κ-opioid

Opioid receptor agonist1 (Compound 2638-28) is an orally active opioid receptor agonist that shows strong affinity for MOR, DOR, and KOR, with Ki values of 5, 24, and 212 nM, respectively. It exhibits analgesic activity in both the mouse warm water tail-flick model and the acetic acid writhing model.

K-Opioid receptor agonist-1 (Compound 5a) acts as an agonist for the κ-Opioid receptor, exhibiting a K_i of 0.25 nM and an EC_50 of 2 nM. This compound is capable of crossing the blood-brain barrier (BBB), evidenced by brain/plasma ratios ranging from 0.50 to 0.65. Additionally, K-Opioid receptor agonist-1 demonstrates anti-inflammatory effects in dermatitis models induced by either Arachidonic acid or oxazolidinone.

μ/κ/δopioid receptor agonist1 is an agonist for the μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR). It produces potent and long-lasting analgesic effects in the tail flick test through peripheral MOR and KOR activation.

Opioid receptor modulator 1 is a modulator of the opioid receptor.

Opioid receptor antagonist 1 (Compound 10) is an Orvinol-based antagonist of opioid receptors. It exhibits activity as an antagonist against the analgesic properties of morphine.

Compound 4x, also known as σ1 Receptor/μOpioid receptormodulator 2, acts as a μOR agonist and a σ1R antagonist, exhibiting a potent μOR EC50 of 0.6 nM and strong σ1R inhibitory activity (Ki: 363.7 nM). It demonstrates significant analgesic effects in various pain models.

Opioid receptor antagonist2 (Compound 9) is a potent opioid receptor antagonist. It can reverse fentanyl analog-induced respiratory depression and vocal cord closure in mice. Opioid receptor antagonist2 holds promise for research on acute poisoning scenarios, such as respiratory depression resulting from opioid overdose.

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.

Mu opioid receptor antagonist 5 (compound NAP) is a selective mu opioid receptor (MOR) antagonist that crosses the blood-brain barrier, with an EC50 of 1.14 nM and a Ki of 0.37 nM. Mu opioid receptor antagonist 5 can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 2 (compound 25) is a potent and selective mu opioid receptor (MOR) antagonist that permeates the blood-brain barrier (Ki: 0.37 nM, EC50: 0.44 nM), and can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Mu opioid receptor antagonist 4 (compound 31) is a potent and selective MOR antagonist that permeates the blood-brain barrier (Ki: 0.38 nM, EC50: 0.38 nM) and can be used to study opioid use disorder (OUD).

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].

Compound 24, also known as Mu opioid receptor antagonist 7, is a potent, centrally-acting µ-opioid receptor (µOR) antagonist with an inhibitory concentration (IC50) of 29 ± 3.0 nM. It is valuable for pain and opioid use disorder research [1].

Muopioid Receptor Antagonist 8 (368) serves as an antagonist to the μ-opioid receptor, significantly inhibiting the activation of Gi induced by met-enkephalin at the µOR.

Dermorphin is agonist of μ-opioid receptor (MOR) agonist.

Dermorphin TFA is a new class of opioids-like peptides

ZT 52656A is a selective agonist of kappa opioid, and used for the prevention or alleviation of pain in the eye.

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.

Norbinaltorphimine dihydrochloride is a selective and potent κ opioid receptor antagonist that induces itch-associated responses in mice.

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2. 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.

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.