A POSSIBLE MECHANISM OF ACTION OF A BETA-ADRENERGIC PARTIAL AGONIST (CARTEOLOL) IN GUINEA PIG TAENIA CAECUM
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概要
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Carteolol, 5-(3-tert-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril hydrochloride was found to be a beta-adrenergic partical agonist in the taenia caecum of guinea pig. Concentration response curves of carteolol and isoprenaline were parallelly shifted by propranolol (10^<-7> M) suggesting that site of action of both the drugs was the same beta-adrenoceptor. The pD_2-values of carteolol obtained from the concentration action curves in mechanical response and increase of tissue concentration of cyclic AMP were significantly different from its pA_2-value against isoprenaline and its pK_i-value (negative log of its apparent dissociation constant). A possible explanation of our observation would seem to be as follows. Carteolol and isopranaline interact with the same beta-adrenoceptor where there may be two different sites : a binding site for agonist and binding site for antagonist.
- 公益社団法人日本薬学会の論文
著者
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TAKAYANAGI Issei
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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KOIKE Katsuo
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Takayanagi Issei
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo:(correspo
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