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-16996AR
    BD-1047 dihydrobromide (Standard)
    		Antagonist
    BD-1047 (dihydrobromide) (Standard) is the analytical standard of BD-1047 (dihydrobromide). This product is intended for research and analytical applications. 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 (Standard)
  • HY-13575R
    Blonanserin (Standard)
    		Antagonist
    Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-118901S
    Opipramol-d4
    Opipramol-d4 is the deuterium labeled Opipramol.
    Opipramol-d<sub>4</sub>
  • HY-A0139
    Thiothixene
    		Antagonist
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • HY-A0161AR
    Chlophedianol hydrochloride (Standard)
    		Control
    Chlophedianol (hydrochloride) (Standard) is the analytical standard of Chlophedianol (hydrochloride). This product is intended for research and analytical applications. Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs).
    Chlophedianol hydrochloride (Standard)
  • HY-134004R
    Pentoxyverine (Standard)
    		Agonist
    Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance.
    Pentoxyverine (Standard)
  • HY-101484AR
    NE-100 hydrochloride (Standard)
    		Antagonist
    NE-100 hydrochloride (Standard) is the analytical standard of NE-100 hydrochloride (HY-101484A). This product is intended for research and analytical applications. NE-100 hydrochloride is an orally active and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE-100 hydrochloride can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE-100 hydrochloride can be used for research on nervous system diseases.
    NE-100 hydrochloride (Standard)
  • HY-B2087R
    Glycerol phenylbutyrate (Standard)
    Glycerol phenylbutyrate (Standard) is the analytical standard of Glycerol phenylbutyrate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-155484
    SOMCL-668
    		Modulator
    SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research.
    SOMCL-668
  • HY-W714837
    5-Phenyllevulinic acid
    5-Phenyllevulinic acid (4-Oxo-5-phenylpentanoic acid) is an endogenous fungal metabolite with inhibitory activity against the bacterium B. megaterium, the plant pathogenic fungus S. tritici, and the alga C. fusca. 5-Phenyllevulinic acid is also an intermediate in the synthesis of σ receptor ligands. 5-Phenyllevulinic acid holds potential for research in the field of anti-infection studies .
    5-Phenyllevulinic acid
  • HY-B1216R
    Oxeladin citrate (Standard)
    		Agonist
    Oxeladin (citrate) (Standard) is the analytical standard of Oxeladin (citrate). This product is intended for research and analytical applications. Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (Ki = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research.
    Oxeladin citrate (Standard)
  • HY-14218R
    Ditolylguanidine (Standard)
    		Agonist
    Ditolylguanidine (Standard) is the analytical standard of Ditolylguanidine. This product is intended for research and analytical applications. Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer.
    Ditolylguanidine (Standard)
  • HY-169185
    Sigma-2 Radioligand 2
    Sigma-2 Radioligand 2 (compund 4) exhibits low nanomolar affinity (Ki(σ2)=2.30 nM) and high subtype selectivity (Ki(σ1)/Ki(σ2) > 1500) for the σ2 receptor.
    Sigma-2 Radioligand 2
  • HY-13510R
    Cutamesine dihydrochloride (Standard)
    		Agonist
    Cutamesine dihydrochloride (Standard) is the analytical standard of Cutamesine dihydrochloride. This product is intended for research and analytical applications. 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.
    Cutamesine dihydrochloride (Standard)
  • HY-149854B
    AB21 hydrochloride
    		Antagonist 99.93%
    AB21 hydrochloride is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R. AB21 hydrochloride has the effect of reducing mechanical hypersensitivity.
    AB21 hydrochloride
  • HY-108513
    σ1 Receptor antagonist 4
    		Antagonist
    σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters.
    σ1 Receptor antagonist 4
  • HY-118901R
    Opipramol (Standard)
    		Antagonist
    Opipramol (Standard) is the analytical standard of Opipramol. This product is intended for research and analytical applications. 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).
    Opipramol (Standard)
Sigma Receptor Isoform Comparison

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