| 词条 | U-50488 |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 405766426 | IUPAC_name = 2-(3,4-dichlorophenyl)-N-methyl-N-[(1R,2R)-2-pyrrolidin-1-ylcyclohexyl]acetamide | image = U-50488 structure.svg | width = 200 | image2 = U-50488 molecule ball.png | alt2 = Ball-and-stick model of the U-50488 molecule | 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 = {{cascite|correct|??}} | CAS_number = 67198-13-4 | ATC_prefix = | ATC_suffix = | PubChem = 3036289 | IUPHAR_ligand = 1652 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 73358 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 441765 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 2300345 | C=19 | H=26 | Cl=2 | N=2 | O=1 | molecular_weight = 369.329 g/mol | smiles = CN([C@@H]1CCCC[C@H]1N2CCCC2)C(=O)CC3=CC(=C(C=C3)Cl)Cl | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C19H26Cl2N2O/c1-22(19(24)13-14-8-9-15(20)16(21)12-14)17-6-2-3-7-18(17)23-10-4-5-11-23/h8-9,12,17-18H,2-7,10-11,13H2,1H3/t17-,18-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = VQLPLYSROCPWFF-QZTJIDSGSA-N }}U-50488 is a drug which acts as a highly selective κ-opioid agonist, but without any μ-opioid antagonist effects.[1] It has analgesic, diuretic and antitussive effects,[2] and reverses the memory impairment produced by anticholinergic drugs.[3] U-50488 was one of the first selective kappa agonists invented and research on its derivatives has led to the development of a large family of related compounds.[4][5] This compound has never received FDA approval and there are no reported human cases in the literature involving an U-50488 overdose.[6] See also
References1. ^{{cite journal | vauthors = Von Voigtlander PF, Lewis RA | title = U-50,488, a selective kappa opioid agonist: comparison to other reputed kappa agonists | journal = Progress in Neuro-Psychopharmacology & Biological Psychiatry | volume = 6 | issue = 4-6 | pages = 467–70 | year = 1982 | pmid = 6298890 | doi = 10.1016/S0278-5846(82)80130-9 }} {{Opioidergics}}{{Nervous-system-drug-stub}}2. ^{{cite journal | vauthors = Kamei J | title = Role of opioidergic and serotonergic mechanisms in cough and antitussives | journal = Pulmonary Pharmacology | volume = 9 | issue = 5-6 | pages = 349–56 | year = 1996 | pmid = 9232674 | doi = 10.1006/pulp.1996.0046 }} 3. ^{{cite journal | vauthors = Hiramatsu M, Kameyama T | title = Roles of kappa-opioid receptor agonists in learning and memory impairment in animal models | journal = Methods and Findings in Experimental and Clinical Pharmacology | volume = 20 | issue = 7 | pages = 595–9 | date = September 1998 | pmid = 9819804 | doi = 10.1358/mf.1998.20.7.485724 }} 4. ^{{cite journal | vauthors = Szmuszkovicz J | title = U-50,488 and the kappa receptor: a personalized account covering the period 1973 to 1990 | journal = Progress in Drug Research. Fortschritte Der Arzneimittelforschung. Progres Des Recherches Pharmaceutiques | volume = 52 | pages = 167–95 | year = 1999 | pmid = 10396128 }} 5. ^{{cite journal | vauthors = Szmuszkovicz J | title = U-50,488 and the kappa receptor. Part II: 1991-1998 | journal = Progress in Drug Research. Fortschritte Der Arzneimittelforschung. Progres Des Recherches Pharmaceutiques | volume = 53 | pages = 1–51 | year = 1999 | pmid = 10616295 }} 6. ^{{cite journal | vauthors = Amin ZM, Rambaran KA, Fleming SW, Cho K, Chacko L, Alzghari SK | title = Addressing Hazards from Unscheduled Novel Psychoactive Substances as Research Chemicals: The Case of U-50488 | journal = Cureus | volume = 9 | issue = 12 | pages = e1914 | date = December 2017 | pmid = 29441248 | pmc = 5800751 | doi = 10.7759/cureus.1914 }} 4 : Chloroarenes|Acetamides|Pyrrolidines|Kappa agonists |
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