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

doi:10.1021/acs.jmedchem.9b01465

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

Department of Pharmacology

Research output: Contribution to journal › Article › peer-review

108 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 language	English (US)
Pages (from-to)	433-439
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	63
Issue number	1
DOIs	https://doi.org/10.1021/acs.jmedchem.9b01465
State	Published - Jan 9 2020

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/acs.jmedchem.9b01465

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Obeng, S., Kamble, S. H., Reeves, M. E., Restrepo, L. F., Patel, A., Behnke, M., Chear, N. J. Y., Ramanathan, S., Sharma, A., León, F., Hiranita, T., Avery, B. A., McMahon, L. R., & McCurdy, C. R. (2020). Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. Journal of Medicinal Chemistry, 63(1), 433-439. https://doi.org/10.1021/acs.jmedchem.9b01465

Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids. / Obeng, Samuel; Kamble, Shyam H.; Reeves, Morgan E. et al.
In: Journal of Medicinal Chemistry, Vol. 63, No. 1, 09.01.2020, p. 433-439.

Research output: Contribution to journal › Article › peer-review

Obeng, S, Kamble, SH, Reeves, ME, Restrepo, LF, Patel, A, Behnke, M, Chear, NJY, Ramanathan, S, Sharma, A, León, F, Hiranita, T, Avery, BA, McMahon, LR & McCurdy, CR 2020, 'Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids', Journal of Medicinal Chemistry, vol. 63, no. 1, pp. 433-439. https://doi.org/10.1021/acs.jmedchem.9b01465

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

Abstract

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