| Identification | Back Directory | [Name]
Lecozotan hydrochloride | [CAS]
433282-68-9 | [Synonyms]
Sra 333
Sra-333
Lecozotan sr
Lecozotan HCl
Lecozotan hydrochloride
Benzamide, 4-cyano-N-((2R)-2-(4-(2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl)propyl)-N-2-pyridinyl-, monohydrochloride | [Molecular Formula]
C28H29N5O3.ClH | [MDL Number]
MFCD11100262 | [MOL File]
433282-68-9.mol | [Molecular Weight]
520.02 |
| Hazard Information | Back Directory | [Description]
Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model demonstrating 5-HT(1A) receptor function. | [Uses]
Treatment of cognitive deficits associated with Alzheimer’s disease (5-HT1A
receptor antagonist). | [References]
[1] WAYNE E. CHILDERS. Synthesis and Biological Evaluation of Benzodioxanylpiperazine Derivatives as Potent Serotonin 5-HT1A Antagonists: The Discovery of Lecozotan[J]. Journal of Medicinal Chemistry, 2005, 48 10: 3467-3470. DOI:10.1021/jm049493z.
[2] L E SCHECHTER. 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.[J]. Journal of Pharmacology and Experimental Therapeutics, 2005, 314 3: 1274-1289. DOI:10.1124/jpet.105.086363.
[3] KEVIN BOOTH. P3-425: Safety, tolerability and efficacy of lecozotan SR in patients with mild-to-moderate Alzheimer’s disease used as monotherapy or adjunctively with a cholinesterase inhibitor[J]. Alzheimer’s & Dementia, 2012, 8 4S_Part_16: P604. DOI:10.1016/j.jalz.2012.05.2099.
[4] MIGUEL SKIRZEWSKI . Acute lecozotan administration increases learning and memory in rats without affecting anxiety or behavioral depression[J]. Pharmacology Biochemistry and Behavior, 2010, 95 3: Pages 325-330. DOI:10.1016/j.pbb.2010.02.008. |
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