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

Sigma 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-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-A0172
    Captodiame
    		Agonist
    Captodiame (Captodiamine) is a 5-HT2c receptor antagonist and sigma-1 and D3 dopamine receptor agonist. Captodiame shows antidepressant effect.
    Captodiame
  • 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
  • HY-122112
    CM572
    		Agonist
    CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer.
    CM572
  • HY-B1733
    Phenyltoloxamine
    		Modulator
    Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM).
    Phenyltoloxamine
  • HY-18100
    PRE-084
    		Agonist
    PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
    PRE-084
  • HY-149853
    AD186
    		Agonist
    AD186 is a potent and selective S1R agonist with Kis of 2.7, 27 nM for S1R and S2R, respectively. AD186 fully reverses the antiallodynic effect of BD-1063 (HY-18101A).
    AD186
  • HY-120421
    SW116 free base
    SW116 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.
    SW116 free base
  • HY-111081
    (±)-PPCC
    		Agonist
    (±)-PPCC is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.
    (±)-PPCC
  • HY-118279
    KSCM-1
    KSCM-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.
    KSCM-1
  • HY-129485
    CM304
    		Antagonist
    CM304 is a potent S1R inhibitor that can inhibit drug-induced convulsions in rats.
    CM304
  • HY-N15339
    Convolamine
    		Modulator
    Convolamine is an alkaloid found in Convolvulus pluricaulis and an effective positive modulator of the sigma-1 receptor (IC50 = 289 nM), exhibiting cognitive and neuroprotective properties.
    Convolamine
Sigma Receptor Isoform Comparison

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