Lesopitron | CAS#132449-46-8 | 5-HT1A receptor ligand

MedKoo Cat#: 598615 | Name: Lesopitron

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Lesopitron acts as a ligand for central serotonin 5-HT1A receptors.

Chemical Structure

Lesopitron

CAS#132449-46-8

Theoretical Analysis

MedKoo Cat#: 598615

Name: Lesopitron

CAS#: 132449-46-8

Chemical Formula: C15H21ClN6

Exact Mass: 320.1516

Molecular Weight: 320.82

Elemental Analysis: C, 56.16; H, 6.60; Cl, 11.05; N, 26.20

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

Lesopitron;

IUPAC/Chemical Name

2-(4-(4-(4-chloro-1H-pyrazol-1-yl)butyl)piperazin-1-yl)pyrimidine

InChi Key

AHCPKWJUALHOPH-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H21ClN6/c16-14-12-19-22(13-14)7-2-1-6-20-8-10-21(11-9-20)15-17-4-3-5-18-15/h3-5,12-13H,1-2,6-11H2

SMILES Code

ClC1=CN(CCCCN2CCN(C3=NC=CC=N3)CC2)N=C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 320.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Fisas MA, Farré A, Camarasa J, Escubedo E. Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors. Pharmacology. 2004 Oct;72(2):57-67. PubMed PMID: 15331910. 2: Fresquet A, Sust M, Lloret A, Murphy MF, Carter FJ, Campbell GM, Marion-Landais G. Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder. Ann Pharmacother. 2000 Feb;34(2):147-53. PubMed PMID: 10676820. 3: Phillips MA, Szabadi E, Bradshaw CM. 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 Dec;13(4):391-7. PubMed PMID: 10667616. 4: Sramek JJ, Fresquet A, Marion-Landais G, Hourani J, Jhee SS, Martinez L, Jensen CM, Bolles K, Carrington AT, Cutler NR. Establishing the maximum tolerated dose of lesopitron in patients with generalized anxiety disorder: a bridging study. J Clin Psychopharmacol. 1996 Dec;16(6):454-8. PubMed PMID: 8959472. 5: Haj-Dahmane S, Jolas T, Laporte AM, Gozlan H, Farré AJ, Hamon M, Lanfumey L. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat. Eur J Pharmacol. 1994 Apr 1;255(1-3):185-96. PubMed PMID: 8026543. 6: Micheli F. Lesopitron (Esteve). IDrugs. 2001 Feb;4(2):218-24. PubMed PMID: 16032484. 7: Serafini MT, Puig S, García-Encina G, Farran R, García-Soret A, Moragon T, Martínez L. Absorption, distribution and excretion of [14C]-Lesopitron after single and repeated administration in rats and dogs. Methods Find Exp Clin Pharmacol. 1997 Jan-Feb;19(1):61-72. Erratum in: Methods Find Exp Clin Pharmacol 1997 Apr;19(3):212. PubMed PMID: 9098842. 8: Palacios G, Muro MA, Paz Marín A. Differential effects of haloperidol and two anxiolytic drugs, buspirone and lesopitron, on c-Fos expression in the rat striatum and nucleus accumbens. Brain Res. 1996 Dec 2;742(1-2):141-8. PubMed PMID: 9117387. 9: García-Encina G, Farrán R, Puig S, Serafini MT, Martínez L. Automated high-performance liquid chromatographic assay for lesopitron, a novel anxiolytic, in human plasma using on-line solid-phase extraction. J Chromatogr B Biomed Appl. 1995 Aug 4;670(1):103-10. PubMed PMID: 7493067. 10: Ballarín M, Carceller A, Guitart X. Effect of acute administration of the 5-HT1A receptor ligand, lesopitron, on rat cortical 5-HT and dopamine turnover. Br J Pharmacol. 1994 Oct;113(2):425-30. PubMed PMID: 7530571; PubMed Central PMCID: PMC1510099. 11: Adam A, Rojas J, Pretel J, Martínez L, Ong H. Labelling of haptenic drug with digoxigenin for competitive immunoassay: its application to lesopitron, a new anxiolytic agent. J Pharm Biomed Anal. 1996 Oct;15(1):13-9. PubMed PMID: 8895072. 12: Robles LI, Barrios M, Del Pozo E, Dordal A, Baeyens JM. Effects of K+ channel blockers and openers on antinociception induced by agonists of 5-HT1A receptors. Eur J Pharmacol. 1996 Jan 11;295(2-3):181-8. PubMed PMID: 8720582. 13: Glavin GB, Alvarez I, Colombo M, Farré AJ. Effects of a novel 5-HT1A receptor agonist, E4424, on gastric adherent mucus levels following restraint stress in rats. Dig Dis Sci. 1995 Nov;40(11):2317-20. PubMed PMID: 7587808. 14: Lanfumey L, Haj-Dahmane S, Hamon M. Further assessment of the antagonist properties of the novel and selective 5-HT1A receptor ligands (+)-WAY 100 135 and SDZ 216-525. Eur J Pharmacol. 1993 Nov 2;249(1):25-35. PubMed PMID: 8282017. 15: Costall B, Naylor RJ. The influence of 5-HT2 and 5-HT4 receptor antagonists to modify drug induced disinhibitory effects in the mouse light/dark test. Br J Pharmacol. 1997 Nov;122(6):1105-18. PubMed PMID: 9401775; PubMed Central PMCID: PMC1565059. 16: Becker C, Hamon M, Benoliel JJ. Prevention by 5-HT1A receptor agonists of restraint stress- and yohimbine-induced release of cholecystokinin in the frontal cortex of the freely moving rat. Neuropharmacology. 1999 Apr;38(4):525-32. PubMed PMID: 10221756. 17: Corradetti R, Pugliese AM, Le Poul E, Laaris N, Hamon M, Lanfumey L. Electrophysiological effects of WAY 100635, a new 5-HT1A receptor antagonist, on dorsal raphe nucleus serotoninergic neurones and CA1 pyramidal cells in vitro. Acta Physiol Hung. 1996;84(4):407-9. PubMed PMID: 9328615. 18: VASCONCELOS ESTEVES. [Jaundice; progress of its diagnosis and therapy]. Med Contemp. 1950 May;68(5):203-28. Undetermined Language. PubMed PMID: 15416490. 19: Costall B, Domeney AM, Farre AJ, Kelly ME, Martinez L, Naylor RJ. Profile of action of a novel 5-hydroxytryptamine1A receptor ligand E-4424 to inhibit aversive behavior in the mouse, rat and marmoset. J Pharmacol Exp Ther. 1992 Jul;262(1):90-8. PubMed PMID: 1352556. 20: Farré AJ, Colombo M, Alvarez I, Glavin GB. Some novel 5-hydroxytryptamine1A (5-HT1A) receptor agonists reduce gastric acid and pepsin secretion, reduce experimental gastric mucosal injury and enhance gastric mucus in rats. J Pharmacol Exp Ther. 1995 Feb;272(2):832-7. PubMed PMID: 7853201.

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