Chemistry:Capeserod

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Short description: Chemical compound
Capeserod
Capeserod.svg
Clinical data
ATC code
  • None
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC23H25ClN4O4
Molar mass456.93 g·mol−1
3D model (JSmol)

Capeserod (INN;[1] development code 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

References

  1. ↑ "WHO Drug Information. Vol. 20, No. 3, 2006. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 56". World Health Organization. p. 208. http://apps.who.int/medicinedocs/documents/s14181e/s14181e.pdf. 
  2. ↑ 2.0 2.1 "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. August 2002. doi:10.1124/jpet.102.034249. PMID 12130738. https://hal.archives-ouvertes.fr/hal-03161682/file/Version%20HAL.pdf. 
  3. ↑ "Modulation of hippocampal excitability by 5-HT4 receptor agonists persists in a transgenic model of Alzheimer's disease". Neuroscience 129 (1): 49–54. 2004. doi:10.1016/j.neuroscience.2004.06.070. PMID 15489027. 
  4. ↑ "Cognitive effects of SL65.0155, a serotonin 5-HT4 receptor partial agonist, in animal models of amnesia". Brain Research 1121 (1): 207–15. November 2006. doi:10.1016/j.brainres.2006.08.108. PMID 17011531. 
  5. ↑ "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. September 2008. doi:10.1038/sj.npp.1301644. PMID 18075492. 
  6. ↑ "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. July 2008. doi:10.1016/j.nlm.2008.03.010. PMID 18485752. https://univoak.eu/islandora/object/islandora%3A84565. 
  7. ↑ "5-HT4 receptor agonism in the five-choice serial reaction time task". Behavioural Brain Research 195 (1): 180–6. December 2008. doi:10.1016/j.bbr.2008.08.007. PMID 18765258. 
  8. ↑ "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. October 2009. doi:10.1016/j.pnpbp.2009.07.001. PMID 19596038. 
  9. ↑ "5-HT4 receptors". Current Drug Targets. CNS and Neurological Disorders 3 (1): 39–51. February 2004. doi:10.2174/1568007043482615. PMID 14965243. https://hal.archives-ouvertes.fr/hal-01667891/file/2004%20CDT%20Bockaert.pdf. 
  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. https://books.google.com/books?id=J6i6YpvCQfIC&q=SL65.0155%20phase%20II&pg=PA472. 




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