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-18101S
    BD-1063-d8 dihydrochloride
    BD-1063-d8 dihydrochloride is the deuterium labeled BD1063 dihydrochloride (HY-18101A). BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.
    BD-1063-d<sub>8</sub> dihydrochloride
  • HY-123408
    Umespirone
    Umespirone (KC 9172) is a potential antipsychotic/antianxiety agent.
    Umespirone
  • HY-14221B
    Siramesine fumarate
    		Agonist
    Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.
    Siramesine fumarate
  • HY-163075
    SYB4
    SYB4 (compound 5) is a PET tracer which suitable for imaging the Sigma-2 Receptor in the brain of nonhuman primates.
    SYB4
  • HY-158197
    RC-106
    		Inhibitor
    RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity. RC-106 has antiproliferative activity against cancer cells including glioblastoma (GB) and multiple myeloma (MM).
    RC-106
  • HY-149855
    AB10
    		Antagonist
    AB10 is a selective S1R antagonist. AB10 with Ki of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model.
    AB10
  • HY-174155
    Sigma-2 Receptor ligand 1
    		Ligand
    Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective Sigma-2 receptor ligand with a Ki value of 40 nM. Sigma-2 Receptor ligand 1 is promising for research of Alzheimer's disease.
    Sigma-2 Receptor ligand 1
  • HY-159997
    AD353
    AD353 is a selective sigma-1 receptor ligand with antiallodynic activity. AD353 exhibits high potency both in a model of Capsaicin (HY-10448)-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile.
    AD353
  • HY-119386
    SAS-0132
    		Antagonist
    SAS-0132 is a selective Sigma 2 receptor (Sig2R) antagonist (Ki: 90 nM) that can cross the blood-brain barrier. SAS-0132 is capable of regulating intracellular Ca2+ levels and modulating PGRMC1-related pathways. SAS-0132 exhibits neuroprotective activity and can improve cognitive impairment in Alzheimer's disease mice. SAS-0132 can be used in the research of neurocognitive disorders such as Alzheimer's disease.
    SAS-0132
  • HY-129485
    CM304
    		Antagonist
    CM304 is a potent S1R inhibitor that can inhibit drug-induced convulsions in rats.
    CM304
  • HY-155616
    KSK94
    		Antagonist
    KSK94 is a high-affinity histamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain.
    KSK94
  • HY-147560
    σ1 Receptor/μ Opioid receptor modulator 1
    		Antagonist
    σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain.
    σ1 Receptor/μ Opioid receptor modulator 1
  • HY-131914
    EST64454
    		Antagonist
    EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain.
    EST64454
  • HY-175367
    H3R antagonist 6
    		Inhibitor
    H3R antagonist 6 (Compounds 3) (H3-2406) is a Histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. H3R antagonist 6 labeled with 18F has high radiochemical yield, molar activity and moderate brain uptake, but with an off-target binding to the Sigma-1 receptor. H3R antagonist 6 can be used as a PET radioligand for positron emission tomography imaging for central nervous system (CNS) disorders research.
    H3R antagonist 6
  • HY-121867
    KSCM-11
    KSCM-11 is a ligand of thesigma receptor.
    KSCM-11
  • HY-100930
    L-693403 maleate
    L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research.
    L-693403 maleate
  • HY-155155
    SARS-CoV-2-IN-57
    SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively.
    SARS-CoV-2-IN-57
  • HY-173475
    CM699
    		Inhibitor
    CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively.
    CM699
  • HY-121033
    BS148
    		Agonist
    BS148 is a selective sigma-2 receptor (S2R) agonist with a Ki 20 nM. BS148 shows >80-fold selective for S2R than S1R. BS148 activates the endoplasmic reticulum stress response through the upregulation of protein kinase R-like ER kinase (PERK), activating transcription factor 4 (ATF4) genes, and C/EBP homologous protein (CHOP). BS148 induces apoptosis in melanoma cell. BS148 downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. BS148 can be used for the study of melanoma.
    BS148
  • HY-116586A
    (Rac)-AF710B
    		Agonist
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    (Rac)-AF710B
Sigma Receptor Isoform Comparison

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