- Signaling Pathways
- Neuronal Signaling
- Sigma Receptor
Sigma Receptor
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
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Sigma Receptor Inhibitors
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Sigma Receptor Agonists
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Sigma Receptor Antagonists
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Sigma Receptor Activators
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Sigma Receptor Modulators
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Sigma Receptor Control
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Sigma Receptor Ligands
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Sigma Receptor Related Products (192)
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Sigma Receptor Isoform Comparison
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BD-1063-d8 dihydrochloride
0 ImagesCat. No.: HY-18101SCAS No.: 1246819-69-1BD-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. -
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Umespirone
0 ImagesCat. No.: HY-123408CAS No.: 107736-98-1Synonyms: KC 9172Umespirone (KC 9172) is a potential antipsychotic/antianxiety agent. -
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Siramesine fumarate
0 ImagesCat. No.: HY-14221BCAS No.: 163630-79-3Synonyms: LU-28-179 fumarateSiramesine (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. -
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SYB4
0 ImagesCat. No.: HY-163075CAS No.: 2101953-60-8SYB4 (compound 5) is a PET tracer which suitable for imaging the Sigma-2 Receptor in the brain of nonhuman primates. -
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RC-106
0 ImagesCat. No.: HY-158197CAS No.: 1346216-50-9RC-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). -
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- AB10
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- Sigma-2 Receptor ligand 1
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- AD353
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SAS-0132
0 ImagesCat. No.: HY-119386CAS No.: 1644629-60-6SAS-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. -
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CM304
0 ImagesCat. No.: HY-129485CAS No.: 1417742-48-3Synonyms: FTC-146 hydrochlorideCM304 is a potent S1R inhibitor that can inhibit drug-induced convulsions in rats. -
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KSK94
0 ImagesCat. No.: HY-155616CAS No.: 2566716-07-0KSK94 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. -
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σ1 Receptor/μ Opioid receptor modulator 1
0 ImagesCat. No.: HY-147560CAS No.: 2412700-00-4σ1 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. -
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EST64454
0 ImagesCat. No.: HY-131914CAS No.: 1351438-26-0EST64454 (compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki 22 nM. EST64454 can be used to study pain. -
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H3R antagonist 6
0 ImagesCat. No.: HY-175367CAS No.: 2183338-59-0H3R 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. -
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KSCM-11
0 ImagesCat. No.: HY-121867CAS No.: 1415247-16-3KSCM-11 is a ligand of thesigma receptor. -
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L-693403 maleate
0 ImagesCat. No.: HY-100930CAS No.: 207455-21-8L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research. -
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SARS-CoV-2-IN-57
0 ImagesCat. No.: HY-155155CAS No.: 1265624-68-7SARS-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. -
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CM699
0 ImagesCat. No.: HY-173475CAS No.: 1259949-84-2CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively. -
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BS148
0 ImagesCat. No.: HY-121033CAS No.: 2162116-09-6BS148 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. -
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(Rac)-AF710B
0 ImagesCat. No.: HY-116586ACAS No.: 1235733-73-9 -
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