Opioid Receptor

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

Opioid Receptor产品

所有产品(16) Opioid Receptor抑制剂(2) Opioid Receptor拮抗剂(4) Opioid Receptor激动剂(8) Opioid Receptor调节剂(1)

目录号	产品描述	文献引用	实验数据
S2503	Racecadotril Racecadotril (Acetorphan) 是一种外周性的脑啡肽酶抑制剂，IC50为4.5 μM。
S5701	Alvimopan dihydrate (LY246736 dihydrate) Alvimopan (LY-246736)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上
S3066	Naloxone HCl Naloxone HCl是阿片反向激动剂药物，用来中和过量阿片的效果。	Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 J Pain Res, 2020, 13:1803-1810
S2722	JTC-801 JTC-801是一种选择性opioid receptor-like1 (ORL1) receptor（阿片受体样1受体）拮抗剂，IC50为94 nM，微弱抑制受体δ， κ和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是一种阿片受体拮抗剂，主要用于治疗酒精依赖和阿片类药物依赖。	Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2 Sci Rep, 2021, 11(1):9300 BMC Evol Biol, 2018, 18(1):89	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)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上。
S2480	Loperamide HCl Loperamide HCl (ADL 2-1294)是一种阿片受体激动剂，ED50为0.15 mg/kg。	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是一种δ-opioid receptor激动剂，K_i为0.8 nM，选择性作用于opioid receptor κ，μ，对hERG通道具有微弱的抑制活性。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.
E0013^New	DAMGO DAMGO (DAGO) 是一种有效的选择性 μ 阿片受体(μ opioid receptor) 激动剂，ki 为 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是一种在植物Sophora属中发现的生物碱，具有多种药理作用，包括抗癌作用，是κ阿片受体激动剂。	J Med Virol, 2019, 91(8):1440-1447
S2085	Trimebutine Trimebutine (Mebutin) 是一种外周μ，κ和δ阿片受体激动剂，用作解痉剂用于治疗急性和慢性腹痛。
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 HCl是一种独特的中枢神经系统阿片类镇痛药,可以抑制[³H]二氢吗啡的结合，IC50为58nM。
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)是一种用于治疗便秘的泻药。

目录号

产品描述

文献引用

实验数据

S2503

Racecadotril

Racecadotril (Acetorphan) 是一种外周性的脑啡肽酶抑制剂，IC50为4.5 μM。

S5701

Alvimopan dihydrate (LY246736 dihydrate)

Alvimopan (LY-246736)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上

目录号	产品描述	文献引用	实验数据
S3066	Naloxone HCl Naloxone HCl是阿片反向激动剂药物，用来中和过量阿片的效果。	Hum Cell, 2021, 10.1007/s13577-021-00579-z Cancer Cell Int, 2020, 19;20:58 J Pain Res, 2020, 13:1803-1810
S2722	JTC-801 JTC-801是一种选择性opioid receptor-like1 (ORL1) receptor（阿片受体样1受体）拮抗剂，IC50为94 nM，微弱抑制受体δ， κ和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是一种阿片受体拮抗剂，主要用于治疗酒精依赖和阿片类药物依赖。	Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2 Sci Rep, 2021, 11(1):9300 BMC Evol Biol, 2018, 18(1):89	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)是一种有效的、相对非选择性的opioid拮抗剂，对μ, δ 和 κ opioid receptors的Ki值分别为0.77、4.4和40 nM，选择性比对其他胺类G蛋白偶联受体高100倍以上。

目录号	产品描述	文献引用	实验数据
S2480	Loperamide HCl Loperamide HCl (ADL 2-1294)是一种阿片受体激动剂，ED50为0.15 mg/kg。	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是一种δ-opioid receptor激动剂，K_i为0.8 nM，选择性作用于opioid receptor κ，μ，对hERG通道具有微弱的抑制活性。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.
E0013^New	DAMGO DAMGO (DAGO) 是一种有效的选择性 μ 阿片受体(μ opioid receptor) 激动剂，ki 为 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是一种在植物Sophora属中发现的生物碱，具有多种药理作用，包括抗癌作用，是κ阿片受体激动剂。	J Med Virol, 2019, 91(8):1440-1447
S2085	Trimebutine Trimebutine (Mebutin) 是一种外周μ，κ和δ阿片受体激动剂，用作解痉剂用于治疗急性和慢性腹痛。
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 HCl是一种独特的中枢神经系统阿片类镇痛药,可以抑制[³H]二氢吗啡的结合，IC50为58nM。

目录号	产品描述	文献引用	实验数据
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

目录号

产品描述

文献引用

实验数据

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