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Sigma Receptor

Sigma Receptor

Sigma receptors (subtypes sigma-1 and sigma-2) are a unique class of binding sites expressed throughout the mammalian body.Although the natural ligand for these sites is unknown, steroid hormones—especially progesterone—amines derived from sphingolipids, and N,N-dimethyltryptamine—all have a relatively high affinity for binding.

The sigma-1 receptor (σ1R) is a chaperone protein that resides in the endoplasmic reticulum (ER) and functions as an inter-organelle signaling modulator. Numerous biological processes are impacted by it, such as nociception, drug addiction, cardiac activity, cancer, stroke, memory, and Alzheimer's disease. Numerous human tumors exhibit overexpression of the sigma-2 (σ2R) receptor. Its status as a proliferating tumor biomarker has been confirmed.

Sigma Receptor related products

Structure Cat No. Product Name CAS No. Product Description
(±)-PPCC V93275 (±)-PPCC 932736-90-8 (±)-PPCC is a sigma-1 agonist that primarily interacts with the sigma-1 receptor with a Ki of 1.5 nM.
(±)-PPCC hemioxalate V87843 (±)-PPCC hemioxalate 932736-91-9 (±)-PPCC hemioxalate is a compound with sigma-1 receptor modulatory activity.
AB21 hydrochloride V87845 AB21 hydrochloride 3026677-24-4 AB21 hydrochloride is a potent and selective S1R antagonist with Ki values of 13 nM and 102 nM for S1R and S2R, respectively.
AD353 V103727 AD353 AD353 is a selective sigma-1 receptor ligand.
Anavex2-73 HCl V7110 Anavex2-73 HCl 195615-84-0 Anavex2-73 (Anavex-273; AE-37) HCl is a novel and potent muscarinic/σ1 ( Sigma-1) ligand/agonist (IC50 = 860 nM) with therapeutic potential for treating Alzheimer's disease.
BD-1047 V129953 BD-1047 138356-20-4 BD-1047 is a selective sigma receptor antagonist.
BS148 V116166 BS148 2162116-09-6 BS148 is a selective σ-2 receptor (S2R) agonist with a Ki value of 20 nM.
CM304 free base V108977 CM304 free base 1350296-21-7 CM304 free base (FTC-146) is a potent S1R antagonist.
EST64454 V94242 EST64454 1351438-26-0 EST64454 (Compound 9k) is a selective, orally active sigma-1 receptor antagonist with Ki of 22 nM.
H3R antagonist 6 V137058 H3R antagonist 6 2183338-59-0 H3R antagonist 6 is a histamine receptor 3 (H3R) antagonist with an IC50 value of 5.6 nM.
MS-377 V116204 MS-377 206862-30-8 MS-377 is a selective, orally effective σ-1 receptor ligand (Ki = 73 nM), with a weak affinity for σ-2 receptors (Ki = 6900 nM), and no affinity for other receptors (including dopamine receptors, serotonin receptors, PCP receptors, glutamate receptors, γ-aminobutyric acid receptors, adenosine receptors, and adrenaline receptors) (Ki > 10 μM).
NMDA receptor antagonist 9 V141437 NMDA receptor antagonist 9 NMDA receptor antagonist 9 is a selective GluN2B subunit NMDA receptor antagonist with a Ki value of 5.2 nM.
Opipramol dihydrochloride V102730 Opipramol dihydrochloride 909-39-7 Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA).
PW507 V89040 PW507 2573850-59-4 PW507 is a potent, blood-brain permeable and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R.
RC-106 V87694 RC-106 1346216-50-9 RC-106 is a proteasome inhibitor (IC50: 35 μM) and Sigma receptor modulator with anticancer activity.
S1R agonist 3 V144465 S1R agonist 3 401501-66-4 S1R agonist 3 is a highly potent, selective, and blood-brain barrier-penetrating σ-1 receptor (S1R) agonist with a Ki value of 1.5 nM.
S1R agonist/BChE-IN-1 V110368 S1R agonist/BChE-IN-1 S1R agonist/BChE-IN-1 (compound 7c) is an S1R agonist (IC50: 19 nM) and a selective BChE inhibitor (IC50 for human BChE: 37 nM).
SAS-0132 V115296 SAS-0132 2095551-89-4 SAS-0132 is a selective, blood-brain barrier-crossing Sigma 2 receptor (Sig2R) antagonist (Ki: 90 nM).
SAS-1121 V115989 SAS-1121 2095551-67-8 SAS-1121 is a subtype-selective α2 receptor/PGRMC1 ligand with a Ki value of 16.2 nM.
Sigma-1 receptor antagonist 6 V98949 Sigma-1 receptor antagonist 6 1335032-28-4 Sigma-1 receptor antagonist 6 (Compound 12) is a Sigma-1 receptor (σ1R) antagonist.
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