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Isoforms Recommended: Sigma 1 Receptor
Results for "

σ1R

" in MedChemExpress (MCE) Product Catalog:

16

Inhibitors & Agonists

1

Peptides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18099
    S1RA
    3 Publications Verification

    E-52862

    		 Sigma Receptor 5-HT Receptor Neurological Disease
    S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice [1] .
    S1RA
  • HY-14895
    Fabomotizole

    CM346

    		 Parasite Monoamine Oxidase Sigma Receptor P-glycoprotein Infection Cardiovascular Disease Neurological Disease
    Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects [1] .
    Fabomotizole
  • HY-18099A
    S1RA hydrochloride
    3 Publications Verification

    E-52862 hydrochloride

    		 Sigma Receptor 5-HT Receptor Neurological Disease
    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 [1] .
    S1RA hydrochloride
  • HY-125821
    Sigma-1 receptor antagonist 1

    		Sigma Receptor Neurological Disease
    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 [1].
    Sigma-1 receptor antagonist 1
  • HY-P1341
    OXA(17-33)

    Orexin A (17-33) (human, mouse, rat, bovine)

    		 Orexin Receptor (OX Receptor) Sigma Receptor Phospholipase Neurological Disease
    OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca 2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy [1] .
    OXA(17-33)
  • HY-117731
    UKH-1114

    		Sigma Receptor Neurological Disease
    UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a Ki values of 1279 and 46 nM for σ1R and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research [1].
    UKH-1114
  • HY-125819
    Sigma-1 receptor antagonist 2

    		Sigma Receptor Neurological Disease
    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 [1].
    Sigma-1 receptor antagonist 2
  • HY-176405
    σ1R-IN-1

    		Sigma Receptor Neurological Disease
    σ1R-IN-1 ((R,R)-1a) is a potent σ-1R inhibitor with an IC50 of 110 nM. σ1R-IN-1 is promising for research of neuropsychiatric disorders [1].
    σ1R-IN-1
  • HY-153091
    BMY 14802

    		Adrenergic Receptor 5-HT Receptor Sigma Receptor Neurological Disease
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM [1] .
    BMY 14802
  • HY-149274
    Sigma-1 receptor antagonist 4

    		Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with potential to prevent morphine tolerance [1].
    Sigma-1 receptor antagonist 4
  • HY-134189
    EST73502

    		Opioid Receptor Sigma Receptor Neurological Disease
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity [1].
    EST73502
  • HY-134189A
    EST73502 monohydrochloride

    		Sigma Receptor Opioid Receptor Neurological Disease
    EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity [1].
    EST73502 monohydrochloride
  • HY-181722
    σ1R/H3R ligand-1

    		Sigma Receptor Histamine Receptor Neurological Disease
    σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1R Ki of 8.8 nM and an H3R Ki of 31.2 nM. Through the dual action of simultaneously antagonizing σ1R and H3R, σ1R/H3R ligand-1 exhibits potent dose-dependent analgesic activity in mouse models of visceral pain and neuropathic pain. σ1R/H3R ligand-1 can be used for the research of visceral pain and neuropathic pain [1].
    σ1R/H3R ligand-1
  • HY-163065
    σ1 Receptor/μ Opioid receptor modulator 2

    		Opioid Receptor Sigma Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models [1].
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-162759
    Sigma-1 receptor antagonist 6

    		Sigma Receptor Neurological Disease
    Sigma-1 receptor antagonist 6 (Compound 12) is an antagonist of the Sigma-1 receptor (σ1R). Sigma-1 receptor antagonist 6 exerts a robust antiallodynic effect by antagonizing σ1R. Sigma-1 receptor antagonist 6 can be used in neuropathic pain animal models to alleviate mechanical allodynia induced by paclitaxel (HY-B0015) [1].
    Sigma-1 receptor antagonist 6
  • HY-149335
    Sigma-1 receptor antagonist 5

    		Sigma Receptor Histamine Receptor Neurological Disease
    Sigma-1 receptor antagonist 5 (compound 12)，a 4-pyridylpiperidine derivative with analgesic activity，is an antagonist of sigma receptor (Ki=4.5 nM (σ1R)，10 nM (σ2R)) and histamine H3 (hH3R，Ki=7.7 nM，IC50=215 nM). Sigma-1 receptor antagonist 5 suppresses Capsaicin-induced nociception with antinociceptive activity and shows potent efficacy in nociceptive and neuropathic pain models [1].
    Sigma-1 receptor antagonist 5

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