lesopitron
- CAS No.
- 132449-89-9
- Chemical Name:
- lesopitron
- Synonyms
- E4424;Lesopitron (dihydrochloride);Lesopitron (dihydrochloride) (E4424)
- CBNumber:
- CB51310323
- Molecular Formula:
- C15H22Cl2N6
- Molecular Weight:
- 357.28
- MDL Number:
- MFCD00894211
- MOL File:
- 132449-89-9.mol
| Melting point | 194-197.5° |
|---|---|
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| form | Solid |
| color | White to off-white |
| FDA UNII | 4T5L4T8473 |
lesopitron Chemical Properties,Uses,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-HT1A 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
lesopitron Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38630 | 58 | |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| TargetMol Chemicals Inc. | +8613564774135 | zijue.cai@tsbiochem.com | United States | 19881 | 58 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9729 | 58 |
| Jinan ponder chemical co. LTD | 0531-0000 | thinklifescience@163.com | China | 19689 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10524 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223; | psaitong@jm-bio.com | China | 29774 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24642 | 58 |
| Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 15162312715 | sales@szzxbio.com | China | 2972 | 58 |
View Lastest Price from lesopitron manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-10-28 | Lesopitron dihydrochloride
132449-89-9
|
US $2500.00-1520.00 / mg | 10g | TargetMol Chemicals Inc. |
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- Lesopitron dihydrochloride
132449-89-9
- US $2500.00-1520.00 / mg
- TargetMol Chemicals Inc.