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Cat. No.: HY-W754019

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Cinuperone

Cinuperone is a multi-target competitive receptor ligand and σ receptor antagonist that acts on Dopamine D1, σ, Dopamine D1, and 5-HT₂ receptors. Cinuperone shows significantly higher affinity for σ receptors than for Dopamine D1 receptors, and only exhibits moderate binding activity for dopamine D2 receptors. Cinuperone can be used in the research of central nervous system diseases.

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

CAS No.: 82117-51-9
Formula: C₂₃H₂₄FN₃O
Molecular Weight:377.46

Storage:

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

Cinuperone Chemical Structure

CAS No.: 82117-51-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[2]

D₂ Receptor

75 nM (IC₅₀)

D₁ Receptor

6200 nM (IC₅₀)

5-HT₂ Receptor

240 nM (IC₅₀)

All Sigma Receptor Isoforms :

All Dopamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

In Vitro

Cinuperone potently inhibits [³H]-spiperone binding to dopamine₂ receptors in rat striatal membranes with an IC₅₀ of 76 nM^[2].

Cinuperone weakly inhibits [³H]-SCH 23390 binding to dopamine₁ receptors in rat striatal membranes with an IC₅₀ of 6200 nM^[2].

Cinuperone potently inhibits [³H]-haloperidol binding to σ receptors in rat cerebellar membranes with an IC₅₀ of 54 nM^[2].

Cinuperone moderately inhibits [³H]-ketanserin binding to 5-HT₂ receptors in rat frontal cortex membranes with an IC₅₀ of 240 nM^[2].

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

In Vivo

Cinuperone (4.0 μmol/kg; administered 30 minutes prior to amphetamine) antagonizes amphetamine-induced hyperlocomotion in male albino mice with an ED₅₀ of 4.0 μmol/kg^[2].

Cinuperone (10 μmol/kg; administered 30 minutes prior to apomorphine) antagonizes apomorphine-induced climbing in male albino mice with an ED₅₀ of 10 μmol/kg^[2].

Cinuperone (15 μmol/kg; administered 30 minutes prior to apomorphine) antagonizes apomorphine-induced yawning in male albino rats with an ED₅₀ of 15 μmol/kg^[2].

Cinuperone (0.97 μmol/kg; i.p.; administered 30 minutes prior to quipazine) antagonizes quipazine-induced head twitches in male albino rats with an ED₅₀ of 0.97 μmol/kg^[2].

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

Chemical Information

CAS No. 82117-51-9
Molecular Weight 377.46
Formula C₂₃H₂₄FN₃O
SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CCN(C=3N=CC4=CC=CC=C4C3)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Berardi F, et al. New σ and 5-HT₁A Receptor Ligands: ω-(Tetralin-1-yl)-n-alkylamine Derivatives. Journal of Medicinal Chemistry. 1996;39(1):176-182.

[2]. Lang A, et al. Pharmacological comparison of antipsychotic drugs and sigma-antagonists in rodents. Pharmacology & toxicology. 1994;75(3-4):222-7. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Cinuperone

All Sigma Receptor Isoforms

All Dopamine Receptor Isoforms

All 5-HT Receptor Isoforms