SL65.0155

SL65.0155
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
Identifikatori
ATC kodnone
PubChemCID 9805718
ChemSpider7981478
Hemijski podaci
FormulaC23H26Cl2N4O4
Molarna masa493,38 g/mol
  • Cl.O=C1O/C(=NN1C3CCN(CCc2ccccc2)CC3)c5cc(Cl)c(c4OCCOc45)N

SL65.0155 je selektivni parcijalni agonist 5-HT4 receptora (Ki = 0.6 nM; IA = 40-50% (relativno na 5-HT)).[1] On potencijalno poboljšava spoznaju, učenje, i memoriju,[1][2][3][4][5][6] a poseduje i antidepresivna svojstva.[7] SL65.0155 je bio u fazi II kliničkih ispitivanja tokom 2004-2006 za lečenje amnezije i demencije.[8][9]

Reference

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  1. ^ а б Moser PC; Bergis OE; Jegham S; et al. (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. PMID 12130738. S2CID 18256582. doi:10.1124/jpet.102.034249. 
  2. ^ 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. PMID 15489027. S2CID 41720408. doi:10.1016/j.neuroscience.2004.06.070. 
  3. ^ Micale V, Leggio GM, Mazzola C, Drago F (2006). „Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia”. Brain Research. 1121 (1): 207—15. PMID 17011531. S2CID 25494253. doi:10.1016/j.brainres.2006.08.108. 
  4. ^ Restivo L, Roman F, Dumuis A, Bockaert J, Marchetti E, Ammassari-Teule M (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. PMID 18075492. S2CID 13405059. doi:10.1038/sj.npp.1301644. 
  5. ^ Marchetti E; Jacquet M; Jeltsch H; et al. (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. PMID 18485752. S2CID 38967009. doi:10.1016/j.nlm.2008.03.010. 
  6. ^ Hille C, Bate S, Davis J, Gonzalez MI (2008). „5-HT4 receptor agonism in the five-choice serial reaction time task”. Behavioural Brain Research. 195 (1): 180—6. PMID 18765258. S2CID 1063310. doi:10.1016/j.bbr.2008.08.007. 
  7. ^ Tamburella A, Micale V, Navarria A, Drago F (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. PMID 19596038. S2CID 207408833. doi:10.1016/j.pnpbp.2009.07.001. 
  8. ^ Bockaert J, Claeysen S, Compan V, Dumuis A (2004). „5-HT4 receptors” (PDF). Current Drug Targets. CNS and Neurological Disorders. 3 (1): 39—51. PMID 14965243. doi:10.2174/1568007043482615. 
  9. ^ Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 978-1-58829-568-2. 

Literatura

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