Lecozotan

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]

Lecozotan
Identifiers
IUPAC name
  • 4-Cyano-N-[(2R)-2-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl]propyl]-N-2-pyridinylbenzamide hydrochloride
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H30ClN5O3
Molar mass520.03 g·mol−1
3D model (JSmol)
SMILES
  • C[C@H](CN(C1=CC=CC=N1)C(=O)C2=CC=C(C=C2)C#N)N3CCN(CC3)C4=C5C(=CC=C4)OCCO5
InChI
  • InChI=1S/C28H29N5O3/c1-21(31-13-15-32(16-14-31)24-5-4-6-25-27(24)36-18-17-35-25)20-33(26-7-2-3-12-30-26)28(34)23-10-8-22(19-29)9-11-23/h2-12,21H,13-18,20H2,1H3/t21-/m1/s1
  • Key:NRPQELCNMADTOZ-OAQYLSRUSA-N
  (verify)

Method of action

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

References
  1. Spreitzer H (August 13, 2008). "Neue Wirkstoffe - Lecozotan". Österreichische Apothekerzeitung (in German) (17/2007): 805.
  2. ClinicalTrials
  3. Schechter LE, Smith DL, Rosenzweig-Lipson S, Sukoff SJ, Dawson LA, Marquis K, et al. (September 2005). "Lecozotan (SRA-333): a selective serotonin 1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties". The Journal of Pharmacology and Experimental Therapeutics. 314 (3): 1274–89. arXiv:1506.05421. doi:10.1124/jpet.105.086363. PMID 15951399.
  4. Childers Jr WE, 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.


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