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- Title
Quercetin Inhibits the 5-Hydroxytryptamine Type 3 Receptormediated Ion Current by Interacting with Pre-Transmembrane Domain I.
- Authors
Byung-Hwan Lee; Sang-Min Jung; Jun-H ngo Lee; Jong-Hoon Kim; In-Soo Yoon; Joon-Hee Lee; Sun-Hye Choi; Sang-Mok Lee; Choon-Gon Chang; Hyung-Chun Kim; YeSun Han; Hyun-Dong Paik; Yangmee Kim; Seung-Yeol Nah
- Abstract
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-HT3A) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The 5-HT3A receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with 5-HT3A receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current (I5-HT) with an IC50 of 64.7 ± 2.2 μM. Inhibition was competitive and voltage-independent. Point mutations of pretransmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the 5-HT3A receptor.
- Publication
Molecules & Cells (Springer Nature), 2005, Vol 20, Issue 1, p69
- ISSN
1016-8478
- Publication type
Article
- DOI
10.1016/s1016-8478(23)13200-6