SL65.0155

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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
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 - уреди | uredi izvor]

  1. 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. http://www.sciencedirect.com/science/article/pii/S1359644610007737.  edit
  2. 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. 
  3. 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. http://www.jcheminf.com/content/2/1/3.  edit
  4. 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. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12130738. 
  5. 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. http://linkinghub.elsevier.com/retrieve/pii/S0306-4522(04)00623-2. 
  6. 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. http://linkinghub.elsevier.com/retrieve/pii/S0006-8993(06)02658-8. 
  7. 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. 
  8. 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. http://linkinghub.elsevier.com/retrieve/pii/S1074-7427(08)00059-2. 
  9. 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. http://linkinghub.elsevier.com/retrieve/pii/S0166-4328(08)00436-1. 
  10. 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. http://linkinghub.elsevier.com/retrieve/pii/S0278-5846(09)00215-2. 
  11. 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. 
  12. Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0. http://books.google.com/books?id=J6i6YpvCQfIC&lpg=PA472&ots=83um0yH2Yr&dq=SL65.0155%20phase%20II&pg=PA472#v=onepage&q=&f=false. 

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