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Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2019-12-27 , DOI: 10.1021/acs.jmedchem.9b01465
Samuel Obeng 1, 2 , Shyam H Kamble 3, 4 , Morgan E Reeves 1 , Luis F Restrepo 1 , Avi Patel 1 , Mira Behnke 1 , Nelson J-Y Chear 5 , Surash Ramanathan 5 , Abhisheak Sharma 3, 4 , Francisco León 2 , Takato Hiranita 1 , Bonnie A Avery 3 , Lance R McMahon 1 , Christopher R McCurdy 2, 4
Affiliation  

Selected indole-based kratom alkaloids were evaluated for their opioid and adrenergic receptor binding and functional effects, in vivo antinociceptive effects, plasma protein binding, and metabolic stability. Mitragynine, the major alkaloid in Mitragyna speciosa (kratom), had higher affinity at opioid receptors than at adrenergic receptors while the vice versa was observed for corynantheidine. The observed polypharmacology of kratom alkaloids may support its utilization to treat opioid use disorder and withdrawal.

中文翻译:

肾上腺皮质激素和阿片类药物的结合亲和力,代谢稳定性,血浆蛋白结合特性以及所选的基于吲哚的Kratom生物碱的功能研究。

评价所选的基于吲哚的kratom生物碱的阿片样物质和肾上腺素能受体结合和功能作用,体内抗伤害感受作用,血浆蛋白结合和代谢稳定性。Mitragynine(Mitragyna speciosa(kratom)中的主要生物碱)对阿片样物质受体的亲和力高于对肾上腺素能受体的亲和力,而对于Corynantheidine则相反。观察到的kratom生物碱的多药理学可能支持其用于治疗阿片类药物使用障碍和戒断。
更新日期:2019-12-29
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