Partial Agonistic Effects of Carteolol on Atypical β-Adrenoceptors in the Guinea Pig Gastric Fundus
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概要
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The properties of the β1-/β2-adrenoceptor partial agonist carteolol were investigated in atypical β-adrenoceptors on the guinea pig gastric fundus. Carteolol induced concentration-dependent relaxation in this tissue (pD2=5.55, intrinsic activity=0.94). However, a combination of the selective β1-adrenoceptor antagonist atenolol (100 μM) and the selective β2-adrenoceptor antagonist butoxamine (100 μM) produced only small rightward shifts in the concentration-response curves of carteolol in the gastric fundus (pD2=4.91, intrinsic activity=0.94). In the presence of both atenolol (100 μM) and butoxamine (100 μM), the non-selective β1-, β2- and β3-adrenoceptor antagonist (±)-bupranolol (10-100 μM) caused a concentration-dependent right-ward shift of the concentration-response curves for carteolol in the guinea pig gastric fundus. Schild plot analyses of the effects of (±)-bupranolol against carteolol gave the pA2 value of 5.29 and the Schild slope was not significantly different from unity. Furthermore, carteolol (10 μM) weakly but significantly antagonized the relaxant responses to catecholamines ((−)-isoprenaline, (−)-noradrenaline and (−)-adrenaline), a selective β3-adrenoceptor agonist BRL37344 ((R*, R*)-(±)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]phenoxyacetic acid sodium salt) and a non-conventional partial β3-adrenoceptor agonist (±)-CGP12177A ([4-[3-[(1, 1-dimethylethyl)amino]-2-hydroxypropoxy]-1, 3-dihydro-2H-benzimidazol-2-one] hydrochloride) in the guinea pig gastric fundus. These results suggest that the partial agonistic effects of carteolol are mediated by atypical β-adrenoceptors in the guinea pig gastric fundus.
- 社団法人 日本薬理学会の論文
- 2000-11-01
著者
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Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Horinouchi Takahiro
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Horinouchi Takahiro
Department Of Cellular Pharmacology Hokkaido University Graduate School Of Medicine
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Horinouchi Takahiro
Department Of Cellular Pharmacology Graduate School Of Medicine Hokkaido University
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