1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Sigma Receptor

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 Related Products (42):

Cat. No. Product Name Effect Purity
  • HY-16996A
    BD-1047 dihydrobromide Antagonist 99.78%
    BD-1047 (dihydrobromide) is a selective functional antagonist of sigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
  • HY-18100A
    PRE-084 hydrochloride Agonist 99.80%
    PRE-084 hydrochloride is a high affinity, selective σ1 agonist, has an IC50 of 44 nM in the sigma receptor assay.
  • HY-B2215
    Dimemorfan phosphate Agonist 99.87%
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
  • HY-13510
    Cutamesine dihydrochloride Agonist 99.48%
    Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
  • HY-14221A
    Siramesine hydrochloride Agonist 99.85%
    Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
  • HY-134189A
    EST73502 hydrochloride Antagonist 98.12%
    EST73502 hydrochloride 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 hydrochloride has antinociceptive activity.
  • 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.
  • HY-134189
    EST73502 Antagonist
    EST73502 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.
  • HY-101864
    Blarcamesine hydrochloride Agonist 99.85%
    Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
  • HY-B2087
    Glycerol phenylbutyrate 99.81%
    Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger drug.
  • HY-18101A
    BD1063 dhydrochloride Antagonist >98.0%
    BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.
  • HY-18099A
    S1RA hydrochloride Antagonist 99.24%
    S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
  • HY-13751
    SR-31747 99.80%
    SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
  • HY-13575
    Blonanserin Antagonist 99.77%
    Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
  • HY-111669
    Sigma-2 receptor antagonist 1 Antagonist
    Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.
  • HY-19469
    Roluperidone 98.08%
    Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
  • HY-14218
    Ditolylguanidine Agonist 99.26%
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
  • 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.
  • HY-100155
    4-IBP Agonist 99.81%
    4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
  • HY-125821
    Sigma-1 receptor antagonist 1 Antagonist 99.76%
    Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain.
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