オピオイド受容体
阻害剤の選択性比較
カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
---|---|---|---|---|
水 | DMSO | アルコール | ||
S2503 | Racecadotril | <1 mg/mL | 22 mg/mL | 77 mg/mL |
S5701 | Alvimopan dihydrate (LY246736 dihydrate) | -1 mg/mL | 92 mg/mL | -1 mg/mL |
S3066 | Naloxone HCl | 72 mg/mL | 72 mg/mL | <1 mg/mL |
S2722 | JTC-801 | <1 mg/mL | 90 mg/mL | 31 mg/mL |
S2103 | Naltrexone HCl | 14 mg/mL | 14 mg/mL | <1 mg/mL |
S5935 | Alvimopan | <1 mg/mL | 85 mg/mL | <1 mg/mL |
S2480 | Loperamide HCl | <1 mg/mL | 22 mg/mL | 4 mg/mL |
S1139 | ADL5859 HCl | 5 mg/mL | 86 mg/mL | 1 mg/mL |
S5507 | Trimebutine maleate | -1 mg/mL | 100 mg/mL | -1 mg/mL |
S2322 | (+)-Matrine | 11 mg/mL | 49 mg/mL | 49 mg/mL |
S2085 | Trimebutine | <1 mg/mL | 50 mg/mL | <1 mg/mL |
S5087 | Tianeptine | -1 mg/mL | 87 mg/mL | '-1 mg/mL |
S3204 | Meptazinol HCl | 53 mg/mL | 53 mg/mL | 53 mg/mL |
S3972 | Lobeline hydrochloride | -1 mg/mL | 74 mg/mL | -1 mg/mL |
S4588 | Docusate Sodium | 18 mg/mL | 88 mg/mL | '88 mg/mL |
亜型選択性的な製品
Opioid Receptor製品
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S2503 |
RacecadotrilRacecadotril (Acetorphan) is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM. |
||
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. |
||
S3066 |
Naloxone HClNaloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose. |
||
S2722 |
JTC-801JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
![]() ![]() The effects of JTC-801, chloroquine phosphate, and SCF antibody on the expression of collagen type I in the dorsal skin of tranexamic acid-treated NOA mice. The values are expressed as the mean ± SD derived from 10 animals. *p < 0.05. |
|
S2103 |
Naltrexone HClNaltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. |
![]() ![]() The sex difference in epidermal melanocytes after tranexamic acid treatment following naltrexone treatment. Naltrexone was injected intraperitoneally into the mice throughout the experimental period. Five days after the final UVB irradiation of the eye, the number of Dopa-positive melanocytes in the epidermal sheets prepared from the ear was determined. The values are presented as the means±SD derived from six animals (biological replicates; *P < 0.05). |
|
S5935 |
AlvimopanAlvimopan (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. |
||
S2480 |
Loperamide HClLoperamide HCl (ADL 2-1294) 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. |
![]() ![]() Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given. |
|
S1139 |
ADL5859 HClADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2. |
![]() ![]() ADL-5859 respectively ADL-5747 were dopioid agonists (DORs) which were developed as analgesics for post-operative, neuropathic or musculoskeletal pain. They were expected to have superior analgesic potency over the existing ones, due to the different receptor targeted. However their development was stopped due to unconvincing efficacy. |
|
S5507 |
Trimebutine maleateTrimebutine 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. |
||
S2322 |
(+)-MatrineMatrine((+)-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. |
||
S2085 |
TrimebutineTrimebutine (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. |
||
S5087 |
TianeptineTianeptine (S-1574, JNJ-39823277, TPI-1062) is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. |
||
S3204 |
Meptazinol HClMeptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM. |
||
S3972 |
Lobeline hydrochlorideLobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors. |
||
S4588 |
Docusate SodiumDocusate 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. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S2503 |
RacecadotrilRacecadotril (Acetorphan) is a peripherally acting enkephalinase inhibitor with an IC50 of 4.5 μM. |
||
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. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S3066 |
Naloxone HClNaloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate overdose. |
2020, 19;20:58 2020, 13:1803-1810 2020, 10.1007/s13577-020-00425-8 |
|
S2722 |
JTC-801JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
2021, 10.1038/s41589-021-00751-4 2017, 33(2):84-91 2016, 80:16-22 |
![]() ![]() The effects of JTC-801, chloroquine phosphate, and SCF antibody on the expression of collagen type I in the dorsal skin of tranexamic acid-treated NOA mice. The values are expressed as the mean ± SD derived from 10 animals. *p < 0.05. |
S2103 |
Naltrexone HClNaltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence. |
2021, 10.1038/s41386-021-00962-2 2018, 18(1):89 2017, 33(2):84-91 |
![]() ![]() The sex difference in epidermal melanocytes after tranexamic acid treatment following naltrexone treatment. Naltrexone was injected intraperitoneally into the mice throughout the experimental period. Five days after the final UVB irradiation of the eye, the number of Dopa-positive melanocytes in the epidermal sheets prepared from the ear was determined. The values are presented as the means±SD derived from six animals (biological replicates; *P < 0.05). |
S5935 |
AlvimopanAlvimopan (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. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S2480 |
Loperamide HClLoperamide HCl (ADL 2-1294) 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. |
2020, 2020/9/20.4.7.30734 2019, 17(2):1312-1320 2017, 9(12) |
![]() ![]() Low-micromolar amounts of loperamide inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 8 μM LPM (C). Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given. |
S1139 |
ADL5859 HClADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2. |
2012, 21(11):1607-18 |
![]() ![]() ADL-5859 respectively ADL-5747 were dopioid agonists (DORs) which were developed as analgesics for post-operative, neuropathic or musculoskeletal pain. They were expected to have superior analgesic potency over the existing ones, due to the different receptor targeted. However their development was stopped due to unconvincing efficacy. |
S5507 |
Trimebutine maleateTrimebutine 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. |
||
S2322 |
(+)-MatrineMatrine((+)-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. |
2019, 91(8):1440-1447 |
|
S2085 |
TrimebutineTrimebutine (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. |
||
S5087 |
TianeptineTianeptine (S-1574, JNJ-39823277, TPI-1062) is an antidepressant agent that act as an atypical agonist of the μ-opioid receptor with clinically negligible effects on the δ- and κ-opioid receptors. |
||
S3204 |
Meptazinol HClMeptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S3972 |
Lobeline hydrochlorideLobeline hydrochloride is an alkaloid that acts on nicotinic cholinergic receptors but is less potent than nicotine. It is also a VMAT2 ligand and an antagonist of μ-opioid receptors. |
2020, 10.1111/jcmm.16029 |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S4588 |
Docusate SodiumDocusate 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. |