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 (71)
Related Products (71)
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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.
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JVW-1009
0 ImagesCat. No.: HY-116968CAS No.: 2089059-30-1JVW-1009 is a Sig2R/PGRMC1 antagonist (Sig1R Ki = 96 nM; Sig2R Ki = 70 nM). JVW-1009 acts as a neuroprotective agent. JVW-1009 can be used in the research of Alzheimer's disease.
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SW116 free base
0 ImagesCat. No.: HY-120421CAS No.: 1036759-00-8SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research.
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KSCM-1
0 ImagesCat. No.: HY-118279CAS No.: 1415247-17-4KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors.
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BD-1063
0 ImagesCat. No.: HY-18101CAS No.: 150208-28-9BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 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 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.
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Convolamine hydrochloride
0 ImagesCat. No.: HY-N15339ACAS No.: 5896-59-3Convolamine hydrochloride is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC50 value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease.
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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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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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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.
