lesopitron

Product Name: lesopitron
CAS No.: 132449-89-9
Chemical Name: lesopitron
Synonyms: E4424;Lesopitron (dihydrochloride);Lesopitron (dihydrochloride) (E4424);2-(4-(4-(4-Chloro-1H-pyrazol-1-yl)butyl)piperazin-1-yl)pyrimidine dihydrochloride
CBNumber: CB51310323
Molecular Formula: C15H22Cl2N6
Formula Weight: 357.28
MOL File: 132449-89-9.mol

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lesopitron Property

Melting point:: 194-197.5°
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P501Dispose of contents/container to..…

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lesopitron Chemical Properties,Usage,Production

Uses

Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.

Biological Activity

Lesopitron dihydrochloride is a selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membrane.

in vitro

In vitro binding and autoradiographic studies with [ ³ H]8-OH-DPAT and [ ³ H]Lesopitron as radioligands confirm that Lesopitron binds to 5 -HT _1A receptors in the rat brain with a relatively high affinity (pK _i =7.35). As expected of a full agonist at postsynaptic 5-HT _{1A < /sub> receptors, Lesopitron (IC ₅₀ =125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC ₅₀ =120 nM).}

in vivo

Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID ₅₀ =35 μg/kg iv). It administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, ip) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates.

target

5-HT _1A Receptor

125 nM (IC ₅₀ , in rat hippocampal membranes)

IC 50

5-HT_1A Receptor: 125 nM (IC₅₀, in rat hippocampal membranes)

References

[1] 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 Apr 1;255(1-3):185-96. DOI:10.1016/0014-2999(94)90097-3
[2] 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 Oct;113(2):425-30. DOI:10.1111/j.1476-5381.1994.tb17006.x

lesopitron Preparation Products And Raw materials

Raw materials

Preparation Products

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lesopitron Suppliers

China 9 United States 5 Global 14

Fan De(Beijing) Biotechnology Co., Ltd.

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TargetMol Chemicals Inc.

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132449-89-9, lesopitronRelated Search:

Lesopitron (dihydrochloride)

E4424

Lesopitron (dihydrochloride) (E4424)

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

132449-89-9