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.

9 Items

  • E1R
    Cat. No.
    A18825

    E1R

    E1R is a novel positive allosteric modulator of sigma-1 receptors.

    2 mg
    $235.00
    5 mg
    $280.00
    All 7 sizes
  • Convolamine
    Cat. No.
    A79286

    Convolamine

    Convolamine is a sigma-1 receptor modulator derived from Convolvulus pluricaulis. It demonstrates positive modulation of the sigma-1 receptor with an IC50 of 289 nM. This compound exhibits notable cognitive-enhancing and neuroprotective activities, making it a valuable tool for research into neurological disorders and cognitive function enhancement.

    5 mg
    $55.00
    10 mg
    $90.00
    All 5 sizes
  • KSCM-11
    Cat. No.
    A79293

    KSCM-11

    KSCM-11 is a selective ligand for the sigma receptor, functioning as a modulator of sigma receptor activity. This compound exhibits significant potential in neuroscience research, contributing to studies on neuroprotection, pain management, and the modulation of psychotropic effects. Its targeted action on sigma receptors makes it a valuable tool for exploring therapeutic avenues in neurological disorders.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • (2S,3S)-E1R
    Cat. No.
    A79295

    (2S,3S)-E1R

    (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances cognitive and memory functions. This enantiomer of E1R is designed for research applications exploring the modulation of sigma-1 receptor activity, which has implications in treating cognition and memory disorders. Its selectivity and mechanism of action make it a valuable reagent in neuroscience studies.

    5 mg
    $245.00
    10 mg
    $405.00
    All 5 sizes
  • (±)-PPCC hemioxalate
    Cat. No.
    A79300

    (±)-PPCC hemioxalate

    (±)-PPCC hemioxalate is a selective modulator of the sigma-1 receptor, which plays a critical role in regulating intracellular calcium signaling between the endoplasmic reticulum and mitochondria. This compound promotes the dissociation of the sigma-1 receptor from the BIP complex, influencing cellular bioenergetics and survival. (±)-PPCC hemioxalate is suitable for research applications related to cocaine addiction, memory processes, pain modulation, depression, Alzheimer's disease, stroke, and cancer studies.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • (Rac)-E1R
    Cat. No.
    A79303

    (Rac)-E1R

    (Rac)-E1R is a racemic mixture that functions as a positive allosteric modulator of the sigma-1 receptor (Sig1R PAM). This compound has been investigated for its potential role in enhancing cognitive functions and memory processes. Research applications include the study of cognitive and memory disorders, making it a valuable tool in neuroscientific investigations.

    5 mg
    $230.00
    10 mg
    $370.00
    All 5 sizes
  • (2R,3S)-E1R
    Cat. No.
    A79304

    (2R,3S)-E1R

    (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances receptor activity. This compound has demonstrated potential in the treatment of cognition and memory disorders by modulating signaling pathways associated with neuroprotection and cognitive enhancement. Its unique mechanism of action makes it a valuable tool for research in neurobiology and the development of therapies for neurodegenerative diseases.

    5 mg
    $245.00
    10 mg
    $405.00
    All 5 sizes
  • (2R,3R)-E1R
    Cat. No.
    A79308

    (2R,3R)-E1R

    (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM), specifically designed for enhancing cognitive function and memory. This enantiomer of E1R exhibits significant biological activity in modulating Sig1R, which is implicated in various neurological processes. Research applications include the investigation of cognitive and memory disorders, offering potential therapeutic insights for related conditions.

    5 mg
    $245.00
    10 mg
    $405.00
    All 5 sizes
  • SOMCL-668
    Cat. No.
    A79322

    SOMCL-668

    SOMCL-668 is a selective and potent allosteric modulator of the sigma-1 receptor. It has been demonstrated to enhance social interaction and alleviate cognitive impairments induced by the sigma-1 agonist PRE084. Additionally, SOMCL-668 exhibits anti-seizure properties, making it a valuable tool for research into psychotic illnesses and related neurological disorders.

    Out of stock

    All 3 sizes

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