2. Neuronal Signaling
  3. Sigma Receptor
  4. Sigma-1 receptor antagonist 4

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance.

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Sigma-1 receptor antagonist 4 Chemical Structure

Sigma-1 receptor antagonist 4 Chemical Structure

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Sigma-1 receptor antagonist 4 Related Antibodies

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Description

Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance[1].

IC50 & Target

IC50: 19.1 ± 0.6 nM (σ1R)[1]
In Vivo

Sigma-1 receptor antagonist 4 (0–60 mg/kg; i.p.; single dose) dose-dependently enhances morphine-induced analgesia within a dose of 40 mg/kg[1].
Sigma-1 receptor antagonist 4 (30 mg/kg; i.p.; single dose) potentiates antinociception via enhancing the morphineinduced MOR agonism[1].

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

Animal Model: Mouse model[1]
Dosage: 10, 20, 30, 40, 50, 60 mg/kg
Administration: i.p.; dissolved in saline with 30% PEG300 and 5% DMSO; measured the percentage of maximal possible effect (% MPE)after 30 min
Result: Dose-dependently enhanced morphine-induced analgesia within a dose of 40 mg/kg. Potentiated antinociception via enhancing the morphine-induced MOR agonism.
Molecular Weight

334.45

Formula

C22H26N2O
SMILES

CC1=CC=C(C=C1)CCCN2CC3(C2)CC(N(C3)C4=CC=CC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

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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:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    dissolved in saline with 30% PEG300 and 5% DMSO

In Vivo Dissolution Calculator
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Purity & Documentation
References
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Sigma-1 receptor antagonist 4 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:

Sigma-1 receptor antagonist 4Sigma Receptorσ1R antagonistmorphineInhibitorinhibitorinhibit

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Sigma-1 receptor antagonist 4
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