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

Lesopitron dihydrochloride  (Synonyms: E4424)

Cat. No.: HY-101609 Purity: ≥98.0%
SDS COA Handling Instructions Technical Support

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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Based on 1 publication(s) in Google Scholar

Other Forms of Lesopitron dihydrochloride:

Lesopitron dihydrochloride Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Lesopitron dihydrochloride Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

393.74

Formula

C15H23Cl3N6
CAS No.
Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (31.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5397 mL 12.6987 mL 25.3975 mL
5 mM 0.5079 mL 2.5397 mL 5.0795 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

SDS (252 KB)

COA (246 KB) HNMR (242 KB)

Handling Instructions (2659 KB)
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5397 mL 12.6987 mL 25.3975 mL 63.4937 mL
5 mM 0.5079 mL 2.5397 mL 5.0795 mL 12.6987 mL
10 mM 0.2540 mL 1.2699 mL 2.5397 mL 6.3494 mL
15 mM 0.1693 mL 0.8466 mL 1.6932 mL 4.2329 mL
20 mM 0.1270 mL 0.6349 mL 1.2699 mL 3.1747 mL
25 mM 0.1016 mL 0.5079 mL 1.0159 mL 2.5397 mL
30 mM 0.0847 mL 0.4233 mL 0.8466 mL 2.1165 mL
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Lesopitron dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lesopitron132449-89-9E4424E 4424E-44245-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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