.BETA.-Carbolines selectively antagonize the cholecystokinin action in isolated guinea-pig gallbladder muscle.
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概要
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Two β-carbolines, methyl β-carboline-3-carboxylate (β-CCM) and ethyl β-carboline-3-carboxylate (β-CCE), caused the parallel shift of the doseresponse curve for cholecystokinin (CCK) in isolated guinea-pig gallbladder muscle. The Schild plot regarding the parallel shift in the dose-response curves had a regression line with a slope of 1.03 and a pA<SUB>2</SUB> value of 5.17 for β-CCE, while the method of van Rossum gave a pA<SUB>2</SUB> value of 5.24 for β-CCE and 5.53 for β-CCM. Both the β-carbolines protected CCK receptors in the gallbladder muscle from alkylation by dibenamine, but β-CCM did not protect acetylcholine receptors from dibenamine alkylation. These results suggest that 9-CCM and 3-CCE, so-called inverse agonists of benzodiazepines (BZP), antagonize the CCK action in the gallbladder muscle in a competitive manner, and the antagonism takes place at CCK receptor sites. No spare receptors for CCK were found in the guinea-pig gallbladder muscle.
- 公益社団法人 日本薬理学会の論文
著者
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Kubota Kazuhiko
Department Of Pharmacology Faculty Of Pharmaceutical Science Science University Of Tokyo
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Itonaga Masahiro
Department Of Gastroenterology Kyoto Second Red Cross Hospital
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- .BETA.-Carbolines selectively antagonize the cholecystokinin action in isolated guinea-pig gallbladder muscle.