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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

Obeng S 1 , Kamble SH 2 , Reeves ME 1 , Restrepo LF 1 , Patel A 1 , Behnke M 1 Show all authors , Chear NJ 3 , Ramanathan S 3 , Sharma A 2 , León F 4 , Hiranita T 1 , Avery BA 2 , McMahon LR 1 , McCurdy CR 4

Affiliations 

  • 1 Department of Pharmacodynamics, College of Pharmacy , University of Florida , Gainesville , Florida 32610 , United States
  • 2 Department of Pharmaceutics, College of Pharmacy , University of Florida , Gainesville , Florida 32610 , United States
  • 3 Centre for Drug Research , Universiti Sains Malaysia , 11800 Minden , Penang , Malaysia
  • 4 Department of Medicinal Chemistry , College of Pharmacy, University of Florida , Gainesville , Florida 32610 , United States
J Med Chem, 2020 01 09;63(1):433-439.
PMID: 31834797 DOI: 10.1021/acs.jmedchem.9b01465

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.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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