JNJ42165279
| CAS号 | 1346528-50-4 | 货号 | BCP16594 |
| 中文名 | JNJ42165279 | ||
| 英文名 | JNJ42165279 | ||
| 中文别名 | |||
| 英文别名 | JNJ-42165279;JNJ 42165279; | ||
| 分子式 | C18H17ClF2N4O3 | 分子量 | 410.8 |
| 生物活性 | JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting | ||
| 信号通路 | Protease/Metabolic Enzyme Neuro Signaling Pathway | ||
| 靶 点 | FAAH | ||
结构式
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