化学
类阿片
药理学
吲哚试验
受体
止痛药
阿片受体
天然产物
立体化学
生物化学
医学
作者
Hiromitsu Takayama,Hayato Ishikawa,Mika Kurihara,Mariko Kitajima,Norio Aimi,Dhavadee Ponglux,Fumi Koyama,Kenjiro Matsumoto,Tomoyuki Moriyama,Leonard T. Yamamoto,Kazuo Watanabe,Toshihiko Murayama,Syunji Horie
摘要
Mitragynine (1) is a major alkaloidal component in the Thai traditional medicinal herb, Mitragyna speciosa, and has been proven to exhibit analgesic activity mediated by opioid receptors. By utilizing this natural product as a lead compound, synthesis of some derivatives, evaluations of the structure-activity relationship, and surveys of the intrinsic activities and potencies on opioid receptors were performed with guinea pig ileum. The affinities of some compounds for mu-, delta-, and kappa-receptors were determined in a receptor binding assay. The essential structural moieties in the Corynanthe type indole alkaloids for inducing the opioid agonistic activity were also clarified. The oxidative derivatives of mitragynine, i.e., mitragynine pseudoindoxyl (2) and 7-hydroxymitragynine (12), were found as opioid agonists with higher potency than morphine in the experiment with guinea pig ileum. In addition, 2 induced an analgesic activity in the tail flick test in mice.
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