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

Samuel Obeng, Shyam H. Kamble, Morgan E. Reeves, Luis F. Restrepo, Avi Patel, Mira Behnke, Nelson J.Y. Chear, Surash Ramanathan, Abhisheak Sharma, Francisco León, Takato Hiranita, Bonnie A. Avery, Lance R Mcmahon, Christopher R. McCurdy

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)433-439
Number of pages7
JournalJournal of Medicinal Chemistry
Volume63
Issue number1
DOIs
StatePublished - Jan 9 2020

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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