SL65.0155

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SL65.0155
SL650155-structure.png
Systematic (IUPAC) name
5-(5-amino-6-chloro-2,3-dihydro-1,4-benzodioxin-8-yl)-3-(1-phenethyl-4-piperidyl)-1,3,4-oxadiazol-2-one hydrochloride
Clinical data
Legal status
?
Identifiers
CAS number ?
ATC code None
PubChem CID 9805718
ChemSpider 7981478
Chemical data
Formula C23H26Cl2N4O4 
Mol. mass 493.38 g/mol

SL65.0155 is a selective 5-HT4 receptor partial agonist (Ki = 0.6 nM; IA = 40-50% (relative to 5-HT)).[1] It potently enhances cognition, learning, and memory,[1][2][3][4][5][6] and also possesses antidepressant effects.[7] SL65.0155 was in phase II clinical trials around 2004-2006 for the treatment of memory deficits and dementia but no new information has surfaced since and it appears to have been abandoned.[8][9]

See also[edit]

References[edit]

  1. ^ a b 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. 
  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. doi:10.1016/j.neuroscience.2004.06.070. PMID 15489027. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ Bockaert J, Claeysen S, Compan V, Dumuis A (February 2004). "5-HT4 receptors". Current Drug Targets. CNS and Neurological Disorders 3 (1): 39–51. doi:10.2174/1568007043482615. PMID 14965243. 
  9. ^ Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.