1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Lesopitron dihydrochloride

Lesopitron dihydrochloride (Synonyms: E4424)

Cat. No.: HY-101609
Handling Instructions

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

For research use only. We do not sell to patients.

Lesopitron dihydrochloride Chemical Structure

Lesopitron dihydrochloride Chemical Structure

CAS No. : 132449-89-9

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Description

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

IC50 & Target

5-HT1A Receptor

125 nM (IC50, in rat hippocampal membranes)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

393.74

Formula

C₁₅H₂₃Cl₃N₆

CAS No.

132449-89-9

SMILES

ClC1=CN(CCCCN2CCN(C3=NC=CC=N3)CC2)N=C1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Animal Administration
[2]

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).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

LesopitronE4424E 4424E-44245-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
Lesopitron dihydrochloride
Cat. No.:
HY-101609
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