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• W2029485545 abstract "In Brief Although tramadol is widely available as an analgesic, its mechanism of antinociception remains unresolved. Serotonin (5-hydroxytryptamine, 5-HT) is a monoaminergic neurotransmitter that modulates numerous sensory, motor, and behavioral processes. The 5-HT type 2C receptor (5-HT2CR) is one of the major 5-HT receptor subtypes and is implicated in many important effects of 5-HT, including pain, feeding, and locomotion. In this study, we used a whole-cell voltage clamp to examine the effects of tramadol on 5-HT-induced Ca2+-activated Cl− currents mediated by 5-HT2CR expressed in Xenopus oocytes. Tramadol inhibited 5-HT-induced Cl− currents at pharmacologically relevant concentrations. The protein kinase C (PKC) inhibitor, bisindolylmaleimide I (GF109203×), did not abolish the inhibitory effects of tramadol on the 5-HT2CR-mediated events. We also studied the effects of tramadol on [3H]5-HT binding to 5-HT2CR expressed in Xenopus oocytes, and found that it inhibited the specific binding of [3H]5-HT to 5-HT2CR. Scatchard analysis of [3H]5-HT binding revealed that tramadol altered the apparent dissociation constant for binding without changing maximal binding, indicating competitive inhibition. The results suggest that tramadol inhibits 5-HT2CR function, and the mechanism of this inhibitory effect seems to involve competitive displacement of the 5-HT binding to the 5-HT2CR, rather than via activation of the PKC pathway. IMPLICATIONS: We examined the effects of tramadol on 5-hydroxy-tryptamine type 2C receptor (5-HT2CR) expressed in Xenopus oocytes. Tramadol inhibited 5-HT2CR function and the specific binding of [3H]5-HT to 5-HT2CR in a competitive manner. From these data, the mechanism of the inhibitory effect on 5-HT2CR might involve the competitive displacement of 5-HT binding to the 5-HT2CR." @default.
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• W2029485545 date "2004-05-01" @default.
• W2029485545 modified "2023-10-03" @default.
• W2029485545 title "The Inhibitory Effects of Tramadol on 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes" @default.
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• W2029485545 doi "https://doi.org/10.1213/01.ane.0000108963.77623.a4" @default.
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