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-149274
    Sigma-1 receptor antagonist 4
    		Antagonist
    Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance.
    Sigma-1 receptor antagonist 4
  • HY-164010
    SUN-1334H free base
    		Inhibitor
    SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.
    SUN-1334H free base
  • HY-176405
    σ1R-IN-1
    		Inhibitor
    σ1R-IN-1 ((R,R)-1a) is a potent σ-1R inhibitor with an IC50 of 110 nM. σ1R-IN-1 is promising for research of neuropsychiatric disorders.
    σ1R-IN-1
  • HY-100966
    BD-1008 dihydrobromide
    		Antagonist 98.07%
    BD-1008 dihydrobromide is a selective sigma 1 (σ1) receptor antagonist with a Ki of 2 nM. BD-1008 dihydrobromide exhibits 4-fold selectivity over the sigma-2 receptor (Ki of 8 nM). BD-1008 dihydrobromide can be used for the study of neurological diseases.
    BD-1008 dihydrobromide
  • HY-122224
    SW43
    		Agonist
    SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.
    SW43
  • HY-116463D
    (Rac)-E1R
    		Agonist 98.48%
    (Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.
    (Rac)-E1R
  • HY-151951
    Antidepressant agent 4
    Antidepressant agent 4 is an orally active antidepressant agent. Antidepressant agent 4 exhibits antidepressant, anxiolytic, performance enhancing and nootropic activities.
    Antidepressant agent 4
  • HY-116463A
    (2R,3S)-E1R
    		Agonist 98.84%
    (2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2R,3S)-E1R
  • HY-RS12908
    SIGMAR1 Human Pre-designed siRNA Set A
    		Inhibitor

    SIGMAR1 Human Pre-designed siRNA Set A contains three designed siRNAs for SIGMAR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    SIGMAR1 Human Pre-designed siRNA Set A
  • HY-161873
    PW507
    		Antagonist
    PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN).
    PW507
  • 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 98.41%
    BD-1008 is a selective sigma 1 (σ1) receptor antagonist with a Ki of 2 nM. BD-1008 exhibits 4-fold selectivity over the sigma-2 receptor (Ki of 8 nM). BD-1008 can be used for the study of neurological diseases.
    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
Sigma Receptor Isoform Comparison

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