3)C4=C2CCCCCC4 | StdInChI = 1S/C25H33N3O4S/c29-22(30)13-12-19-16-33-25(26-19)27-23(31)20-14-18-10-6-1-2-7-11-21(18)28(24(20)32)15-17-8-4-3-5-9-17/h14,16-17H,1-13,15H2,(H,29,30)(H,26,27,31) | StdInChIKey = SYBONVBDFTYUQP-UHFFFAOYSA-N }}S-444,823 is a drug developed by Shionogi which is a cannabinoid agonist.[1] It was developed as an antipruritic, and has moderate selectivity for the CB2 subtype, having a CB2 affinity of 18nM, and 32x selectivity over the CB1 receptor. In animal studies it showed analgesic effects and strongly reduced itching responses, but without producing side effects such as sedation and catalepsy that are seen with centrally acting CB1 agonists.[2] See also
References1. ^Arimura A. Novel Use of Cannabinoid Receptor Agonist. Patent WO 2005/016351 {{Cannabinoids}}{{cannabinoid-stub}}2. ^Odan M, et al. Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent. Bioorganic & Medicinal Chemistry Letters. 2012 Apr 15;22(8):2898-901. {{PMID|22421019}} 1 : Cannabinoids |
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