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XB-ART-44740
Biochem Biophys Res Commun 2011 Nov 18;4152:416-20. doi: 10.1016/j.bbrc.2011.10.084.
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Anticancer drug irinotecan inhibits homomeric 5-HT3A and heteromeric 5-HT3AB receptor responses.

Nakamura Y , Ishida Y , Yamada T , Shimada S .


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It has been shown that anti-cancer drug induces secretion of serotonin (5-HT) from small intestine which activates serotonin type 3 (5-HT(3)) receptor to cause nausea and vomiting. In general, antagonist for 5-HT(3) receptor is used as anti-emetics during chemotherapy. However, we found that anti-cancer drug irinotecan itself inhibits 5-HT-gated current through the homomeric 5-HT(3A) and heteromeric 5-HT(3AB) receptor in a concentration-dependent manner. The inhibitory effect of irinotecan on 5-HT(3A) receptor was more potent than that on 5-HT(3AB) receptor. On the other hand, SN-38, a metabolite of irinotecan, had no effect on the responsiveness. Our findings suggest that irinotecan itself could have anti-emetic activities through inhibition of the 5-HT(3A) and 5-HT(3AB) receptor.

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