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

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2019 Dec 14

PMID 31834797

Citations 61

Authors

Samuel Obeng

Shyam H Kamble

Morgan E Reeves

Luis F Restrepo

Avi Patel

Mira Behnke

Nelson J-Y Chear

Surash Ramanathan

Abhisheak Sharma

Francisco Leon

Takato Hiranita

Bonnie A Avery

Lance R McMahon

Christopher R McCurdy

Affiliations

Soon will be listed here.

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 (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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Mitragynine and morphine produce dose-dependent bimodal action on food but not water intake in rats.

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