μ-opioid receptor

Loperamide hydrochloride (ADL 2-1294) is a synthetic, piperidine derivative and opioid agonist with antidiarrheal activity.

ML-335 is a μ-δ isomer-targeted agonist, a μOR-δOR-biased ligand that can serve as a scaffold for the development of unique types of (isomer-biased) drugs.ML-335 is a MOR (μ-opioid receptor) DOR (δ-opioid receptor) heterodimer, with anti-injury sensory activity and pain inhibitory activity.

Endomorphin 1 is a high affinity and selective agonist of the μ-opioid receptor and displays reasonable affinities for kappa3 binding sites (Ki: 20~30 nM).

Apitegromab (SRK-015) is a new myostatin inhibitor, an antibody targeting myostatin precursor, which can be used to study neuromuscular diseases including spinal muscular atrophy.

Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM. It holds promise for research into pain management and neuropsychiatric disorders [1].

μ opioid receptor agonist 2 (Compound H-3) is a MOR receptor agonist used for research on pain and pain-related diseases.

σ 1 Receptor μ Opioid receiver modulator 1 (Compound 44) is an effective σ 1 receptor antagonist (Ki=1.86 nM) and μ Opioid receptor agonists (Ki=2.1 nM). Opioid receptor modulator 1 shows potent analgesic activity, and can be used for the research of neuropathic pain.

μ opioid receptor agonist 1 (Compound H-1a) is an optically pure oxyheterocyclic substituted pyrroloxypyrazole derivative and an MOR receptor agonist that can be used in the study of pain and pain-related disorders.

Cebranopadol (GRT6005) is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP) and δ-opioid (DOP) receptor, respectively.

SCH-486757 is an agonist of nociceptin-1 (NOP1) and orphanin FQ peptide receptors and is used in the study of cough.

CP 866087 is an opioid receptor antagonist for the study of female sexual dysfunction.

Trimebutine CTB salt (GIC-1001) is an opioid receptor agonist used in the study of pain.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Naltrexone hydrochloride (Naltrexone HCl) is a synthetic opioid antagonist used in the prevention of relapse of opiate addiction and alcoholism.

Progesterone (Pregn-4-ene-3,20-dione) is the major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production.

Salvinorin A is a non-nitrogenous κ-opioid selective agonist.

Cerivastatin sodium (BAY W 6228 sodium) is an orally active and highly potent HMG-CoA reductase inhibitor with lipid-lowering activity that can reduce low-density lipoprotein cholesterol levels. Cerivastatin sodium has anticancer effects and can be used to study primary hyperlipidemia.

[DPro10] Dynorphin A (1-11)acetate,porcine is a highly potent κ-opioid receptor agonist with a Ki value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine is an n-alkylated derivative with analgesic activity.

U-48520 is an agonist of the μ-opioid receptor (μ-opioid receptor) with an EC50 of 1561 nM.

KOR agonist 4 (compound 39) is an agonist targeting the κ opioid receptor (Kappa Opioid Receptor) and activates G protein signaling. It has an EC50 of 14 nM and an Emax of 83% for binding to GTPγS. This compound demonstrates moderate to high intrinsic clearance in human liver cells and shows selectivity for the κ opioid receptor over the μ (MOR) and δ (DOR) opioid receptors by factors of 60 and 810, respectively. KOR agonist 4 is useful for research into central nervous system (CNS) disorders.

DALDA TFA is a potent, μ-opioid receptor agonist exhibiting high selectivity and an affinity constant (K i) of 1.69 nM. It demonstrates antinociceptive properties and influences respiratory functions [1].

AP-238 is a novel synthetic opioid (NSO) that acts as an agonist for the μ-opioid receptor (MOR), with an EC50 of 248 nM. Additionally, AP-238 exhibits analgesic properties.

KOR agonist 3 (Compound 5) is an agonist of the κ opioid receptor (κOR) with an EC50 of 0.88 nM. It also exhibits some activation of μOR, with an EC50 of 720 nM. However, KOR agonist 3 does not activate δOR at concentrations below 1 μM. Its ability to recruit β-Arrestin-2 is lower than that of U50488.