High Affinity Binding of Azasetron Hydrochloride to 5-Hydroxytryptamine3 Receptors in the Small Intestine of Rats. | Zendy

Kenichi Katayama | Zendy; Kiyoshi Asano | Zendy; Keiichiro Haga | Zendy; Takemi Fukuda | Zendy

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High Affinity Binding of Azasetron Hydrochloride to 5-Hydroxytryptamine3 Receptors in the Small Intestine of Rats.

Author(s) -

Kenichi Katayama,

Kiyoshi Asano,

Keiichiro Haga,

Takemi Fukuda

Publication year - 1997

Publication title -

the japanese journal of pharmacology

Language(s) - English

Resource type - Journals

eISSN - 1347-3506

pISSN - 0021-5198

DOI - 10.1254/jjp.73.357

Subject(s) - receptor , chemistry , hydrochloride , small intestine , medicine , pharmacology , biochemistry , biology

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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