1. Signaling Pathways
  2. 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 (61):

Cat. No. Product Name Effect Purity
  • HY-18100A
    PRE-084 hydrochloride
    Agonist 99.79%
    PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
  • 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-101864
    Blarcamesine hydrochloride
    Agonist 99.85%
    Blarcamesine hydrochloride is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
  • HY-B2215
    Dimemorfan phosphate
    Agonist 99.97%
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
  • 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-118901
    Opipramol
    Antagonist
    Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD).
  • 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.
  • 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.
  • HY-14221A
    Siramesine hydrochloride
    Agonist 99.74%
    Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride 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 hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.
  • HY-18099A
    S1RA hydrochloride
    Antagonist 99.85%
    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-13510
    Cutamesine dihydrochloride
    Agonist 98.01%
    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-111669
    CT1812
    Antagonist
    CT1812 (Sigma-2 receptor antagonist 1) is a sigma-2 (σ-2) receptor antagonist.
  • HY-19469
    Roluperidone
    99.91%
    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-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-18101A
    BD1063 dhydrochloride
    Antagonist ≥98.0%
    BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.
  • HY-13575
    Blonanserin
    Antagonist 98.73%
    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-B1813A
    (±)-Vesamicol hydrochloride
    99.72%
    (±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.
  • HY-10815
    σ1 Receptor antagonist-1
    Antagonist 99.70%
    σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells.
  • HY-145628
    CM398
    98.09%
    CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.
  • HY-108511
    PB28 dihydrochloride
    Modulator 99.53%
    PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.