SL65.0155
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| |||
| (IUPAC) ime | |||
|---|---|---|---|
| 5-(5-amino-6-hloro-2,3-dihidro-1,4-benzodioksin-8-il)-3-(1-fenetil-4-piperidil)-1,3,4-oksadiazol-2-on hidrohlorid | |||
| Klinički podaci | |||
| Identifikatori | |||
| ATC kod | nije dodeljen | ||
| PubChem[1][2] | 9805718 | ||
| ChemSpider[3] | 7981478 | ||
| Hemijski podaci | |||
| Formula | C23H26Cl2N4O4 | ||
| Mol. masa | 493,38 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
SL65.0155 je selektivni parcijalni agonist 5-HT4 receptora (Ki = 0.6 nM; IA = 40-50% (relativno na 5-HT)).[4] On potencijalno poboljšava spoznaju, učenje, i memoriju,[4][5][6][7][8][9] a poseduje i antidepresivna svojstva.[10] SL65.0155 je bio u fazi II kliničkih ispitivanja tokom 2004-2006 za lečenje amnezije i demencije.[11][12]
Reference[uredi | uredi kod]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.
- ↑ 4,0 4,1 Moser PC, Bergis OE, Jegham S, et al. (August 2002). „SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties”. The Journal of Pharmacology and Experimental Therapeutics 302 (2): 731-41. DOI:10.1124/jpet.102.034249. PMID 12130738.
- ↑ Spencer JP, Brown JT, Richardson JC, et al. (2004). „Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease”. Neuroscience 129 (1): 49-54. DOI:10.1016/j.neuroscience.2004.06.070. PMID 15489027.
- ↑ Micale V, Leggio GM, Mazzola C, Drago F (November 2006). „Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia”. Brain Research 1121 (1): 207-15. DOI:10.1016/j.brainres.2006.08.108. PMID 17011531.
- ↑ Restivo L, Roman F, Dumuis A, Bockaert J, Marchetti E, Ammassari-Teule M (September 2008). „The promnesic effect of G-protein-coupled 5-HT4 receptors activation is mediated by a potentiation of learning-induced spine growth in the mouse hippocampus”. Neuropsychopharmacology 33 (10): 2427-34. DOI:10.1038/sj.npp. 1301644. PMID 18075492.
- ↑ Marchetti E, Jacquet M, Jeltsch H, et al. (July 2008). „Complete recovery of olfactory associative learning by activation of 5-HT4 receptors after dentate granule cell damage in rats”. Neurobiology of Learning and Memory 90 (1): 185-91. DOI:10.1016/j.nlm.2008.03.010. PMID 18485752.
- ↑ Hille C, Bate S, Davis J, Gonzalez MI (December 2008). „5-HT4 receptor agonism in the five-choice serial reaction time task”. Behavioural Brain Research 195 (1): 180-6. DOI:10.1016/j.bbr.2008.08.007. PMID 18765258.
- ↑ Tamburella A, Micale V, Navarria A, Drago F (October 2009). „Antidepressant properties of the 5-HT4 receptor partial agonist, SL65.0155: behavioral and neurochemical studies in rats”. Progress in Neuro-psychopharmacology & Biological Psychiatry 33 (7): 1205-10. DOI:10.1016/j.pnpbp.2009.07.001. PMID 19596038.
- ↑ Bockaert J, Claeysen S, Compan V, Dumuis A (February 2004). „5-HT4 receptors”. Current Drug Targets. CNS and Neurological Disorders 3 (1): 39-51. PMID 14965243.
- ↑ Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.
Literatura[uredi | uredi kod]
- Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.
