Opioid Receptors

Opioid receptor agonists and antagonists act on mu, delta and kappa receptors and the related nociceptin receptor. All four are G protein-coupled receptors that respond to endogenous peptides such as endorphins, enkephalins and dynorphins. Expression cloning of the delta opioid receptor in 1992 opened the family to molecular study. The nociceptin/orphanin FQ peptide (NOP) receptor, first called opioid receptor-like 1 (ORL1), was matched to its endogenous peptide agonist in 1995. Dynorphin A (1-13) Acetate is a peptide agonist at the kappa receptor, and JDTic is a kappa antagonist. SR-17018 acts as a mu agonist, while alvimopan is a peripherally acting opioid antagonist. MCOPPB trihydrochloride is a NOP agonist, and BAN ORL 24 blocks the same receptor.

7 Items

  • Hemorphin-7
    Cat. No.
    A42300

    Hemorphin-7

    Hemorphin-7 is a hemorphin peptide that acts as an opioid receptor activator. This endogenous opioid, derived from the β-chain of hemoglobin, demonstrates significant antinociceptive and antihypertensive effects. Hemorphin-7 is commonly utilized in research applications exploring pain relief mechanisms and the modulation of blood pressure through opioid receptor pathways and inhibition of angiotensin-converting enzyme (ACE).

    1 mg
    $95.00
    5 mg
    $290.00
    All 3 sizes
  • (±)-Salsolinol hydrochloride
    Cat. No.
    A62339

    (±)-Salsolinol hydrochloride

    (±)-Salsolinol hydrochloride is a potent μ-opioid receptor (MOR) activator derived from dopamine. This compound modulates neuronal activity by reducing GABAergic transmission and enhancing the excitability of dopamine neurons. Its effects on neuronal firing rates in the posterior ventral tegmental area (pVTA) make it valuable for research applications focused on opioid signaling and dopamine-related pathways.

    25 mg
    $35.00
    50 mg
    $55.00
    All 3 sizes
  • ERG-IN-6
    Cat. No.
    A62416

    ERG-IN-6

    ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation.

    5 mg
    $350.00
    10 mg
    $650.00
    All 3 sizes
  • Helianorphin-19
    Cat. No.
    A62457

    Helianorphin-19

    Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator, exhibiting a Ki of 21 nM and an EC50 of 45 nM. It demonstrates significant KOR-specific peripheral analgesic activity in mouse models of chronic visceral pain. This compound is valuable for investigating the role of KOR in pain modulation and may provide insights into therapeutic approaches for pain management.

    0.5 mg
    $330.00
    1 mg
    $530.00
    All 2 sizes
  • Bromadoline maleate
    Cat. No.
    A62524

    Bromadoline maleate

    Bromadoline maleate is a selective activator of the μ-opioid receptor, demonstrating potent analgesic activity across diverse biological matrices. This compound is effective for pain management studies and has been successfully quantified alongside its N-demethylated metabolites in both human and canine biological samples, making it a valuable tool for pharmaceutical research and opioid pharmacokinetics.

    5 mg
    $350.00
    10 mg
    $650.00
    All 3 sizes
  • Ro-48-6791
    Cat. No.
    A62527

    Ro-48-6791

    Ro-48-6791 is an opioid receptor activator that functions by binding to and activating opioid receptors. This compound is known to enhance physiological effects associated with opioid signaling, potentially influencing both therapeutic and adverse outcomes. Research applications include studying opioid receptor-mediated pathways and exploring the pharmacological effects of opioid agonists.

    25 mg
    $1,655.00
    50 mg
    $2,115.00
    All 3 sizes
  • (RS)-Salsolinol hydrobromide
    Cat. No.
    A62600

    (RS)-Salsolinol hydrobromide

    (RS)-Salsolinol hydrobromide is a μ-opioid receptor (MOR) activator derived from dopamine. It has been shown to reduce GABAergic transmission and increase the excitability of dopamine neurons, subsequently enhancing the sustained firing of neurons in the posterior ventral tegmental area (pVTA). This compound is useful in research applications investigating the modulation of dopaminergic signaling and its implications in various neurological conditions.

    10 mg
    $245.00
    100 mg
    $370.00
    All 3 sizes

7 Items

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