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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.

Samuel ObengShyam H KambleMorgan E ReevesLuis F RestrepoAvi PatelMira BehnkeNelson J-Y ChearSurash RamanathanAbhisheak SharmaFrancisco LeónTakato HiranitaBonnie A AveryLance R McMahonChristopher R McCurdy
Published in: Journal of medicinal chemistry (2019)
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.
Keyphrases
  • binding protein
  • chronic pain
  • pain management
  • dna binding
  • amino acid
  • small molecule
  • transcription factor
  • anti inflammatory