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.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Adrenergic Agents / metabolism
-
Adrenergic Agents / pharmacology*
-
Analgesics / metabolism
-
Analgesics / pharmacology*
-
Animals
-
Blood Proteins / metabolism*
-
CHO Cells
-
Cricetulus
-
Dopamine Agents / metabolism
-
Dopamine Agents / pharmacology*
-
Guinea Pigs
-
Humans
-
Microsomes, Liver / metabolism
-
Rats
-
Receptors, Adrenergic / metabolism
-
Receptors, Opioid / metabolism
-
Secologanin Tryptamine Alkaloids / metabolism
-
Secologanin Tryptamine Alkaloids / pharmacology*
Substances
-
Adrenergic Agents
-
Analgesics
-
Blood Proteins
-
Dopamine Agents
-
Receptors, Adrenergic
-
Receptors, Opioid
-
Secologanin Tryptamine Alkaloids
-
mitragynine