cannabinoid CB1 receptors has the potential to become a valuable therapy for chronic pain conditions as long as central nervous system effects are attenuated. A new class of cannabinoid ligands was rationally designed from known aminoalkylindole agonists and showed good binding and functional activities at human CB1 and CB2 receptors. This has led to the discovery of a novel CB1/CB2 dual agonist, naphthal
只要中枢神经系统作用减弱,外周
大麻素CB1受体的选择性激活就有可能成为治疗慢性疼痛的有价值的疗法。从已知的
氨基烷基
吲哚激动剂中合理设计了一类新的
大麻素配体,并在人CB1和CB2受体上表现出良好的结合和功能活性。这导致发现了一种新型的CB1 / CB2双激动剂
萘-1-基-(4-戊氧基
萘-1-基)甲酮(13),在动物模型中显示出良好的口服
生物利用度,有效的抗痛觉过敏活性,并且作用有限。脑部渗透。