μ-opioid

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

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.

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].

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.

BAN ORL 24 is a highly potent nociceptin orphan FQ (N OFQ) receptor (NOP) antagonist that can be used to study neurological diseases.

BPR1M97 is a mu opioid receptor (MOP) and neuropeptide-orphin FQ (NOP) receptor agonist with blood-brain barrier permeability and potency, with Kis values of 1.8 nM for MOP and 4.2 nM for NOP.BPR1M97 exhibits anti-injurious effects and antinociceptive effects.

JNJ-20788560 is a delta opioid receptor (DOR) agonist with analgesic activity. It is more selective for DOR than for mu opioid receptors (MOR).

CP-866087 is a novel, potent and selective mu-opioid receptor antagonist for the study of female sexual dysfunction.

AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors (EC50s of 19.6 and 34.7 nM, respectively.) AT-121 (0.003-0.03 mg kg) reduced capsaicin-induced thermal anisocoria in a dose-dependent manner, but did not increase scratching activity in rhesus monkeys. In rhesus monkey drug self-administration tests, AT-121 at doses of 0.3 to 10 μg kg per injection lacked reinforcing effects (a potential marker of abuse) and did not reduce the reinforcing effects of food pellets.AT-121 (0.01 or 0.03 mg kg) did not induce hyperalgesia, a marker of tolerance, in rhesus monkeys.AT-121 is a safe non-addictive pain reliever with anti-injury and analgesic effects.

Samidorphan HCl is an orally active and highly potent modulator of the opioid system that binds to μ‐opioid, κ‐opioid, and delta-opioid receptors. Samidorphan HCl is a novel μ-opioid receptor antagonist, a partial agonist for k-opioid and delta-opioid receptors. Samidorphan HCl can be used to prevent and treat schizophrenia.

SNC 80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist, Ki = 1.78 nM, IC50 = 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

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

Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders, with IBS being one of the most common multifactorial GI disorders. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Trimebutine is not an FDA-Approved Clinical drug, but it is available in Canada and several other international countries.

Trimebutine maleate (Polibutin) is a weak mu-opioid agonist and has antimuscarinic effects. Trimebutine is an agonist of peripheral mu, delta, and kappa opiate receptors served as a spasmolytic drug for therapy of both chronic and acute abdominal pain.

Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

SR17018, a mu-opioid receptor (MOR) agonist, binds with GTPγS and has an EC50 of 97 nM.

ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.

BW-180C (DADLE) is a prototypical δ-opioid receptor agonist that also displays activity at the μ-opioid receptor. Displays antinociceptive activity in vivo.

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.

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

EST73502 is an agonist of μ-opioid receptor(Ki = 64 nM) agonist and an antagonist of σ1 receptor (Ki = 118 nM). EST73502 displays antinociceptive activity.

1,1'-(Octane-1,8-diyl)diguanidine dihydrochloride is a synthetic opioid peptide derived from the natural opioid peptide enkephalin. It is a potent agonist of the mu-opioid receptor (MOR) with a Ki of 0.14 nM, making it one of the most potent MOR agonists known to date.