Sigma Receptor

Sigma receptor ligands bind sigma-1 and sigma-2 receptors, two unrelated proteins that are not G protein-coupled. The sigma-1 receptor was cloned in 1996 and resembles a yeast sterol isomerase more than any known mammalian receptor. It resides mainly in the endoplasmic reticulum, and its 2016 crystal structure showed a trimer with one transmembrane helix per protomer. The gene for the sigma-2 receptor was identified in 2017 as transmembrane protein 97 (TMEM97). Cutamesine (SA4503) dihydrochloride, 4-IBP and pentoxyverine citrate are sigma-1 agonists, whereas S1RA and BD-1047 2HBr are sigma-1 antagonists. Siramesine is a sigma-2 agonist, and UMB24 a sigma-2 antagonist.

Items 26-31 of 31

  • EST64454 maleate
    Cat. No.
    A79296

    EST64454 maleate

    EST64454 maleate is a potent σ1 receptor antagonist, effectively demonstrating antinociceptive properties suitable for pain management research. With excellent metabolic stability in various species and a favorable pharmacokinetic profile in rodent models, EST64454 maleate stands out as a promising candidate for clinical applications. Its high aqueous solubility and suitable permeability through Caco-2 cell membranes further support its potential in drug development studies.

    1 mg
    $65.00
    5 mg
    $150.00
    All 7 sizes
  • Sigma-1 receptor antagonist 6
    Cat. No.
    A79298

    Sigma-1 receptor antagonist 6

    Sigma-1 receptor antagonist 6 is a selective antagonist of the Sigma-1 receptor (σ1R), exhibiting significant antiallodynic properties. This compound effectively reduces mechanical allodynia in neuropathic pain models, particularly in response to paclitaxel treatment. Its application in research settings enables the exploration of σ1R modulation in pain pathways and the development of novel analgesic therapies.

    Out of stock

    All 3 sizes
  • PW507
    Cat. No.
    A79305

    PW507

    PW507 is a selective antagonist of the sigma 1 receptor (S1R) with a binding affinity of Ki 7.5 nM for the human variant. With minimal interactions with the sigma 2 receptor (S2R) and hERG channel, PW507 is well-suited for studies requiring brain penetration. This compound is particularly relevant for investigating painful diabetic neuropathy (PDN) and other related conditions.

    Out of stock

    All 3 sizes
  • AB21
    Cat. No.
    A79311

    AB21

    AB21 is a potent and selective antagonist of the sigma-1 receptor (S1R), exhibiting an IC50 value of 13 nM for S1R with minimal activity against the sigma-2 receptor (S2R) at 102 nM. This compound is effective in reducing mechanical hypersensitivity, making it a valuable tool for research into pain modulation and related neurological disorders. Additionally, AB21 may facilitate studies into the role of S1R in various physiological and pathological processes.

    Out of stock

    All 3 sizes
  • BD-1047
    Cat. No.
    A79315

    BD-1047

    BD-1047 is a selective functional antagonist targeting sigma receptors. It demonstrates significant activity in modulating behaviors associated with dopamine signaling, reducing apomorphine-induced climbing and phencyclidine-induced head twitches. This compound is valuable for research applications in neuropharmacology and the study of sigma receptor biology.

    Out of stock

    All 3 sizes
  • σ1 Receptor antagonist 4
    Cat. No.
    A79324

    σ1 Receptor antagonist 4

    σ1 Receptor Antagonist 4 is a selective antagonist targeting the sigma1 (σ1) receptor, exhibiting a Ki value of 10 nM. This compound shows weak activity at the sigma2 (σ2) receptor with a Ki of 370 nM and demonstrates no significant effects on dopamine (DAT), serotonin (SERT), or norepinephrine (NET) transporters. σ1 Receptor Antagonist 4 is primarily utilized in research to elucidate the role of the σ1 receptor in various biological processes and its potential implications in neurodegenerative diseases and psychiatric disorders.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 26-31 of 31

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