Sigma 1 Receptor
Sigma-1 receptor (σ1R) is an ER-localized chaperone that regulates Ca2+ signaling and cell survival at the ER-mitochondrion interface[1]. Mechanistically, σ1R stabilizes IRE1 at mitochondrion-associated ER membranes during ER stress, supporting mitochondrion-ER-nucleus survival signaling[2]. In disease-relevant models, σ1R ligands are used to test neuroprotection, ER stress responses, and neuropathic pain mechanisms[3][4]. Compared with the related sigma-2 receptor, σ1R is distinct because sigma-2 was identified as TMEM97, a membrane protein linked to NPC1 binding and cancer biology[5]. For experimental applications, agonists such as PRE-084 support selective σ1R activation studies, whereas antagonists including E-52862 support neuropathic pain model design[3][4].
References:
- [1]. Hayashi T, et al. Sigma-1 receptor chaperones at the ER-mitochondrion interface regulate Ca(2+) signaling and cell survival. Cell. 2007 Nov 2;131(3):596-610. [Content Brief]
- [2]. Mori T, et al. Sigma-1 receptor chaperone at the ER-mitochondrion interface mediates the mitochondrion-ER-nucleus signaling for cellular survival. PLoS One. 2013 Oct 18;8(10):e76941. [Content Brief]
- [3]. Motawe ZY, et al. PRE-084 as a tool to uncover potential therapeutic applications for selective sigma-1 receptor activation. Int J Biochem Cell Biol. 2020 Sep;126:105803. [Content Brief]
- [4]. Gris G, et al. The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats. Sci Rep. 2016 Apr 18;6:24591. [Content Brief]
- [5]. Alon A, et al. Identification of the gene that codes for the σ2 receptor. Proc Natl Acad Sci U S A. 2017 Jul 3;114(27):7160-7165. [Content Brief]
All Product Categories
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Sigma 1 Receptor Related Products (70)
Related Products (70)
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S1R agonist 2
0 ImagesS1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
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NMDA receptor antagonist 9
0 ImagesCat. No.: HY-181007NMDA receptor antagonist 9 is a selective GluN2B subunit-containing NMDA receptor antagonist with a Ki of 5.2 nM. NMDA receptor antagonist 9 exhibits 9-fold selectivity over σ1 receptors, shows poor selectivity towards σ2 receptors. NMDA receptor antagonist 9 inhibits ion flux through GluN2B subunit-containing NMDA receptors. NMDA receptor antagonist 9 can be used for the research of neurological disease, such as alzheimer’s disease and parkinson’s disease.
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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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σ1R/H3R ligand-1
0 ImagesCat. No.: HY-181722σ1R/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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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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S1R agonist/BChE-IN-1
0 ImagesCat. No.: HY-180797S1R agonist/BChE-IN-1 (Compound 7c) is a S1R (IC50: 19 nM) agonist and selective BChE (IC50: 37 nM for hBChE) inhibitor. S1R agonist/BChE-IN-1 can be used in the research of Alzheimer's disease.
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Oxeladin
0 ImagesOxeladin 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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σ1 Receptor ligand 1
0 ImagesCat. No.: HY-168562σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research.
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SUN-1334H free base
0 ImagesCat. No.: HY-164010CAS No.: 607737-00-8SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.
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CM304 free base
0 ImagesCat. No.: HY-129485ACAS No.: 1350296-21-7Synonyms: FTC-146CM304 free base (FTC-146) is a potent S1R antagonist. CM304 free base enhances the antinociceptive effects of the cannabinoid receptor agonists. CM304 free base inhibits convulsions in rats.
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CM764
0 ImagesCat. No.: HY-117420CAS No.: 1350296-29-5CM764 is an activator for sigma receptor with Ki of 86.6 and 3.5 nM for sigma-1 receptor and sigma-2 receptor. CM764 increases cytoplasmic calcium, NAD+/NADH, and ATP levels, and decreases the concentration of ROS.
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Sigma-1 receptor antagonist 7
0 ImagesCat. No.: HY-187185CAS No.: 3050643-44-9Sigma-1 receptor antagonist 7 is a selective sigma-1 receptor antagonist capable of crossing the blood-brain barrier, with an IC50 of 12.7 nM against guinea pig σ1R. Sigma-1 receptor antagonist 7 binds to σ1R, and its binding affinity decreases in the presence of Phenytoin (HY-B0448). Sigma-1 receptor antagonist 7 alleviates mechanical and thermal hyperalgesia induced by acute inflammation in rats. Sigma-1 receptor antagonist 7 can be used for research related to hyperalgesia.
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CB-64D
0 ImagesCat. No.: HY-120360CAS No.: 157752-20-0CB-64D is the agonist for sigma receptor 2 and sigma receptor 1 with Ki of 16.5 and 3063 nM. CB-64D induces apoptosis in cancer cell SK-N-SH.
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E-5842 citrate
0 ImagesCat. No.: HY-106153BCAS No.: 220120-14-9E-5842 citrate is a σ receptor ligand (Ki: 4 nM for σ1 receptor). E-5842 citrate increases levels of Fos in the medial prefrontal cortex and the nucleus accumbens, without affecting the levels of the protein in the striatum. E-5842 citrate can be used in the research of psychiatric disorders.
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AB21
0 ImagesCat. No.: HY-149854CAS No.: 3026677-23-3AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 has the effect of reducing mechanical hypersensitivity.
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Dehydroepiandrosterone sulfate sodium (Standard)
0 ImagesSynonyms: DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt (Standard) is the analytical standard of Dehydroepiandrosterone sulfate sodium salt (HY-B0765). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
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MS-377
0 ImagesCat. No.: HY-120155CAS No.: 206862-30-8MS-377 is a selective and orally active sigma-1 receptor ligand (Ki=73 nM) with weak affinity for sigma-2 receptor (Ki=6900 nM) and no affinity for any other receptors including dopamine, serotonin, PCP site, glutamate, γ-aminobutylic acid, adenosine, adrenergic receptors, etc. (Ki: >10 μM). MS-377 indirectly modulates the NMDA receptor ion-channel complex. MS-377 is a antipsychotic agent. MS-377 inhibits PCP-induced behaviors by inhibition of the increase in dopamine and serotonin release in the rat medial prefrontal cortex. MS-377 can be used for research of schizophrenia.
