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Direct modification of the 5-HT3 receptor current by some anticancer drugs
The serotonin (5-hydroxytryptamine) type 3 (5-HT3) receptor is an important target in the control of emesis, and 5-HT3 receptor antagonists are effective against the early phase chemotherapy evoked vomiting. We recently reported that the anticancer drugs irinotecan and topotecan directly modulate th...
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Published in: | European journal of pharmacology 2018-02, Vol.821, p.21-28 |
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container_title | European journal of pharmacology |
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creator | Nakamura, Yukiko Ishida, Yusuke Kondo, Makoto Shimada, Shoichi |
description | The serotonin (5-hydroxytryptamine) type 3 (5-HT3) receptor is an important target in the control of emesis, and 5-HT3 receptor antagonists are effective against the early phase chemotherapy evoked vomiting. We recently reported that the anticancer drugs irinotecan and topotecan directly modulate the 5-HT-mediated 5-HT3 receptor current in vitro. In addition, the drug response depends on the 5-HT3 subunit composition. Here, we explored the effects of 35 anticancer drugs on the 5-HT3 receptor current. We microinjected Xenopus laevis oocytes with human 5-HT3A cRNA or a combination of human 5-HT3A and human 5-HT3B cRNA, and performed two-electrode voltage clamp recordings of 5-HT3A and 5-HT3AB receptor currents in the presence of each of the 35 drugs. Over 25% of the drugs we tested inhibited or potentiated the 5-HT3 receptor current. The drugs that modulated the 5-HT3 receptor current had molecular weights of approximately 500. These results implied that these anticancer drugs could affect 5-HT3 receptor. |
doi_str_mv | 10.1016/j.ejphar.2017.12.054 |
format | article |
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subjects | 5-HT3A 5-HT3B Anticancer drug Emesis Modulator Vomiting |
title | Direct modification of the 5-HT3 receptor current by some anticancer drugs |
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