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 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-HT

SUBMITTER: Nebrisi EE 

PROVIDER: S-EPMC7490547 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature