Cisapride, a gastroprokinetic agent, binds to 5-HT4 receptors.
-
- KATAYAMA Ken-ichi
- Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
- MORIO Yasunori
- Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
- HAGA Keiichiro
- Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
- FUKUDA Takemi
- Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
Bibliographic Information
- Other Title
-
- シサプリドの5‐HT4受容体への親和性
- シサプリド ノ 5-HT4 ジュヨウタイ エ ノ シンワセイ
Search this article
Abstract
The affinity of cisapride for 5-HT4 receptors was investigated in comparison with those of other 5-HT4 receptor agonists and antagonists, such as 5-HT, 5-MeOT, mosapride, zacopride, metoclopramide, BIMU8, GR113808, SDZ 205-557 and ICS 205-930. Cisapride and the other compounds dose-dependently inhibited specific 3H-GR 113808 binding to 5-HT4 receptors in guinea pig striatal membranes, and complete inhibition of specific 3H-GR1 13808 binding was achieved at the high concentrations of these compounds. Cisapride was 1.9-, 7.3-, 4.3-, 11 and 26-fold more potent than 5-HT, 5-MeOT, mosapride, zacopride and metoclopramide, respectively, in competing for 5-HT4 receptors. To determine the manner of interaction between cisapride and 5-HT4 receptors, Scatchard analysis of 3H-GR113808 specific binding to striatal membranes was performed. Cisapride increased the Kd value of 3H-GR 113808 in striatal membranes in a dose-dependent manner without any influence on the binding density (Bmax) of 3H-GR1 13808. These findings indicate that cisapride binds to 5-HT4 receptors competing with 3H-GR 113808 in guinea pig striatal membranes.
Journal
-
- Folia Pharmacologica Japonica
-
Folia Pharmacologica Japonica 105 (6), 461-468, 1995
The Japanese Pharmacological Society
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1390282679248877952
-
- NII Article ID
- 10005706788
-
- NII Book ID
- AN00198335
-
- COI
- 1:CAS:528:DyaK2MXmtlantrg%3D
-
- ISSN
- 13478397
- 00155691
-
- NDL BIB ID
- 3620374
-
- PubMed
- 7557734
-
- Text Lang
- ja
-
- Data Source
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- Abstract License Flag
- Disallowed