|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|
- Opioid Receptor抑制剂（15）
- 新Opioid Receptor产品
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.
Racecadotril 是一种外周性的脑啡肽酶抑制剂，IC50为4.5 μM。
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。
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
(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
Loperamide 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.
ADL5859 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.
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.
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.
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.