(+__-)-Pindolol Acts as a Partial Agonist at Atypical β-Adrenoceptors in the Guinea Pig Duodenum
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概要
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The agonistic and antagonistic effects of (±)-pindolol (1-(1H-indol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol) were estimated to clarify whether (±)-pindolol acts as a partial agonist on atypical β-adrenoceptors in the guinea pig duodenum. (±)-Pindolol induced concentration-dependent relaxation with a pD2 value of 5.10 ± 0.03 and an intrinsic activity of 0.83 ± 0.03. However, the relaxations to (±)-pindolol were not antagonized by the non-selective β1- and β2-adrenoceptor antagonist (±)-propranolol (1 μM). In the presence of (±)-propranolol (1 μM), the non-selective β1-, β2- and β3-adrenoceptor antagonist (±)-bupranolol (30 μM) induced a rightward shift of the concentration-response curves for (±)-pindolol (apparent pA2 = 5.41 ± 0.06). In the presence of (±)-propranolol, (±)-pindolol (10 μM) weakly but significantly antagonized the relaxant effects 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). These results demonstrate that (±)-pindolol possesses both agonistic and antagonistic effects on atypical β-adrenoceptors in the guinea pig duodenum.
- 社団法人 日本薬理学会の論文
- 2001-01-01
著者
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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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Horinouchi Takahiro
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Horinouchi Takahiro
Department Of Cellular Pharmacology Graduate School Of Medicine Hokkaido University
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HORINOUCHI Takahiro
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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