4.7 Article

Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected lndole-Based Kratom Alkaloids

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JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 1, 页码 433-439

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AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01465

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  1. National Institute on Drug Abuse [DA47855, DA48353]
  2. State of Florida

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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.

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