2. Signaling Pathways
  3. Neuronal Signaling
  4. Sigma Receptor

Sigma Receptor

Sigma Receptor

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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 Isoform Specific Products:

Sigma Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-16996A
    BD-1047 dihydrobromide
    		Antagonist 98.17%
    BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches.
    BD-1047 dihydrobromide
  • HY-18100A
    PRE-084 hydrochloride
    		Agonist 99.92%
    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.
    PRE-084 hydrochloride
  • HY-113416
    Dehydroepiandrosterone sulfate
    		Activator 99.93%
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate
  • 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.
    Siramesine hydrochloride
  • HY-B0765
    Dehydroepiandrosterone sulfate sodium
    		Activator 99.96%
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium salt participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium
  • HY-159997
    AD353
    AD353 is a selective sigma-1 receptor ligand with antiallodynic activity. AD353 exhibits high potency both in a model of Capsaicin (HY-10448)-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile.
    AD353
  • HY-131914B
    EST64454 maleate
    		Antagonist
    EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
    EST64454 maleate
  • HY-168562
    σ1 Receptor ligand 1
    σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research.
    σ1 Receptor ligand 1
  • HY-13510
    Cutamesine dihydrochloride
    		Agonist 98.01%
    Cutamesine (SA4503) dihydrochloride is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine dihydrochloride shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine dihydrochloride has antidepressant effects.
    Cutamesine dihydrochloride
  • HY-B1813A
    (±)-Vesamicol hydrochloride
    		99.81%
    (±)-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.
    (±)-Vesamicol hydrochloride
  • HY-111669
    CT1812
    		Antagonist
    CT1812 (Sigma-2 receptor antagonist 1) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. CT1812 can be used for the research of Alzheimer’s disease.
    CT1812
  • HY-101864
    Blarcamesine hydrochloride
    		Agonist 99.87%
    Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
    Blarcamesine hydrochloride
  • HY-13575
    Blonanserin
    		Antagonist 99.62%
    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.
    Blonanserin
  • HY-18099A
    S1RA hydrochloride
    		Antagonist 99.94%
    S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.
    S1RA hydrochloride
  • 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 agent.
    Glycerol phenylbutyrate
  • HY-19469
    Roluperidone
    		99.86%
    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).
    Roluperidone
  • HY-B2215
    Dimemorfan phosphate
    		Agonist 99.87%
    Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
    Dimemorfan phosphate
  • HY-108511
    PB28 dihydrochloride
    		Modulator 99.97%
    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.
    PB28 dihydrochloride
  • HY-18101A
    BD1063 dhydrochloride
    		Antagonist ≥98.0%
    BD1063 dhydrochloride is a potent and selective sigma 1 receptor antagonist.
    BD1063 dhydrochloride
  • HY-145628
    CM398
    		99.85%
    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.
    CM398
Sigma Receptor Isoform Comparison

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