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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M4808 | TRV130 hydrochloride | TRV130 hydrochloride (Oliceridine) is a novel μ-opioid receptor (MOR) G protein-biased ligand. |
| M9615 | DAMGO | DAMGO is an opioid receptor agonist with the ability to affect the locomotive activity in rodents, Kd value is 3.46 nM for native μ-OPR. |
| M21699 | Nalfurafine (TRK-820) | Nalfurafine is an effective and selective agonist of G protein-biased κ-opioid receptor with high translational potential. |
| M21657 | Bevenopran | Bevenopran (CB-5945) is a peripheral μ-opioid receptor antagonist. |
| M21655 | LY2795050 | LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction. |
| M21654 | BTRX-335140 | BTRX-335140 is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. |
| M21653 | GSK1521498 | GSK1521498 is a novel, potent and selective μ-opioid receptor antagonist. |
| M21375 | BMS-986187 | BMS-986187 is a δ-opioid receptor selective orthosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (~1 μM). bms-986187 has no observable PAM activity at the μ receptor (EC50=3 μM). |
| M21363 | TRV-130 | TRV 130 is a novel μ-opioid receptor (MOR) G protein-biased ligand; elicits robust G protein signaling(pEC50=8.1), with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization. |
| M21325 | β-Casomorphin, human TFA | β-Casomorphin, human TFA is an opioid-like peptide that is an opioid receptor agonist. Sequence: Tyr-Pro-Phe-Val-Glu-Pro-Ile. |
| M21324 | β-Casomorphin, bovine acetate | β-casomorphin, bovine (β-Casomorphin-7 (bovine)) acetate is an opioid-active peptide with an IC50 value of 14 μM for binding to opioid receptors.Sequence：Tyr-Pro-Phe-Pro-Gly-Pro-Ile. |
| M21317 | EST73502 | EST73502 is a selective, orally active, μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist that crosses the blood-brain barrier with Ki values of 64 nM and 118 nM for MOR and σ1R effects, respectively. EST73502 can be used in pain relief studies. |
| M20425 | (-)-Menthol | (-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8. |
| M14033 | Ro 64-6198 | Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. |
| M14032 | Norbinaltorphimine dihydrochloride | Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist. |
| M14031 | Methylnaltrexone Bromide | Methylnaltrexone Bromide, a quaternary derivative of Naltrexone, is an orally active and selective mu-opioid receptor antagonist, functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract. |
| M14030 | Matrine | Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist. |
| M14029 | Aticaprant | Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM. |
| M14028 | Deltorphin 2 TFA | Deltorphin 2 TFA is a selective peptide agonist for the δ opioid receptor. |
| M11311 | BMS-986122 | Bms-986122 is a selective and effective positive allosteric regulator of μ -opioid receptor (µ-OR). Bms-986122 showed enhancement of β -inhibitory protein recruitment, adenylate cyclase inhibition and G-protein activation mediated by normal agonists. Bms-986122 enhances damGO-mediated [35S]GTPγS binding in mouse meninges. |
| M11163 | Dermorphin | Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Dermorphin can be used to suppress neuralgia. |
| M10584 | SR17018 | SR17018 is an mu-opioid-receptor (MOR) agonist, EC50 is 97 nM for binding with GTPγS. |
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