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.

4 Items

  • (±)-Vesamicol hydrochloride
    Cat. No.
    A79263

    (±)-Vesamicol hydrochloride

    Synonyms: (±)-AH5183 hydrochloride

    (±)-Vesamicol hydrochloride is a potent inhibitor of vesicular acetylcholine transport, exhibiting a Ki value of 2 nM. Additionally, it demonstrates a high affinity for σ1 and σ2 receptors, with Ki values of 26 nM and 34 nM, respectively. This compound is valuable for research into cholinergic signaling and receptor interactions, facilitating studies on neurological disorders and synaptic transmission mechanisms.

    2 mg
    $25.00
    5 mg
    $45.00
    All 6 sizes
  • KB-5492 free base
    Cat. No.
    A79275

    KB-5492 free base

    KB-5492 free base is a selective inhibitor of sigma receptors, demonstrating potent activity by inhibiting specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound exhibits anti-ulcer properties, making it valuable for research in gastrointestinal disorders and related therapeutic applications. Its mechanism of action also suggests potential implications in neuropharmacology and pain management studies.

    2 mg
    $30.00
    5 mg
    $45.00
    All 7 sizes
  • KB-5492 anhydrous
    Cat. No.
    A79282

    KB-5492 anhydrous

    KB-5492 anhydrous is a selective inhibitor of the sigma receptor, demonstrating inhibition of specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound has been identified for its potential application as an anti-ulcer agent, making it relevant for research in gastrointestinal disorders and sigma receptor pharmacology. Its activity underscores the significance of sigma receptors in various biological processes, providing valuable insights for therapeutic exploration.

    5 mg
    $355.00
    10 mg
    $590.00
    All 5 sizes
  • CM304
    Cat. No.
    A79291

    CM304

    Synonyms: FTC-146 hydrochloride

    CM304 is a potent sigma-1 receptor (S1R) inhibitor. It demonstrates significant neuroprotective effects by mitigating drug-induced convulsions in rat models. This compound is valuable for research focused on neurological disorders and the modulation of synaptic functions associated with S1R activity.

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

4 Items

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