| 词条 | Igmesine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 451223940 | IUPAC_name = (E)-N-(cyclopropylmethyl)-N-ethyl-3,6-diphenylhex-5-en-3-amine | image = Igmesine.png | width = 250px | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 140850-73-3 | ATC_prefix = none | ATC_suffix = | PubChem = 6438340 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = XA3745J38K | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 4942823 | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C23H29N/c1-3-23(22-14-8-5-9-15-22,24(2)19-21-16-17-21)18-10-13-20-11-6-4-7-12-20/h4-15,21H,3,16-19H2,1-2H3/b13-10+ | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = VCZSWYIFCKGTJI-JLHYYAGUSA-N | C=23 | H=29 | N=1 | molecular_weight = 319.483 g/mol | smiles = N(C(c1ccccc1)(CC)C\\C=C\\c2ccccc2)(C)CC3CC3 }}Igmesine (JO-1,784) is a sigma receptor agonist (IC50 = 39 nM (rat brain)).[1][2] It has neuroprotective and antidepressant-like effects in animal studies,[3][4] as well as nootropic effects in models of age-related cognitive decline.[5] In two phase II clinical trials, igmesine was found to be effective in the treatment of depression and was as active as the comparator fluoxetine.[2] However, in a large phase III clinical trial, igmesine failed to show significant effectiveness for depression.[6] The drug has not been developed further.[7] References1. ^{{cite journal |vauthors=Roman FJ, Pascaud X, Martin B, Vauché D, Junien JL |title=JO 1784, a potent and selective ligand for rat and mouse brain sigma-sites |journal=The Journal of Pharmacy and Pharmacology |volume=42 |issue=6 |pages=439–40 |date=June 1990 |pmid=1979628 |doi= 10.1111/j.2042-7158.1990.tb06588.x|url=}} {{Sigma receptor modulators}}2. ^1 {{cite journal | vauthors = Fishback JA, Robson MJ, Xu YT, Matsumoto RR | title = Sigma receptors: potential targets for a new class of antidepressant drug | journal = Pharmacol. Ther. | volume = 127 | issue = 3 | pages = 271–82 | year = 2010 | pmid = 20438757 | pmc = 3993947 | doi = 10.1016/j.pharmthera.2010.04.003 | url = }} 3. ^{{cite journal |vauthors=O'Neill M, Caldwell M, Earley B, Canney M, O'Halloran A, Kelly J, Leonard BE, Junien JL |title=The sigma receptor ligand JO 1784 (igmesine hydrochloride) is neuroprotective in the gerbil model of global cerebral ischaemia |journal=European Journal of Pharmacology |volume=283 |issue=1-3 |pages=217–25 |date=September 1995 |pmid=7498313 |doi= 10.1016/0014-2999(95)00356-P|url=}} 4. ^{{cite journal |vauthors=Akunne HC, Zoski KT, Whetzel SZ, Cordon JJ, Brandon RM, Roman F, Pugsley TA |title=Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant |journal=Neuropharmacology |volume=41 |issue=1 |pages=138–49 |date=July 2001 |pmid=11445194 |doi= 10.1016/S0028-3908(01)00049-1|url=}} 5. ^{{cite journal |vauthors=Maurice T, Roman FJ, Su TP, Privat A |title=Beneficial effects of sigma agonists on the age-related learning impairment in the senescence-accelerated mouse (SAM) |journal=Brain Research |volume=733 |issue=2 |pages=219–30 |date=September 1996 |pmid=8891305 |doi= 10.1016/0006-8993(96)00565-3|url=}} 6. ^{{cite journal | vauthors = Hayashi T, Tsai SY, Mori T, Fujimoto M, Su TP | title = Targeting ligand-operated chaperone sigma-1 receptors in the treatment of neuropsychiatric disorders | journal = Expert Opin. Ther. Targets | volume = 15 | issue = 5 | pages = 557–77 | year = 2011 | pmid = 21375464 | pmc = 3076924 | doi = 10.1517/14728222.2011.560837 | url = }} 7. ^{{cite journal |vauthors=Volz HP, Stoll KD |title=Clinical trials with sigma ligands |journal=Pharmacopsychiatry |volume=37 Suppl 3 |issue= |pages=S214–20 |date=November 2004 |pmid=15547788 |doi=10.1055/s-2004-832680 |url=}} 4 : Amines|Alkene derivatives|Cyclopropanes|Sigma agonists |
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