Document Type
Article
Publication Date
8-31-2020
Abstract
In this study, effects of capsaicin, an active ingredient of the capsicum plant, were investigated on human 5-hydroxytryptamine type 3 (5-HT3) receptors. Capsaicin reversibly inhibited serotonin (5-HT)-induced currents recorded by two-electrode voltage clamp method in Xenopus oocytes. The inhibition was time- and concentration-dependent with an IC50 = 62 μM. The effect of capsaicin was not altered in the presence of capsazepine, and by intracellular BAPTA injections or trans-membrane potential changes. In radio-ligand binding studies, capsaicin did not change the specific binding of the 5-HT3 antagonist [3H]GR65630, indicating that it is a noncompetitive inhibitor of 5-HT3 receptor. In HEK-293 cells, capsaicin inhibited 5-HT3 receptor induced aequorin luminescence with an IC50 of 54 µM and inhibition was not reversed by increasing concentrations of 5-HT. In conclusion, the results indicate that capsaicin acts as a negative allosteric modulator of human 5-HT3 receptors.
Recommended Citation
Nebrisi EE, Prytkova T, Lorke DE, et al. Capsaicin Is a Negative Allosteric Modulator of the 5-HT3 Receptor. Front Pharmacol. 2020;11:1274. Published 2020 Aug 31. https://doi.org/10.3389/fphar.2020.01274
Copyright
The authors
Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 License.
Included in
Biochemical Phenomena, Metabolism, and Nutrition Commons, Biochemistry Commons, Chemical and Pharmacologic Phenomena Commons, Medical Biochemistry Commons, Other Chemicals and Drugs Commons, Other Chemistry Commons
Comments
This article was originally published in Frontiers in Pharmacology, volume 11, in 2020. https://doi.org/10.3389/fphar.2020.01274