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

Sigma Receptor

Sigma Receptor

Related Products

PDF 0.68 MB

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-181425
    N-Desmethyl xanomeline
    N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline (HY-105182). N-Desmethyl xanomeline binds to muscarinic, serotonergic, histaminergic and dopaminergic receptors. N-Desmethyl xanomeline can be used for the research of schizophrenia.
    N-Desmethyl xanomeline
  • HY-108510R
    Rimcazole dihydrochloride (Standard)
    		Antagonist
    Rimcazole dihydrochloride (Standard) is the analytical standard of Rimcazole (dihydrochloride) (HY-108510). This product is intended for research and analytical applications. Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can reduce locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer.
    Rimcazole dihydrochloride (Standard)
  • HY-184175
    Sigma-2 Receptor ligand 2
    Sigma-2 Receptor ligand 2 is a fluorescence labeled sigma-2 ligand. Sigma-2 Receptor ligand 2 can be used as a fluorescent probe.
    Sigma-2 Receptor ligand 2
  • HY-111081
    (±)-PPCC
    		Agonist
    (±)-PPCC is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.
    (±)-PPCC
  • HY-118279
    KSCM-1
    KSCM-1 is a selective sigma-1 receptor ligand with a Ki of 27.5 nM. KSCM-1 shows more selective for sigma-1 over sigma-2, and shows no significant affinity at non-sigma receptors.
    KSCM-1
  • HY-101864R
    Blarcamesine hydrochloride (Standard)
    		Agonist
    Blarcamesine hydrochloride (Standard) is the analytical standard of Blarcamesine hydrochloride (HY-101864). This product is intended for research and analytical applications. Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
    Blarcamesine hydrochloride (Standard)
  • HY-18101
    BD-1063
    		Antagonist
    BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.
    BD-1063
  • 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-N15339A
    Convolamine hydrochloride
    		Activator
    Convolamine hydrochloride is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC50 value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease.
    Convolamine hydrochloride
  • 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-100985R
    IPAG (Standard)
    		Antagonist
    IPAG (Standard) is the analytical standard of IPAG (HY-100985). This product is intended for research and analytical applications. IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3. IPAG induces apoptosis.
    IPAG (Standard)
  • HY-100155R
    4-IBP (Standard)
    		Agonist
    4-IBP (Standard) is the analytical standard of 4-IBP (HY-100155). This product is intended for research and analytical applications. 4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research.
    4-IBP (Standard)
  • 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-105296R
    Blarcamesine (Standard)
    		Agonist
    Blarcamesine (Standard) is the analytical standard of Blarcamesine (HY-105296). This product is intended for research and analytical applications. Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.
    Blarcamesine (Standard)
  • HY-108509R
    BMY-14802 hydrochloride (Standard)
    		Antagonist
    BMY-14802 hydrochloride (Standard) is the analytical standard of BMY-14802 (hydrochloride) (HY-108509). This product is intended for research and analytical applications. BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
    BMY-14802 hydrochloride (Standard)
  • 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)
Sigma Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.