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

Sigma Receptor

Sigma Receptor

Related Products

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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 Related Products (88):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-125819
    Sigma-1 receptor antagonist 2
    		Antagonist 99.14%
    Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively.
    Sigma-1 receptor antagonist 2
  • HY-153091
    BMY 14802
    		Antagonist 98.96%
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM.
    BMY 14802
  • HY-136281
    DuP 734
    		Antagonist 98.82%
    DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.
    DuP 734
  • HY-116594
    OPC-14523 free base
    		Agonist
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
    OPC-14523 free base
  • HY-116594A
    OPC-14523 hydrochloride
    		Inhibitor 99.90%
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
    OPC-14523 hydrochloride
  • HY-131914A
    EST64454 hydrochloride
    		Inhibitor 99.19%
    EST64454 hydrochloride is a selective and orally active sigma-1 receptor antagonist with a Ki of 22 nM. EST64454 hydrochloride has the potential for the research of the pain.
    EST64454 hydrochloride
  • HY-116463
    E1R
    		Agonist 99.28%
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
    E1R
  • HY-14813
    Cutamesine
    		Agonist
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
    Cutamesine
  • HY-13751A
    SR-31747 free base
    SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
    SR-31747 free base
  • HY-105296
    Blarcamesine
    		Agonist 99.51%
    Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
    Blarcamesine
  • HY-13575A
    Blonanserin dihydrochloride
    		Antagonist
    Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin dihydrochloride
  • HY-14221B
    Siramesine fumarate
    		Agonist
    Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.
    Siramesine fumarate
  • HY-149855
    AB10
    		Antagonist
    AB10 is a selective S1R antagonist. AB10 with Ki of 10, 165 nM for S1R and S2R, respectively. AB10 reverses the effect of Capsaicin (HY-10448) caused pain in model.
    AB10
  • HY-149803
    S1R agonist 1
    		Agonist ≥98.0%
    S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 1
  • HY-155616
    KSK94
    		Antagonist
    KSK94 is a high-affinity histamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain.
    KSK94
  • HY-147560
    σ1 Receptor/μ Opioid receptor modulator 1
    		Antagonist
    σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain.
    σ1 Receptor/μ Opioid receptor modulator 1
  • HY-47228
    KB-5492 free base
    		Inhibitor 99.06%
    KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent.
    KB-5492 free base
  • HY-100930
    L-693403 maleate
    L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research.
    L-693403 maleate
  • HY-149803A
    S1R agonist 1 hydrochloride
    		Agonist 99.83%
    S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.
    S1R agonist 1 hydrochloride
  • HY-155155
    SARS-CoV-2-IN-57
    SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively.
    SARS-CoV-2-IN-57