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Capsaicin Is a Negative Allosteric Modulator of the 5-HT3 Receptor.

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 ?M. 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.

SUBMITTER: Nebrisi EE 

PROVIDER: S-EPMC7490547 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Capsaicin Is a Negative Allosteric Modulator of the 5-HT<sub>3</sub> Receptor.

Nebrisi Eslam El EE   Prytkova Tatiana T   Lorke Dietrich Ernst DE   Howarth Luke L   Alzaabi Asma Hassan AH   Yang Keun-Hang Susan KS   Howarth Frank C FC   Oz Murat M  

Frontiers in pharmacology 20200831

In this study, effects of capsaicin, an active ingredient of the capsicum plant, were investigated on human 5-hydroxytryptamine type 3 (5-HT<sub>3</sub>) receptors. Capsaicin reversibly inhibited serotonin (5-HT)-induced currents recorded by two-electrode voltage clamp method in <i>Xenopus</i> oocytes. The inhibition was time- and concentration-dependent with an IC<sub>50</sub> = 62 μM. The effect of capsaicin was not altered in the presence of capsazepine, and by intracellular BAPTA injections  ...[more]

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