σ1R/H3R ligand-1
σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain.
For research use only. We do not sell to patients.
- Formula: C22H25FN2
- Molecular Weight:336.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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human H3 receptor 31.2 nM (Ki) |
guinea pig σ1R 8.8 nM (Ki) |
σ1R/H3R ligand-1 (Compound 67) potently binds to σ1R in guinea pig brain cell membranes, with a Ki value of 8.8 nM[1].
σ1R/H3R ligand-1 potently binds to human H3R with a Kd value of 31.2 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
σ1R/H3R ligand-1 (0.0125-0.2 mg/kg; s.c.) potently and dose-dependently reverses mechanical hyperalgesia in a mouse model of paclitaxel (HY-B0015)-induced neuropathic pain, with an ED50 of 0.06 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (female, 20-32 g)[1]
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Dosage:0.04 mg/kg; 0.2 mg/kg; 1 mg/kg
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Administration:s.c.
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Result:Produced antinociceptive inhibition rates of 20.1%, 53.4%, and 83.2% at doses of 0.04 mg/kg, 0.2 mg/kg, and 1 mg/kg respectively.
Reached an ED50 of 0.18 mg/kg (95% CI, 0.167-0.183 mg/kg).
Achieved an antinociceptive effect with MPE = 53.42%.
Had its antinociceptive effect significantly reversed by co-administration with either the H3R agonist RαMH (15 mg/kg, s.c.) or the σ1R agonist PRE-084 (HY-18100) (32 mg/kg, s.c.).
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Animal Model:ICR mice (female, 20-32 g, paclitaxel-induced neuropathic pain model)[1]
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Dosage:0.0125 mg/kg; 0.05 mg/kg; 0.2 mg/kg
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Administration:s.c.
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Result:Produced inhibition rates of mechanical allodynia of 24.72%, 48.56%, and 74.75% at doses of 0.0125 mg/kg, 0.05 mg/kg, and 0.2 mg/kg respectively.
Reached a maximum effect at 45 minutes post-administration, and an ED50 of 0.06 mg/kg.
Chemical Information
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Molecular Weight 336.45
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Formula C22H25FN2
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SMILES
FC1=CC=C(NC=C2CCCN3CCC(C4=CC=CC=C4)CC3)C2=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
σ1R/H3R ligand-1 Related Classifications
HY-181722 Related Classifications
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