Sigma Receptor
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
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Sigma Receptor Inhibitors
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Sigma Receptor Agonists
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Sigma Receptor Antagonists
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Sigma Receptor Activators
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Sigma Receptor Modulators
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Sigma Receptor Control
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Sigma Receptor Ligands
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Sigma Receptor Related Products (196)
Related Products (196)
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Sigma Receptor Isoform Comparison
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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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WLB-87848
0 ImagesCat. No.: HY-158693CAS No.: 2839205-09-1WLB-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.
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Pentoxyverine citrate (Standard)
0 ImagesSynonyms: Carbetapentane citrate (Standard)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].
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(±)-PPCC oxalate
0 ImagesCat. No.: HY-111081CCAS No.: 1781628-91-8(±)-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.
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Captodiame
0 ImagesCaptodiame (Captodiamine) is a 5-HT2c receptor antagonist and sigma-1 and D3 dopamine receptor agonist. Captodiame shows antidepressant effect.
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Sigma-2 Radioligand 1
0 ImagesCat. No.: HY-156124CAS No.: 2860554-32-9Sigma-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.
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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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CB-184
0 ImagesCat. No.: HY-14220CAS No.: 165307-47-1CB-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.
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S1R agonist 2 hydrochloride
0 ImagesCat. No.: HY-149804APurity: ≥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.
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BD-1047
0 ImagesCat. No.: HY-16996CAS No.: 138356-20-4BD-1047 is a selective functional antagonist of sigma receptors. BD-1047 attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.
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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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KOR agonist 7
0 ImagesCat. No.: HY-178945KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.
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EST73502
0 ImagesCat. No.: HY-134189CAS No.: 1838622-25-5EST73502 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.
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AF710B
0 ImagesCat. No.: HY-116586AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease.
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CM572
0 ImagesCat. No.: HY-122112CAS No.: 1121932-91-9CM572 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.
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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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PRE-084
0 ImagesCat. No.: HY-18100CAS No.: 138847-85-5PRE-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.
