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Lesopitron

Catalog No. T25672 CAS 132449-46-8

Lesopitron is an anxiolytic with pre- and postsynaptic 5-HT1A agonist activity and is more effective than 5-HT1A agonists in rat social interaction and marmoset anxiety models. lesopitron counteracts benzodiazepine withdrawal-induced anxiety in rodents with low acute toxicity and does not potentiate the effects of alcohol or barbiturates.

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Lesopitron, CAS 132449-46-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 143.00
5 mg	In stock	$ 360.00
10 mg	In stock	$ 530.00
25 mg	In stock	$ 859.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,590.00
500 mg	In stock	$ 3,190.00
1 mL * 10 mM (in DMSO)	In stock	$ 358.00

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Purity: 98.92%

Purity: 98.60%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

In vivo

Lesopitron (30 micrograms kg-1, i.p.) administered at a dose that induces anxiolytic behavior in rats markedly reduced 5-HT levels (to 45% of the basal value) in cortical perfusates, having no effect on 5-HIAA, DOPAC and HVA.[1]
Intraraphe administration of lesopitron (10 microM) caused a decrease incortical 5-HT levels (the effect being of the same order as that obtained after systemic injection), with no effect on 5-HIAA, DOPAC and HVA.[1]

Molecular Weight	320.82
Formula	C15H21ClN6
CAS No.	132449-46-8

Storage

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

Solubility Information

DMSO: 3.21 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. Ballarín M, et al. Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 ; 113(2):425-430. 2. Fisas MA, et al. Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors. Pharmacology. 2004 ; 72(2):57-67. 3. Fresquet A, et al. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. Ann Pharmacother. 2000 ; 34(2):147-15 4. Phillips MA, et al. The effects of the novel anxiolytic drug lesopitron, a full and selective 5-HT1A receptor agonist, on pupil diameter and oral temperature in man: comparison with buspirone. J Psychopharmacol. 1999 ; 13(4):391-397. 5. Sramek JJ, et al. Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. J Clin Psychopharmacol. 1996 ; 16(6):454-8. 6. Haj-Dahmane S, et al. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat. Eur J Pharmacol. 1994 ; 255(1-3):185-196.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library Neuronal Signaling Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max

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Keywords

Lesopitron 132449-46-8 GPCR/G Protein Neuroscience 5-HT Receptor inhibitor inhibit

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