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 (26):

Cat. No. Product Name Effect Purity
  • HY-13980
    UNC0642 Inhibitor 99.81%
    UNC0642 is a potent and selective G9a/GLP inhibitor, with an IC50 of less than 2.5 nM.
  • HY-16996A
    BD-1047 dihydrobromide Antagonist 98.18%
    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 98.74%
    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-13716
    Noscapine Activator
    Noscapine is an orally administrable drug used worldwide for cough suppression, primarily mediated by its σ-receptor agonist activity, and possess anticancer activity.
  • HY-125820
    Sigma-1 receptor antagonist 3 Antagonist
    Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (σ1) receptor antagonist with a Ki of 1.14 nM. Sigma-1 receptor antagonist 3 inhibits Human Ether-a-go-go-Related Gene (hERG) with an IC50 of 1.54 μM. Sigma-1 receptor antagonist 3 is for treating neuropathic pain.
  • HY-125819
    Sigma-1 receptor antagonist 2 Antagonist
    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.
  • 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.
  • 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-18101A
    BD1063 dhydrochloride Antagonist >98.0%
    BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.
  • HY-101864
    AVex-73 hydrochloride Agonist 99.72%
    AVex-73 hydrochloride is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
  • HY-19469
    Roluperidone 98.26%
    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-B2215
    Dimemorfan phosphate Agonist 98.42%
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
  • HY-100155
    4-IBP Agonist 98.90%
    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-14218
    Ditolylguanidine Agonist 99.26%
    Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).
  • HY-116463
    E1R Agonist 99.28%
    E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.
  • 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-14813
    Cutamesine Agonist
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  • HY-111669
    Sigma-2 receptor antagonist 1 Antagonist
    Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.
  • HY-116463B
    (2S,3S)-E1R Agonist
    (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.
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