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Lecozotan HCl

Catalog No. T27806 CAS 433282-68-9

Synonyms: SRA-333, SRA333, SRA 333, Lecozotan hydrochloride

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.

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Lecozotan HCl, CAS 433282-68-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 162.00
5 mg	In stock	$ 390.00
10 mg	In stock	$ 590.00
25 mg	In stock	$ 943.00
50 mg	In stock	$ 1,280.00
100 mg	In stock	$ 1,730.00
500 mg	In stock	$ 3,460.00

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Description

In vivo

Lecozotan HCl (0.3 mg/kg; s.c.) antagonized the decrease in hippocampal extracellular 5-HT induced by 8-hydroxy-2-dipropylaminotetralin (8-OH-DPAT) and had no effects alone at doses 10-fold higher. Lecozotan HCl significantly potentiated the potassium chloride-stimulated release of glutamate and acetylcholine in the dentate gyrus of the hippocampus. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model indicative of 5-HT(1A) receptor function.[1]
In drug discrimination studies, Lecozotan HCl (0.01-1 mg/kg i.m.) did not substitute for 8-OH-DPAT and produced a dose-related blockade of the 5-HT(1A) agonist discriminative stimulus cue. In aged rhesus monkeys, Lecozotan HCl produced a significant improvement in task performance efficiency at an optimal dose (1 mg/kg p.o.). Learning deficits induced by the glutamatergic antagonist MK-801 [(-)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate] (assessed by perceptually complex and visual spatial discrimination) and by specific cholinergic lesions of the hippocampus (assessed by visual spatial discrimination) were reversed by Lecozotan HCl (2 mg/kg i.m.) in marmosets.[1]

Synonyms	SRA-333, SRA333, SRA 333, Lecozotan hydrochloride
Molecular Weight	520.02
Formula	C28H30ClN5O3
CAS No.	433282-68-9

Storage

keep away from moisture,store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Schechter LE, et al. 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 Pharmacol Exp Ther. 2005;314(3):1274-1289. 2. Skirzewski M, et al. Acute lecozotan administration increases learning and memory in rats without affecting anxiety or behavioral depression. Pharmacol Biochem Behav. 2010;95(3):325-330. 3. Patat A, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of ascending single and multiple doses of lecozotan in healthy young and elderly subjects. Br J Clin Pharmacol. 2009;67(3):299-308. 4. Parks V, et al. Concomitant blockade of 5-HT(1A) receptor and 5-HT transporter: use of the Hunter Serotonin toxicity criteria in a clinical pharmacology study. Eur Neuropsychopharmacol. 2012;22(2):92-99. 5. Raje S, et al. A positron emission tomography study to assess binding of lecozotan, a novel 5-hydroxytryptamine-1A silent antagonist, to brain 5-HT1A receptors in healthy young and elderly subjects, and in patients with Alzheimer's disease. Clin Pharmacol Ther. 2008;83(1):86-96.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library GPCR Compound Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Membrane Protein-targeted Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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Keywords

Lecozotan HCl 433282-68-9 GPCR/G Protein Neuroscience 5-HT Receptor SRA-333 SRA333 SRA 333 Lecozotan Hydrochloride Lecozotan hydrochloride inhibitor inhibit

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