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Alisol derivatives are unique protostane-type triterpenoid compounds that are isolated from Alismatis rhizoma, which is a well-known traditional medicine in East Asia. In the present study, we investigated the effects of protostane-type triterpenoids (AA, Alisol A; AB, Alisol B; AB-ac, Alisol B 23-acetate; AC-ac, Alisol C 23-aceteate) on 5-HT-induced currents mediated by the human 5-HT(3)A receptor expressed in Xenopus laevis oocytes. Co-treatment with triterpenoids regulated the 5-HT-induced inward peak current in a concentration-dependent and reversible manner. In addition, regulation of I(5-HT) by triterpenoids occurred in a non-competitive manner. Taken together, these results indicate that triterpenoids may regulate the 5-HT(3)A receptors that are expressed in Xenopus oocytes. Furthermore, this regulation of the ligand-gated ion channel activity by triterpenoids may be one of the pharmacological actions of Alismatis rhizoma. Copyright 2010 Elsevier B.V. All rights reserved.

Citation

Jun-Ho Lee, Yoo-Jin Lee, Seok-Woo Kang, Yangseok Kim, Minkyu Shin, Moochang Hong, Eun-Kyoung Seo, Sung-Hoon Kim, Seung-Yeol Nah, Hyunsu Bae. Effects of protostane-type triterpenoids on the 5-HT3A receptor-mediated ion current in Xenopus oocytes. Brain research. 2010 May 17;1331:20-7

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PMID: 20307506

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