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Lecozotan

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Lecozotan
Systematic (IUPAC) name
4-Cyano-N-[(2R)-2-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl]propyl]-N-2-pyridinylbenzamide hydrochloride
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 434283-16-6
ATC code None
PubChem CID 11156648
UNII 48854OTZ5E YesY
KEGG D04683 YesY
Chemical data
Formula C28H30ClN5O3 
Mol. mass 520.021 g/mol
SMILES eMolecules & PubChem
 YesY(what is this?)  (verify)

Lecozotan is an investigational drug by Wyeth tested for improvement of cognitive functions of Alzheimer's disease patients.[1] As of June 2008, the first Phase III clinical trial has been completed.[2]

[edit] Method of action

Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3] which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

[edit] References

  1. ^ H. Spreitzer (August 13, 2008). "Neue Wirkstoffe - Lecozotan" (in German). Österreichische Apothekerzeitung (17/2007): 805. 
  2. ^ ClinicalTrials
  3. ^ Schlechter, LE; Smith, DL; Rosenzweig-Lipson, S; Sukoff, SJ; Dawson, LA; Marquis, K; Jones, D; Piesla, M et al. (June 10, 2005). "Lecotozan (SRA-333): A selective serotonin1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and promotes procognitive effects". Journal of Pharmacology and Experimental Therapeutics 314 (3): 1274. doi:10.1124/jpet.105.086363. PMID 15951399. http://jpet.aspetjournals.org/cgi/content/short/jpet.105.086363v1. 
  4. ^ Childers, WE Jr, Harrison, BL, Abou-Gharbia, MA, Raje, S, Parks, V, Pangalos, MN, Schechter, LE (2007). "Lecozotan Hydrochloride". Drugs of the Future 32 (5): 399–407. doi:10.1358/dof.2007.032.05.1092901. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1092901&p_IsPs=N. 


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