doi: 10.1254/jjp.73.357.
High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats
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- PMID: 9165374
- DOI: 10.1254/jjp.73.357
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High affinity binding of azasetron hydrochloride to 5-hydroxytryptamine3 receptors in the small intestine of rats
Jpn J Pharmacol.
1997 Apr.
Free article
Abstract
The binding affinity of azasetron hydrochloride (azasetron) for the 5-hydroxytryptamine3 (5-HT3) receptor in a tissue preparation of rat small intestine was investigated by using [3H]granisetron as a radioligand. Scatchard analysis of specific [3H]granisetron binding revealed a single population of saturable binding sites in the tissue preparation. At this site, azasetron was concentration-dependently competitive with [3H]granisetron, and it inhibited the specific [3H]granisetron binding with a Ki value of 0.33 nM. Azasetron has a high affinity for 5-HT3 receptor in the gastrointestinal organ, the very site of its antiemetic action against chemotherapy-induced emesis.
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