132449-89-9
132449-89-9 structure
- Name: Lesopitron (dihydrochloride)
- Chemical Name: 2-[4-[4-(4-chloropyrazol-1-yl)butyl]piperazin-1-yl]pyrimidine,dihydrochloride
- CAS Number: 132449-89-9
- Molecular Formula: C15H23Cl3N6
- Molecular Weight: 393.74200
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2017-05-07 09:52:17
- Modify Date: 2024-01-12 09:41:39
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Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
| Name | 2-[4-[4-(4-chloropyrazol-1-yl)butyl]piperazin-1-yl]pyrimidine,dihydrochloride |
|---|---|
| Synonyms |
E 4424
C15H21ClN6.2HCl LESOPITRON DIHYDROCHLORIDE Lesopitron (dihydrochloride) |
| Description | Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. |
|---|---|
| Related Catalog | |
| Target |
IC50:125 nM (5-HT1A receptor, in rat hippocampal membranes)[1] |
| In Vitro | In vitro binding and autoradiographic studies with [3H]8-OH-DPAT and [3H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT1A receptors in the rat brain with a relatively high affinity (pKi=7.35). As expected of a full agonist at postsynaptic 5-HT1A receptors, 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]. |
| 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]. |
| Animal Admin | Rats[2] Male Wistar rats weighing 270-300 g, are used. Lesopitron is administered either through the dialysis probe (dissolved in artificial CSF) or i.p. (dissolved in 0.9% saline, 2 mL/kg body weight). |
| References |
| Density | 1.31g/cm3 |
|---|---|
| Boiling Point | 504ºC at 760mmHg |
| Molecular Formula | C15H23Cl3N6 |
| Molecular Weight | 393.74200 |
| Flash Point | 258.6ºC |
| Exact Mass | 392.10500 |
| PSA | 50.08000 |
| LogP | 3.53580 |