Pharmacological aspects of the effects of tramadol on G-protein coupled receptors.

Article Details

Citation

Copy to clipboard

Minami K, Uezono Y, Ueta Y

Pharmacological aspects of the effects of tramadol on G-protein coupled receptors.

J Pharmacol Sci. 2007 Mar;103(3):253-60.

PubMed ID

17380034 [ View in PubMed

]

Abstract

Tramadol is an analgesic that is used worldwide, but its mechanisms of action have not been elucidated. It has been speculated that tramadol acts primarily through the activation of micro-opioid receptors and the inhibition of monoamine reuptake. The majority of studies to date have focused on ion channels in the central nervous system as targets of anesthetics and analgesics. During the past decade, major advances have been made in our understanding of the physiology and pharmacology of G-protein coupled receptor (GPCR) signaling. Several studies have shown that GPCRs and ion channels are targets for analgesics and anesthetics. In particular, tramadol has been shown to affect GPCRs, including muscarinic acetylcholine receptors and 5-hydroxytryptamine receptors. Here, the effects of tramadol on monoamine transporters, GPCRs, and ion channels are presented, and recent research on the pharmacology of tramadol is discussed.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Tramadol	Mu-type opioid receptor	Protein	Humans	Yes	Agonist	Details