Capeserod

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Capeserod
Capeserod.svg
Systematic (IUPAC) name
5-(5-amino-6-chloro-2,3-dihydro-1,4-benzodioxin-8-yl)-3-[1-(2-phenylethyl)piperidin-4-yl]-1,3,4-oxadiazol-2-one
Identifiers
CAS Number 769901-96-4
ATC code None
PubChem CID 9805719
IUPHAR/BPS 29
ChemSpider 7981479
UNII 8163770L8P
ChEMBL CHEMBL2027925
Chemical data
Formula C23H25ClN4O4
Molar mass 456.93 g·mol−1

Capeserod (INN,[1] previously known as SL65.0155) is a selective 5-HT4 receptor partial agonist with Ki = 0.6 nM and IA = 40–50% (relative to serotonin).[2] It potently enhances cognition, learning, and memory,[2][3][4][5][6][7] and also possesses antidepressant effects.[8] Capeserod 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.[9][10]

See also[edit]

References[edit]

  1. ^ "WHO Drug Information. Vol. 20, No. 3, 2006. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 56" (PDF). World Health Organization. p. 208. Retrieved 25 April 2016. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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. 
  6. ^ 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. 
  7. ^ 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. 
  8. ^ 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. 
  9. ^ 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. 
  10. ^ Roth, Bryan L. (2006). The Serotonin Receptors: From Molecular Pharmacology to Human Therapeutics (The Receptors). Totowa, NJ: Humana Press. ISBN 1-58829-568-0.