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Lesopitron dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lesopitron dihydrochloride图片
CAS NO:132449-89-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品名称
E4424
产品介绍
Lesopitron dihydrochloride 是选择性的5-HT1A受体激动剂,作用于大鼠海马膜,IC50为 125 nM。
生物活性

Lesopitron dihydrochloride is a full and selective5-HT1Areceptor agonist withIC50of 125 nM in rat hippocampal membranes.

IC50& Target

5-HT1AReceptor

125 nM (IC50, in rat hippocampal membranes)

体外研究
(In Vitro)

In vitro binding and autoradiographic studies with [3H]8-OH-DPAT and [3H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT1Areceptors in the rat brain with a relatively high affinity (pKi=7.35). As expected of a full agonist at postsynaptic 5-HT1Areceptors, Lesopitron (IC50=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, IC50=120 nM)[1].

体内研究
(In Vivo)

Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID50=35 μg/kg i.v.)[1]. Lesopitron administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, i.p.) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates[2].

分子量

393.74

性状

Solid

Formula

C15H23Cl3N6

CAS 号

132449-89-9

中文名称

来索吡琼二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)