μ Opioid Receptor/MOR Agonist

DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).

KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC₅₀ of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus.

Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC₅₀ of 226 μM. Corydaline is a μ-opioid receptor (K_i of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC₅₀ of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.

Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (K_i: 1.11 nM), displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties.

PZM21 is a potent and selective μ opioid receptor agonist with an EC₅₀ of 1.8 nM.

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [³⁵S]GTPγS binding in mouse brain membranes.

Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC₅₀ of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms.

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

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.

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.

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.

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.

Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (K_i: 1.11 nM), displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties.

Acetyl tetrapeptide-15 is a synthetic peptide. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioid receptor via an endorphin-like pathway. Acetyl tetrapeptide-15 is used in the cosmetics for sensitive skin.

SC13 is an orally active, selective Flap structure-specific endonuclease 1 (FEN1) inhibitor and mu opioid receptor (MOR) activator. SC13 impairs DNA damage repair and induces apoptosis in cancer cells. SC13 activates cGAS-STING signaling, increases chemokine secretion, and promotes CAR-T cell infiltration at solid tumour sites. SC13 can be used for the research of solid tumours and pain.