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 (100):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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
  • HY-101043
    4-PPBP maleate
    		Agonist 99.63%
    4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection.
    4-PPBP maleate
  • HY-116586A
    (Rac)-AF710B
    		Agonist
    (Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.
    (Rac)-AF710B
  • HY-116463B
    (2S,3S)-E1R
    		Agonist 98.24%
    (2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.
    (2S,3S)-E1R
  • HY-155614
    KSK68
    		Antagonist
    KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain.
    KSK68
  • HY-149335
    Sigma-1 receptor antagonist 5
    		Antagonist
    Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models.
    Sigma-1 receptor antagonist 5
  • HY-155615
    KSK67
    		Antagonist
    KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain.
    KSK67
  • HY-108515
    (+)-Igmesine hydrochloride
    		Agonist
    (+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ receptor ligand with neuroprotective and anti-amnesic activities.
    (+)-Igmesine hydrochloride
  • HY-163065
    σ1 Receptor/μ Opioid receptor modulator 2
    		Antagonist
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models.
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-107708
    threo-Ifenprodil hemitartrate
    		Agonist
    threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity.
    threo-Ifenprodil hemitartrate
  • HY-108511A
    PB28
    		Modulator
    PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
    PB28
  • HY-108514
    (±)-PPCC hemioxalate
    		Modulator
    (±)-PPCC hemioxalate is a compound that has the ability to regulate the activity of the sigma-1 receptor. (±)-PPCC hemioxalate can selectively bind sigma-1 protein (s1), and then activate s1 receptor leading to dissociation of s1-BIP complex to regulate ER-mitochondrial calcium signaling, which plays an important role in cell bioenergy and cell survival. (±)-PPCC hemioxalate can be used to study sigma-1 receptors in cocaine addiction, forgetting, pain, depression, Alzheimer's disease, stroke, and cancer.
    (±)-PPCC hemioxalate
  • 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-101626A
    Sigma-LIGAND-1 hydrochloride
    		99.13%
    Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor.
    Sigma-LIGAND-1 hydrochloride
  • 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-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-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)