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-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
  • HY-13575R
    Blonanserin (Standard)
    		Antagonist
    Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin (Standard)
  • HY-118901S
    Opipramol-d4
    Opipramol-d4 is the deuterium labeled Opipramol[1].
    Opipramol-d<sub>4</sub>
  • HY-A0139
    Thiothixene
    		Antagonist
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • HY-14895
    Fabomotizole
    		Inhibitor 99.96%
    Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects.
    Fabomotizole
  • HY-134004R
    Pentoxyverine (Standard)
    		Agonist
    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.
    Pentoxyverine (Standard)
  • HY-100966
    BD-1008 dihydrobromide
    		Antagonist 98.07%
    BD-1008 dihydrobromide is an antagonist of sigma Receptor.
    BD-1008 dihydrobromide
  • HY-101484AR
    NE-100 hydrochloride (Standard)
    		Antagonist
    NE-100 (hydrochloride) (Standard) is the analytical standard of NE-100 (hydrochloride). This product is intended for research and analytical applications. NE-100 (hydrochloride) is a potent and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 (hydrochloride) exerts antipsychotic activity in vivo. NE-100 (hydrochloride) also suppresses ER stress-induced hippocampal cell death.
    NE-100 hydrochloride (Standard)
  • HY-B2087R
    Glycerol phenylbutyrate (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.
    Glycerol phenylbutyrate (Standard)
  • HY-155484
    SOMCL-668
    		Modulator
    SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research.
    SOMCL-668
  • HY-W714837
    5-Phenyllevulinic acid
    5-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 .
    5-Phenyllevulinic acid
  • HY-B1216R
    Oxeladin (citrate) (Standard)
    		Agonist
    Oxeladin (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.
    Oxeladin (citrate) (Standard)
Sigma Receptor Isoform Comparison

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