Opioid Receptor
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S5701 | Alvimopan dihydrate (LY246736 dihydrate) | -1 mg/mL | 92 mg/mL | -1 mg/mL |
| S2503 | Racecadotril | <1 mg/mL | 22 mg/mL | 77 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 |
| 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 |
| S5087 | Tianeptine | -1 mg/mL | 87 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 |
| S4714 | (-)-Menthol | 16 mg/mL | 31 mg/mL | 31 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 |
特异性亚型抑制剂
- Opioid Receptor抑制剂（15）
- 新Opioid Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S5701New |
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. |
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| S2503 |
RacecadotrilRacecadotril 是一种外周性的脑啡肽酶抑制剂，IC50为4.5 μM。 |
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| S3066 |
Naloxone HClNaloxone HCl是阿片反向激动剂药物，用来中和过量阿片的效果。 |
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| S2722 |
JTC-801JTC-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。 |
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
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| S2103 |
Naltrexone HClNaltrexone 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。 |
(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
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| S2480 |
Loperamide HClLoperamide HCl是一种阿片受体激动剂，ED50为0.15 mg/kg。 |
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. |
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| S1139 |
ADL5859 HClADL5859 HCl是一种δ-opioid receptor激动剂，Ki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。 |
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. |
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| S5507New |
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. |
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| S5087New |
TianeptineTianeptine 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. |
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| 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。 |
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| S2085 |
TrimebutineTrimebutine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。 |
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| S4714 |
(-)-Menthol(-)-Menthol是薄荷醇的左旋异构体，常被用作冷却剂，可激活TRPM8。 |
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| S3204 |
Meptazinol HClMeptazinol 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。 |
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| S3972New |
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. |
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| S4588 |
Docusate SodiumDocusate Sodium是一种用于治疗便秘的泻药。 |
