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 (196)
Related Products (196)
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Sigma Receptor Isoform Comparison
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Chlophedianol hydrochloride (Standard)
0 ImagesCat. No.: HY-A0161ARCAS No.: 511-13-7Synonyms: Clofedanol hydrochloride (Standard); Calmotusin hydrochloride (Standard); NSC 113595 hydrochloride (Standard)Chlophedianol (hydrochloride) (Standard) is the analytical standard of Chlophedianol (hydrochloride). This product is intended for research and analytical applications. Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs).
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Pentoxyverine (Standard)
0 ImagesSynonyms: Carbetapentane (Standard)Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
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NE-100 hydrochloride (Standard)
0 ImagesCat. No.: HY-101484ARCAS No.: 149409-57-4NE-100 hydrochloride (Standard) is the analytical standard of NE-100 hydrochloride (HY-101484A). This product is intended for research and analytical applications. NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases.
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Glycerol phenylbutyrate (Standard)
0 ImagesCat. No.: HY-B2087RCAS No.: 611168-24-2Synonyms: HPN-100 (Standard)Glycerol phenylbutyrate (Standard) is the analytical standard of Glycerol phenylbutyrate. This product is intended for research and analytical applications. Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent.
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PB28 dihydrochloride (Standard)
0 ImagesCat. No.: HY-108511RCAS No.: 172907-03-8PB28 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.
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Igmesine
0 ImagesCat. No.: HY-169914ACAS No.: 140850-73-3Synonyms: JO 1784Igmesine (JO 1784) is a selective σ-1 receptor agonist (IC50 = 39 nM) with oral activity and blood-brain barrier penetration. Igmesine stimulates duodenal bicarbonate secretion in rats via a σ1/vagal/CCK-A-dependent pathway, without antisecretory activity. Igmesine centrally blocks CRF-mediated gastrin-inhibitory effects, and in TMT toxicity and MCAO focal ischemia models, it downregulates PTBBS, reduces NOS, and modulates M1/M2 density. Igmesine is used in research on duodenal ulcers, Alzheimer's disease, and related diseases.
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5-Phenyllevulinic acid
0 ImagesCat. No.: HY-W714837CAS No.: 3183-15-1Synonyms: 4-Oxo-5-phenylpentanoic acid; 5-Phenyl-4-oxopentanoic acid5-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 .
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Oxeladin citrate (Standard)
0 ImagesCat. No.: HY-B1216RCAS No.: 52432-72-1Oxeladin (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.
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SV119 hydrochloride
0 ImagesCat. No.: HY-177345ACAS No.: 913816-12-3SV119 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.
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RTI-371
0 ImagesCat. No.: HY-129215CAS No.: 652978-45-5RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC50 = 8.7 nM) and shows high binding affinity for rat DAT with a Ki value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.
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Sigma-2 Radioligand 2
0 ImagesCat. No.: HY-169185CAS No.: 2860554-31-8Sigma-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.
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Cutamesine dihydrochloride (Standard)
0 ImagesSynonyms: SA4503 dihydrochloride (Standard); AGY94806 dihydrochloride (Standard)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.
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Sigma ligand-1 (Standard)
0 ImagesCat. No.: HY-101626RCAS No.: 139652-01-0Sigma 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.
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σ1 Receptor antagonist 4
0 ImagesCat. No.: HY-108513CAS No.: 362512-81-0σ1 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.
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Sigma ligand-1 hydrochloride (Standard)
0 ImagesCat. No.: HY-101626ARCAS No.: 139652-86-1Sigma 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.
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Opipramol (Standard)
0 ImagesCat. No.: HY-118901RCAS No.: 315-72-0Synonyms: Ensidon (Standard); G-33040 (Standard)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).
