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 Opioid Receptor抑制剂(2) Opioid Receptor拮抗剂(4) Opioid Receptor激动剂(8) Opioid Receptor调节剂(1) Opioid Receptor化学产品(1) 新Opioid Receptor产品

产品目录	产品描述	文献引用	实验数据
S5701^New	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
S2503	Racecadotril Racecadotril 是一种外周性的脑啡肽酶抑制剂，IC50为4.5 μM。
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。
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。	Biomedicine & Pharmacotherapy, 2016, 80:16-22 Photochem Photobiol, 2016, 92(5):728-34 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91	The effect of JTC-801 and naltrexone. (B) plasma IL-6 and (C) plasma TNF-α concentrations in the colon carcinoma model. The values represent the mean±SD derived from 6 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。	Photodermatol Photoimmunol Photomed, 2015, 10.1111/phpp.12231 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91 Sci Rep, 2014, 4:7270	(b) plasma IL-6 and (c) plasma tumornecrosis factor (TNF)-a concentrations in the colon carcinomamodel. The values represent the mean±SD derived from sixanimals. *P < 0.05
S5935^New	Alvimopan 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。
S2480	Loperamide HCl Loperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Neurogastroenterol Motil, 2016, 28(8):1241-51	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.
S5507^New	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.
S5087^New	Tianeptine Tianeptine 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.
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。
S2085	Trimebutine Trimebutine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。
S4714	(-)-Menthol (-)-Menthol是薄荷醇的左旋异构体，常被用作冷却剂，可激活TRPM8。
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^New	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.
S4588	Docusate Sodium Docusate Sodium是一种用于治疗便秘的泻药。

产品目录

产品描述

文献引用

实验数据

S5701^New

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

S2503

Racecadotril

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

产品目录	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。
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。	Biomedicine & Pharmacotherapy, 2016, 80:16-22 Photochem Photobiol, 2016, 92(5):728-34 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91	The effect of JTC-801 and naltrexone. (B) plasma IL-6 and (C) plasma TNF-α concentrations in the colon carcinoma model. The values represent the mean±SD derived from 6 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。	Photodermatol Photoimmunol Photomed, 2015, 10.1111/phpp.12231 Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91 Sci Rep, 2014, 4:7270	(b) plasma IL-6 and (c) plasma tumornecrosis factor (TNF)-a concentrations in the colon carcinomamodel. The values represent the mean±SD derived from sixanimals. *P < 0.05
S5935^New	Alvimopan 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。

产品目录	产品描述	文献引用	实验数据
S2480	Loperamide HCl Loperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Neurogastroenterol Motil, 2016, 28(8):1241-51	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.
S5507^New	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.
S5087^New	Tianeptine Tianeptine 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.
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。
S2085	Trimebutine Trimebutine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。
S4714	(-)-Menthol (-)-Menthol是薄荷醇的左旋异构体，常被用作冷却剂，可激活TRPM8。
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。

产品目录	产品描述	文献引用	实验数据
S3972^New	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.

产品目录

产品描述

文献引用

实验数据

S3972^New

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.