2. Signaling Pathways
  3. Neuronal Signaling
  4. Sigma Receptor

Sigma Receptor

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-117420
    CM764
    		Activator
    CM764 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.
    CM764
  • HY-135608
    BD-1008
    		Antagonist
    BD-1008 is a selective antagonist of the sigma receptors, demonstrating a binding affinity of K? = 2 ± 1 nM for the sigma-1 receptor and exhibiting fourfold selectivity over the sigma-2 receptor.
    BD-1008
  • HY-149854A
    AB21 oxalate
    		Antagonist
    AB21 oxalate is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 oxalate has the effect of reducing mechanical hypersensitivity.
    AB21 oxalate
  • HY-116463C
    (2R,3R)-E1R
    		Agonist 98.79%
    (2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2R,3R)-E1R
  • HY-118901A
    Opipramol dihydrochloride
    		Antagonist
    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).
    Opipramol dihydrochloride
  • HY-120360
    CB-64D
    		Agonist
    CB-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.
    CB-64D
  • HY-119196
    Caprospinol
    		Ligand
    Caprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.
    Caprospinol
  • HY-149854
    AB21
    		Antagonist
    AB21 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.
    AB21
  • HY-151950
    Antidepressant agent 3
    Antidepressant agent 3 is an orally active antidepressant agent. Antidepressant agent 3 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 3
  • HY-158693
    WLB-87848
    		Agonist
    WLB-87848 is a selective, orally active, and blood-brain barrier (BBB) permeable σ1 receptor agonist with the Ki of 9 nM. WLB-87848 rescues recognition memory impairment.
    WLB-87848
  • HY-B1055R
    Pentoxyverine (citrate) (Standard)
    		Agonist
    Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate 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 membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[4].
    Pentoxyverine (citrate) (Standard)
  • HY-111081C
    (±)-PPCC oxalate
    		Agonist
    (±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.
    (±)-PPCC oxalate
  • HY-14222
    UMB24
    		Antagonist
    UMB24 is a potent antagonist of σ2 receptor, with Ki values of 170 nM anf 322 nM for σ2 receptor and σ1 receptor, respectively. UMB24 attenuats cocaine-induced convulsions and locomotor activity, but not lethality.
    UMB24
  • HY-117731
    UKH-1114
    		Agonist
    UKH-1114 is a potent σ2 receptor/Tmem97 agonist with a Ki value of 46 nM, showing antimechanical hypersensitivity effects. UKH-1114 alleviates mechanical hypersensitivity caused by nerve injury without any movement disorders in mice. UKH-1114 is promising for research of neuropathic pain.
    UKH-1114
  • HY-156124
    Sigma-2 Radioligand 1
    Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts.
    Sigma-2 Radioligand 1
  • HY-B0765R
    Dehydroepiandrosterone sulfate sodium (Standard)
    		Activator
    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.
    Dehydroepiandrosterone sulfate sodium (Standard)
  • HY-14220
    CB-184
    CB-184 is a selective ligand for sigma-2 (σ2), with Ki values of 7436 nM for σ1 and 13.4 nM for σ2. CB-184 promotes apoptosis and has antitumor activity.
    CB-184
  • HY-149804A
    S1R agonist 2 hydrochloride
    		Agonist ≥98.0%
    S1R agonist 2 (Compound 8b) hydrochloride is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 2 hydrochloride
  • HY-16996
    BD-1047
    		Antagonist
    BD-1047 is a selective functional antagonist of sigma receptors. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.
    BD-1047
  • HY-134189
    EST73502
    		Antagonist
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
    EST73502
Sigma Receptor Isoform Comparison

Sigma 1 Receptor

Sigma 2 Receptor

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Please try each isoform separately.

Sigma Receptor Inhibitors, Agonists, Antagonists, Activators & Modulators
Product NameSigma 1 ReceptorSigma 2 ReceptorPurity    
BD-1047 dihydrobromide
Sigma 1 Receptor
 98.17%
PRE-084 hydrochloride
Sigma 1 Receptor
 99.92%
Dehydroepiandrosterone sulfate
Sigma 1 Receptor
 99.93%
Siramesine hydrochloride
Sigma 1 Receptor
 99.74%
Dehydroepiandrosterone sulfate sodium
Sigma 1 Receptor
 99.96%
σ1 Receptor ligand 1
σ1, Ki: 3.9 nM
 
Cutamesine dihydrochloride
Sigma 1 Receptor, IC50: 17.4 nM
Sigma 2 Receptor, IC50: 1784 nM
98.01%
(±)-Vesamicol hydrochloride
Sigma 1 Receptor
Sigma 2 Receptor
99.81%
CT1812 
Sigma 2 Receptor
Blarcamesine hydrochloride
Sigma 1 Receptor
 99.87%
S1RA hydrochloride
Sigma 1 Receptor
 99.94%
Glycerol phenylbutyrate 
Sigma 2 Receptor
99.81%
Dimemorfan phosphate
Sigma 1 Receptor
 99.87%
BD1063 dhydrochloride
Sigma 1 Receptor
 ≥98.0%
σ1 Receptor antagonist-1
Sigma 1 Receptor
 99.87%
SKF 83959
Sigma 1 Receptor
 98.94%
S1RA
human σ1R, Ki: 17 nM
guinea pig σ1R, Ki: 23.5 nM
guinea pig σ2R, Ki: >1000 nM
rat σ2R, Ki: 9300 nM
99.43%
Pentoxyverine citrate
σ1, Ki: 41 nM
σ2, Ki: 894 nM
99.57%
Ditolylguanidine
Sigma 1 Receptor
Sigma 2 Receptor
99.66%
Pentoxyverine
σ1, Ki: 41 nM
σ2, Ki: 894 nM
98.91%
Blarcamesine
Sigma 1 Receptor
 99.51%
Sigma-1 receptor antagonist 1
Sigma 1 Receptor
 98.64%
Dehydroepiandrosterone sulfate-d6 sodium dihydrate
Sigma 1 Receptor
 98.00%
Dehydroepiandrosterone sulfate (Standard)
Sigma 1 Receptor
 
Sigma-1 receptor antagonist 2
Sigma 1 Receptor
 99.76%
BMY 14802
Sigma 1 Receptor
 98.96%
E1R
Sigma 1 Receptor
 99.83%
S1R agonist 2
Sigma 1 Receptor, Ki: 1.1 nM
Sigma 2 Receptor, Ki: 88 nM
≥98.0%
Dehydroepiandrosterone sulfate sodium-d6
Sigma 1 Receptor
 99.61%
Cutamesine
Sigma 1 Receptor, IC50: 17.4 nM
Sigma 2 Receptor, IC50: 1784 nM
4-IBP
Sigma 1 Receptor
Sigma 2 Receptor
98.90%
S1R agonist 1
Sigma 1 Receptor, Ki: 0.93 nM
Sigma 2 Receptor, Ki: 72 nM
≥98.0%
Sigma-1 receptor antagonist 3
Sigma 1 Receptor
 99.47%
Siramesine
Sigma 1 Receptor
 
AB10
Sigma 1 Receptor, Ki: 10 nM
Sigma 2 Receptor, Ki: 165 nM
EST64454
σ1R, Ki: 22 nM
 
SUN-1334H free base
σ1, IC50: 5.46 μM
 
CM764
Sigma 1 Receptor, Ki: 86.6 nM
Sigma 2 Receptor, Ki: 3.5 nM
CB-64D
Sigma 1 Receptor, Ki: 3063 nM
Sigma 2 Receptor, Ki: 16.5 nM
AB21
Sigma 1 Receptor, Ki: 13 nM
Sigma 2 Receptor, Ki: 102 nM
UMB24
σ1, Ki: 322 nM
σ2, Ki: 170 nM
Dehydroepiandrosterone sulfate sodium (Standard)
Sigma 1 Receptor
 
Phenyltoloxamine
Sigma 1 Receptor, Ki: 160 nM
 
AD186
Sigma 1 Receptor, Ki: 2.7 nM
Sigma 2 Receptor, Ki: 27 nM
SW116 free base
Sigma 1 Receptor, Ki: 1055 nM
Sigma 2 Receptor, Ki: 14 nM
KSCM-1
Sigma 1 Receptor, Ki: 27.5 nM
Sigma 2 Receptor, Ki: 528 nM
Fabomotizole
Sigma 1 Receptor
 99.96%
σ1 Receptor antagonist 4
σ1R, Ki: 10 nM
σ2, Ki: 370 nM