Opioid Receptor Agonist

CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain.

Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with K_i of 12 nM.

Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC₅₀s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS).

SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC₅₀ of 12 nM and K_i of 0.3 nM. SCH 221510 shows an anxiolytic-like effect.

[Leu5]-Enkephalin, amide is a δ opioid receptor agonist.

Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect.

Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with K_i valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE₂ (HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea.

ICI-199441 hydrochloride is a potent and selective κ-opioid receptor agonist with analgesic effects. ICI 199441 hydrochloride can improve heart resistance to ischemia/reperfusion.

Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

[D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin analog used to study the signaling pathway of delta opioid receptors.

Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a K_i of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (K_i>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.

KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (K_i = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases.

Corydine is a HIV-1 reverse transcriptase inhibitor and μ-opioid receptor (MOR) agonist, with an IC₅₀ of 356.7 μg/mL against HIV-1 reverse transcriptase, an EC₅₀ of 0.51 μM for MOR, and a K_i of 2.82 μM for MOR. Corydine produces antinociceptive effects by inhibiting acetic acid-induced writhing behavior in a MOR-dependent manner. Corydine inhibits the proliferation of cancer cells, mitogen-stimulated lymphocytes and IL-2-dependent cells. Corydine can be used in studies related to human immunodeficiency virus infection, visceral pain, leukemia, melanoma, bladder cancer and colon adenocarcinoma.

ADL-5747 is a selective and orally active agonist of the δ-opioid receptor (DOR). By binding to the δ-opioid receptors, ADL-5747 activates these receptors, thereby playing a role in pain management pathways. ADL-5747 can be used for research into pain management mechanisms.

β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties.

Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats.

GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus.

Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole can be used for the research of depression.

N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC₅₀ = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC₅₀ = 12.3 μM). The IC₅₀ values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca²⁺-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer.