S3066 |
Naloxone HCl
|
Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose. |
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Pharmacol Res Perspect, 2022, 10(5):e01016
-
Toxicol Res (Camb), 2022, 11(3):498-510
|
|
S2103 |
Naltrexone HCl
|
Naltrexone HCl(PTI-901) is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. |
-
Transl Psychiatry, 2024, 14(1):165
-
Toxicol Res (Camb), 2022, 11(3):498-510
-
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
|
|
S2722 |
JTC-801
|
JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
-
Heliyon, 2024, 10(11):e32571
-
Sci Rep, 2023, 13(1):1483
-
Sci Rep, 2023, 13(1):1483
|
|
S2480 |
Loperamide HCl
|
Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
-
Front Neurosci, 2024, 18:1424936
-
Front Cell Infect Microbiol, 2023, 13:1139152
-
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
|
|
S2322 |
(+)-Matrine
|
Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist. |
-
J Vet Res, 2024, 68(1):35-44
-
Transl Oncol, 2023, 35:101712
-
Front Pharmacol, 2022, 13:1027441
|
|
S2503 |
Racecadotril
|
Racecadotril (Acetorphan) is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM. |
|
|
S0009 |
Asimadoline hydrochloride
|
Asimadoline hydrochloride (EMD-61753 hydrochloride) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). |
|
|
E0472 |
BMS-986122
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR), shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation, and potentiates DAMGO-mediated [35S]GTPγS binding in mouse brain membranes. |
|
|
S5701 |
Alvimopan dihydrate (LY246736 dihydrate)
|
Alvimopan (LY-246736) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors. |
|
|
E4647New |
Aticaprant
|
Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD). |
|
|
S5507 |
Trimebutine maleate
|
Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. |
|
|
E2868 |
Naloxegol Oxalate
|
Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation. |
|
|
S4588 |
Docusate Sodium
|
Docusate Sodium (Aerosol OT, Bis(2-ethylhexyl) sulfosuccinate sodium salt, Constonate) is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally. |
|
|
E2880 |
methylnaltrexone bromide
|
Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation. |
|
|
S2085 |
Trimebutine
|
Trimebutine (Mebutin) is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain. |
|
|
S5935 |
Alvimopan
|
Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors. |
-
Curr Issues Mol Biol, 2024, 46(7):6472-6488
|
|
S2480 |
Loperamide HCl
|
Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
-
Front Neurosci, 2024, 18:1424936
-
Front Cell Infect Microbiol, 2023, 13:1139152
-
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
|
|
S2322 |
(+)-Matrine
|
Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist. |
-
J Vet Res, 2024, 68(1):35-44
-
Transl Oncol, 2023, 35:101712
-
Front Pharmacol, 2022, 13:1027441
|
|
S0009 |
Asimadoline hydrochloride
|
Asimadoline hydrochloride (EMD-61753 hydrochloride) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). |
|
|
S5507 |
Trimebutine maleate
|
Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. |
|
|
S2085 |
Trimebutine
|
Trimebutine (Mebutin) is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain. |
|
|
S3066 |
Naloxone HCl
|
Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose. |
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Pharmacol Res Perspect, 2022, 10(5):e01016
- Toxicol Res (Camb), 2022, 11(3):498-510
|
|
S2103 |
Naltrexone HCl
|
Naltrexone HCl(PTI-901) is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. |
- Transl Psychiatry, 2024, 14(1):165
- Toxicol Res (Camb), 2022, 11(3):498-510
- Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
|
|
S2722 |
JTC-801
|
JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
- Heliyon, 2024, 10(11):e32571
- Sci Rep, 2023, 13(1):1483
- Sci Rep, 2023, 13(1):1483
|
|
E4647New |
Aticaprant
|
Aticaprant (CERC-501, LY-2456302) is a potent, orally bioavailable, centrally-penetrant antagonist of the kappa opioid receptor with a Ki of 0.807 nM. It exhibits an antidepressant effect with the potential to treat major depressive disorder (MDD). |
|
|
E2868 |
Naloxegol Oxalate
|
Naloxegol oxalate (NKTR-118 oxalate) is a μ-opioid-receptor antagonist with a Ki of 33.8 nM. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation. |
|
|
E2880 |
methylnaltrexone bromide
|
Methylnaltrexone bromide is an antagonist of µ-opioid receptor that reduces the viability of lung cancer cells by inhibiting Src activation. |
|
|
S5935 |
Alvimopan
|
Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors. |
- Curr Issues Mol Biol, 2024, 46(7):6472-6488
|
|
S2480 |
Loperamide HCl
|
Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. |
- Front Neurosci, 2024, 18:1424936
- Front Cell Infect Microbiol, 2023, 13:1139152
- Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
|
|
S2322 |
(+)-Matrine
|
Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist. |
- J Vet Res, 2024, 68(1):35-44
- Transl Oncol, 2023, 35:101712
- Front Pharmacol, 2022, 13:1027441
|
|
S0009 |
Asimadoline hydrochloride
|
Asimadoline hydrochloride (EMD-61753 hydrochloride) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). |
|
|
S5507 |
Trimebutine maleate
|
Trimebutine maleate is the maleate salt form of trimebutine, which is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. |
|
|
S2085 |
Trimebutine
|
Trimebutine (Mebutin) is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain. |
|
|