オピオイド受容体

シグナル伝達経路

研究分野

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)
カタログ番号	製品カタログ	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
P1118	Dermorphin	100 mg/mL	100 mg/mL	100 mg/mL
P1151	Difelikefalin	100 mg/mL	100 mg/mL	100 mg/mL
E0013	DAMGO	100 mg/mL	100 mg/mL	''100 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
E0472	BMS-986122	<1 mg/mL	90 mg/mL	<1 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

All (19) Opioid Receptor阻害剤(2) Opioid Receptor拮抗剤(4) Opioid Receptor作動薬(10) Opioid Receptorモジュレータ(2)

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	Racecadotril Racecadotril (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 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 Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
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.	Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4 Biochem Biophys Res Commun, 2021, 562:55-61 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91	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 HCl Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.	Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2 J Neurosci, 2021, 41(37):7727-7741 Sci Rep, 2021, 11(1):9300	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	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.
S2480	Loperamide HCl Loperamide HCl (ADL 2-1294) is a selective μ-opioid receptor agonist opioid with K_i 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.	bioRxiv, 2020, 2020/9/20.4.7.30734 Exp Ther Med, 2019, 17(2):1312-1320 Nutrients, 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 HCl ADL5859 HCl is a δ-opioid receptor agonist with K_i of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.	Expert Opin Inv Drugs, 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.
P1118^新	Dermorphin Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin, showing inhibition of neuropathic pain.
P1151^新	Difelikefalin Difelikefalin (CR-845, FE-202845), a peripherally restricted and selective agonist of kappa opioid receptor (KOR), produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
E0013^新	DAMGO DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.
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.
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.	Leuk Lymphoma, 2021, 1-10 J Med Virol, 2019, 91(8):1440-1447
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.
S5087	Tianeptine Tianeptine (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 HCl Meptazinol is a unique centrally active opioid analgesic, which inhibits [³H]dihydromorphine binding with IC50 of 58 nM.
E0472^新	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.
S3972	Lobeline hydrochloride Lobeline 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.	J Cell Mol Med, 2020, 10.1111/jcmm.16029
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.

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

Racecadotril

Racecadotril (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 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 Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
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.	Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4 Biochem Biophys Res Commun, 2021, 562:55-61 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91	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 HCl Naltrexone HCl is an opioid receptor antagonist used primarily in the management of alcohol dependence and opioid dependence.	Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2 J Neurosci, 2021, 41(37):7727-7741 Sci Rep, 2021, 11(1):9300	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	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.

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 HCl Loperamide HCl (ADL 2-1294) is a selective μ-opioid receptor agonist opioid with K_i 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.	bioRxiv, 2020, 2020/9/20.4.7.30734 Exp Ther Med, 2019, 17(2):1312-1320 Nutrients, 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 HCl ADL5859 HCl is a δ-opioid receptor agonist with K_i of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel. Phase 2.	Expert Opin Inv Drugs, 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.
P1118^新	Dermorphin Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin, showing inhibition of neuropathic pain.
P1151^新	Difelikefalin Difelikefalin (CR-845, FE-202845), a peripherally restricted and selective agonist of kappa opioid receptor (KOR), produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
E0013^新	DAMGO DAMGO (DAGO) is a potent and selective μ opioid receptor agonist with ki of 17 nM.
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.
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.	Leuk Lymphoma, 2021, 1-10 J Med Virol, 2019, 91(8):1440-1447
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.
S5087	Tianeptine Tianeptine (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 HCl Meptazinol 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
E0472^新	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.
S3972	Lobeline hydrochloride Lobeline 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.	J Cell Mol Med, 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

E0472^新

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.

S3972

Lobeline hydrochloride

Lobeline 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.

J Cell Mol Med, 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 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.

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 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.

研究分野別

製品類型

オピオイド受容体

シグナル伝達経路

研究分野

阻害剤の選択性比較

亜型選択性的な製品

Opioid Receptor製品