Abstract:
: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.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Nakamura Y,Ishida Y,Yamada T,Shimada Sdoi
10.1016/j.bbrc.2011.10.084subject
Has Abstractpub_date
2011-11-18 00:00:00pages
416-20issue
2eissn
0006-291Xissn
1090-2104pii
S0006-291X(11)01896-1journal_volume
415pub_type
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