2. Neuronal Signaling Immunology/Inflammation GPCR/G Protein
  3. Sigma Receptor Histamine Receptor
  4. 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.

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σ1R/H3R ligand-1

σ1R/H3R ligand-1 Chemical Structure

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σ1R/H3R ligand-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

human H3 receptor

31.2 nM (Ki)

guinea pig σ1R

8.8 nM (Ki)

In Vitro

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 Related Antibodies
In Vivo

σ1R/H3R ligand-1 (0.04-1 mg/kg; s.c.) exhibits potent, dose-dependent analgesic activity in a mouse model of acetic acid-induced visceral pain via the dual action of simultaneously antagonizing σ1R and H3R, with an ED50 of 0.18 mg/kg[1].
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.

Animal Model: ICR mice (female, 20-32 g)[1]
Dosage: 0.04 mg/kg; 0.2 mg/kg; 1 mg/kg
Administration: s.c.
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.).
Animal Model: ICR mice (female, 20-32 g, paclitaxel-induced neuropathic pain model)[1]
Dosage: 0.0125 mg/kg; 0.05 mg/kg; 0.2 mg/kg
Administration: s.c.
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.
Molecular Weight

336.45

Formula

C22H25FN2
SMILES

FC1=CC=C(NC=C2CCCN3CCC(C4=CC=CC=C4)CC3)C2=C1
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
References
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σ1R/H3R ligand-1 Related Classifications

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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:

σ1R/H3R ligand-1Sigma ReceptorHistamine Receptorσ1R/H3R antagonistvisceral painneuropathic painICR mice
Inhibitorinhibitorinhibit

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