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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 101-102 of 102

  • Sigma-2 Radioligand 2
    Cat. No.
    A79323
    CAS No.
    2860554-31-8

    Sigma-2 Radioligand 2

    Sigma-2 Radioligand 2 selectively targets the sigma-2 receptor with a low nanomolar affinity (Ki(σ2) = 2.30 nM) and exhibits significant subtype selectivity (Ki(σ1)/Ki(σ2) > 1500). This compound is essential for research applications involving sigma receptor pharmacology, allowing for in-depth studies of receptor function and potential therapeutic implications in neuropsychiatric disorders.

    In stock View Details
    1 mg
    $345.00
    5 mg
    $870.00
    All 6 sizes
  • σ1 Receptor antagonist 4
    Cat. No.
    A79324
    CAS No.
    362512-81-0

    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.

    In stock View Details
    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

Items 101-102 of 102

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