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

Sigma Receptor

Sigma receptor is a non-opioid receptor that binds diverse classes of psychotropic drugs. Sigma receptors are subdivided into two subtypes, sigma-1 and sigma-2. The sigma-1 receptor is a 25-kDa protein possessing one putative transmembrane domain and an endoplasmic reticulum retention signal. Sigma-1 receptors are highly expressed in deeper laminae of the cortex, olfactory bulb, nuclei of mesencephalon, hypothalamus, and Purkinje cells in the brain. Sigma-1 receptors are predominantly localized at the endoplasmic reticulum of both neurons and oligodendrocytes. From behavioral studies, sigma-1 receptors were shown to be involved in higher-ordered brain functions including memory and drug dependence. The sigma-2 receptor (σ2R) is a sigma receptor subtype which preferentially binds to siramesine and PB28. PGRMC1 was recently identified as the sigma-2 receptor. Unlike sigma-1 receptor, it has not yet been cloned. Activation of the receptor can cause apoptosis. A pharmacophore model based on benzooxazolone derivatives has been developed.

Sigma Receptor Related Products (39):

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-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-B2215
    Dimemorfan phosphate Agonist 99.51%
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
  • HY-108512A
    PD 144418 oxalate >98.0%
    PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.
  • HY-19120
    KB-5492 anhydrous Inhibitor 99.50%
    KB-5492 anhydrous 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 anhydrous is an anti-ulcer agent.
  • HY-136280
    Panamesine 99.74%
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent.
  • 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-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-101864
    Blarcamesine hydrochloride Agonist 99.85%
    Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
  • 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-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-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-111669
    Sigma-2 receptor antagonist 1 Antagonist
    Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.
  • 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-14218
    Ditolylguanidine Agonist 99.26%
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
  • 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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