2. Signaling Pathways
  3. Neuronal Signaling
  4. Sigma Receptor

Sigma Receptor

Sigma Receptor

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Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body. The endogenous ligand for these sites has not been identified, but steroid hormones (particularly progesterone), sphingolipid-derived amines and N,N-dimethyltryptamine can bind with fairly high affinity.

The sigma-1 receptor (σ1R) is an endoplasmic reticulum (ER)-resident chaperone protein that acts like an inter-organelle signaling modulator. It participates in many biological processes including nociception, cancer, stroke, memory, drug addiction, cardiac activity, and Alzheimer’s disease. The sigma-2 (σ2R) receptor is overexpressed in various human tumors. It has been validated as a biomarker for proliferating tumors.

Sigma Receptor Isoform Specific Products:

Sigma Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108511R
    PB28 dihydrochloride (Standard)
    		Modulator
    PB28 dihydrochloride (Standard) is the analytical standard of PB28 (dihydrochloride) (HY-108511). This product is intended for research and analytical applications. PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.
    PB28 dihydrochloride (Standard)
  • HY-W714837
    5-Phenyllevulinic acid
    5-Phenyllevulinic acid (4-Oxo-5-phenylpentanoic acid) is an endogenous fungal metabolite with inhibitory activity against the bacterium B. megaterium, the plant pathogenic fungus S. tritici, and the alga C. fusca. 5-Phenyllevulinic acid is also an intermediate in the synthesis of σ receptor ligands. 5-Phenyllevulinic acid holds potential for research in the field of anti-infection studies .
    5-Phenyllevulinic acid
  • HY-B1216R
    Oxeladin citrate (Standard)
    		Agonist
    Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research.
    Oxeladin citrate (Standard)
  • HY-177345A
    SV119 hydrochloride
    		Ligand
    SV119 hydrochloride is a sigma-2 ligand with a Ki value of 5.2 nM. SV119 hydrochloride enhances the efficient transport of drugs across the plasma membrane of cancer cells. The conjugation of dm-Erastin with SV119 hydrochloride successfully overcomes the internalization barrier observed in pancreatic cancer, while preserving the inherent anti-tumor activity of Erastin (HY-15763). Additionally, SV119 hydrochloride demonstrates cytotoxic effects on triple-negative breast cancer (TNBC) cells and induces apoptosis.
    SV119 hydrochloride
  • HY-169185
    Sigma-2 Radioligand 2
    Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor.
    Sigma-2 Radioligand 2
  • HY-13510R
    Cutamesine dihydrochloride (Standard)
    		Agonist
    Cutamesine dihydrochloride (Standard) is the analytical standard of Cutamesine dihydrochloride. This product is intended for research and analytical applications. Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
    Cutamesine dihydrochloride (Standard)
  • HY-101626R
    Sigma ligand-1 (Standard)
    Sigma ligand-1 (Standard) is the analytical standard of Sigma ligand-1 (HY-101626). This product is intended for research and analytical applications. Sigma ligand-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 has a Ki of 4000 nM at the dopamine D2 receptor.
    Sigma ligand-1 (Standard)
  • HY-108513
    σ1 Receptor antagonist 4
    		Antagonist
    σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters.
    σ1 Receptor antagonist 4
  • HY-101626AR
    Sigma ligand-1 hydrochloride (Standard)
    Sigma ligand-1 (hydrochloride) (Standard) is the analytical standard of Sigma ligand-1 (hydrochloride) (HY-101626A). This product is intended for research and analytical applications. Sigma ligand-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma ligand-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor.
    Sigma ligand-1 hydrochloride (Standard)
  • HY-118901R
    Opipramol (Standard)
    		Antagonist
    Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).
    Opipramol (Standard)
Sigma Receptor Isoform Comparison

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