Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom AlkaloidsClick to copy article linkArticle link copied!
- Samuel ObengSamuel ObengDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Samuel Obeng
- Shyam H. KambleShyam H. KambleDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesTranslational Drug Development Core, Clinical and Translational Sciences Institute, University of Florida, Gainesville, Florida 32610, United StatesMore by Shyam H. Kamble
- Morgan E. ReevesMorgan E. ReevesDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Morgan E. Reeves
- Luis F. RestrepoLuis F. RestrepoDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Luis F. Restrepo
- Avi PatelAvi PatelDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Avi Patel
- Mira BehnkeMira BehnkeDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Mira Behnke
- Nelson J.-Y. ChearNelson J.-Y. ChearCentre for Drug Research, Universiti Sains Malaysia, 11800 Minden, Penang, MalaysiaMore by Nelson J.-Y. Chear
- Surash RamanathanSurash RamanathanCentre for Drug Research, Universiti Sains Malaysia, 11800 Minden, Penang, MalaysiaMore by Surash Ramanathan
- Abhisheak SharmaAbhisheak SharmaDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesTranslational Drug Development Core, Clinical and Translational Sciences Institute, University of Florida, Gainesville, Florida 32610, United StatesMore by Abhisheak Sharma
- Francisco LeónFrancisco LeónDepartment of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Francisco León
- Takato HiranitaTakato HiranitaDepartment of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Takato Hiranita
- Bonnie A. AveryBonnie A. AveryDepartment of Pharmaceutics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Bonnie A. Avery
- Lance R. McMahon*Lance R. McMahon*For L.R.M.: E-mail, [email protected]Department of Pharmacodynamics, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesMore by Lance R. McMahon
- Christopher R. McCurdy*Christopher R. McCurdy*For C.M.C.: E-mail, [email protected]Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, Florida 32610, United StatesTranslational Drug Development Core, Clinical and Translational Sciences Institute, University of Florida, Gainesville, Florida 32610, United StatesMore by Christopher R. McCurdy
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.
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