| 词条 | ORG-25935 |
| 释义 |
| verifiedrevid = | IUPAC_name = 2-([(1R,2S)-6-Methoxy-1-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl]methyl-methylamino)acetic acid | image =Org 25935.svg | width = 230 | tradename = | legal_status = | bioavailability = | metabolism = | elimination_half-life = | excretion = | PubChem = 11717074 | CAS_number = 949588-40-3 | ChemSpiderID = 9891795 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 55L20667O4 | C = 21 | H = 25 | N = 1 | O = 3 | molecular_weight = 339.427 g/mol | smiles = O=C(O)CN(C)C[C@@H]2[C@@H](c1c(cc(OC)cc1)CC2)c3ccccc3 | StdInChI = 1S/C21H25NO3/c1-22(14-20(23)24)13-17-9-8-16-12-18(25-2)10-11-19(16)21(17)15-6-4-3-5-7-15/h3-7,10-12,17,21H,8-9,13-14H2,1-2H3,(H,23,24)/t17-,21+/m1/s1 | StdInChIKey = UEBBYLJZCHTLEG-UTKZUKDTSA-N }}ORG-25935, also known as SCH-900435 is a synthetic drug developed by Organon International, which acts as a selective inhibitor of the glycine transporter GlyT-1. In animal tests it reduces alcohol consumption and has analgesic and anticonvulsant effects, but it has mainly been studied for its antipsychotic properties, and in human trials it was shown to effectively counteract the effects of the dissociative drug ketamine.[1][2][3][4][5][6][7][8] See also
References1. ^Molander A, Lidö HH, Löf E, Ericson M, Söderpalm B. The glycine reuptake inhibitor Org 25935 decreases ethanol intake and preference in male wistar rats. Alcohol and Alcoholism. 2007 Jan-Feb;42(1):11-8. {{PMID|17098748}} {{Glycine receptor modulators}}{{nervous-system-drug-stub}}2. ^Morita K, Motoyama N, Kitayama T, Morioka N, Dohi T. Antinociceptive effects of glycine transporter inhibitors in neuropathic pain models in mice. Nihon Yakurigaku Zasshi. 2007 Dec;130(6):458-63. {{PMID|18079595}} 3. ^Lidö HH, Stomberg R, Fagerberg A, Ericson M, Söderpalm B. The glycine reuptake inhibitor org 25935 interacts with basal and ethanol-induced dopamine release in rat nucleus accumbens. Alcoholism: Clinical and Experimental Research. 2009 Jul;33(7):1151-7. {{PMID|19389199}} 4. ^Kalinichev M, Starr KR, Teague S, Bradford AM, Porter RA, Herdon HJ. Glycine transporter 1 (GlyT1) inhibitors exhibit anticonvulsant properties in the rat maximal electroshock threshold (MEST) test. Brain Research. 2010 May 17;1331:105-13. {{PMID|20303337}} 5. ^Vengeliene V, Leonardi-Essmann F, Sommer WH, Marston HM, Spanagel R. Glycine transporter-1 blockade leads to persistently reduced relapse-like alcohol drinking in rats. Biological Psychiatry. 2010 Oct 15;68(8):704-11. {{PMID|20655511}} 6. ^Musante V, Summa M, Cunha RA, Raiteri M, Pittaluga A. Pre-synaptic glycine GlyT1 transporter--NMDA receptor interaction: relevance to NMDA autoreceptor activation in the presence of Mg2+ ions. Journal of Neurochemistry. 2011 May;117(3):516-27. DOI 10.1111/j.1471-4159.2011.07223.x. {{PMID|21348870}} 7. ^Jardemark K, Marcus MM, Malmerfelt A, Shahid M, Svensson TH. Differential effects of AMPA receptor potentiators and glycine reuptake inhibitors on antipsychotic efficacy and prefrontal glutamatergic transmission. Psychopharmacology. 2011 Nov 9. {{PMID|22068461}} 8. ^D'Souza DC, Singh N, Elander J, Carbuto M, Pittman B, de Haes JU, Sjogren M, Peeters P, Ranganathan M, Schipper J. Glycine Transporter Inhibitor Attenuates the Psychotomimetic Effects of Ketamine in Healthy Males: Preliminary Evidence. Neuropsychopharmacology. 2011 Nov 23. DOI 10.1038/npp.2011.295. {{PMID|22113087}} 2 : Drugs acting on the nervous system|Glycine reuptake inhibitors |
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