132449-89-9
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- CAS号:
- 132449-89-9
- 英文名:
- lesopitron
- 英文别名:
- E4424;Lesopitron (dihydrochloride);Lesopitron (dihydrochloride) (E4424)
- 中文名:
- 132449-89-9
- 中文别名:
- 来索吡琼二盐酸盐;化合物 T11839
- CBNumber:
- CB51310323
- 分子式:
- C15H22Cl2N6
- 分子量:
- 357.28
- MOL File:
- 132449-89-9.mol
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132449-89-9化学性质
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熔点:
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194-197.5°
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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132449-89-9性质、用途与生产工艺
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。
5-HT
1A
Receptor
125 nM (IC
50
, in rat hippocampal membranes)
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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
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).
Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID
50
=35 μg/kg i.v.). 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.
132449-89-9
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-101609 | Lesopitron dihydrochloride | | 1 mg | 8500元 |
2023/03/20 | HY-101609 | 132449-89-9 Lesopitron dihydrochloride | 132449-89-9 | 5mg | 29000元 |
132449-89-9, 132449-89-9 相关搜索:
- 化合物 T11839
- 来索吡琼二盐酸盐
- 132449-89-9
- Lesopitron (dihydrochloride) (E4424)
- E4424
- Lesopitron (dihydrochloride)