Quercetin Inhibits the 5-Hydroxytryptamine Type 3 Receptor-mediated Ion Current by Interacting with Pre-Transmembrane Domain I
2005
Lee, B.H. (Konkuk University, Seoul, Republic of Korea) | Chang, C.G. (Sungkyunkwan University, Suwon, Republic of Korea) | Kim, H.C. (Kangwon National University, Chuncheon, Republic of Korea) | Jeong, S.M. (Konkuk University, Seoul, Republic of Korea) | Lee, J.H. (Konkuk University, Seoul, Republic of Korea) | Kim, J.H. (Konkuk University, Seoul, Republic of Korea) | Yoon, I.S. (Konkuk University, Seoul, Republic of Korea) | Lee, J.H. (Konkuk University, Seoul, Republic of Korea) | Choi, S.H. (Konkuk University, Seoul, Republic of Korea) | Lee, S.M. (Konkuk University, Seoul, Republic of Korea) | Han, Y.S. (Konkuk University, Seoul, Republic of Korea) | Paik, H.D. (Konkuk University, Seoul, Republic of Korea) | Kim, Y.M. (Konkuk University, Seoul, Republic of Korea) | Nah, S.Y. (Konkuk University, Seoul, Republic of Korea), E-mail: [email protected]
The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 (5-HT∧3A) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The 5-HT∧3A receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with 5-HT∧3A receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current (I∧5-HT) with an IC∧50 of 64.7±2.2 μM. Inhibition was competitive and voltage-independent.
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