Desensitization and Selective Down - Regulation of Rat Cardiac β_1 - Adrenoceptors by Prolonged In Vivo Infusion of T - 0509, a β_1 - Adrenoceptor Full Agonist

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概要

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• We studied the effects of prolonged infusion of a selective β<SUB>1</SUB>-adrenoceptor (β<SUB>1</SUB>AR) full agonist, T-0509 [(-)-(<I>R</I>)-1-(3, 4-dihydroxyphenyl)-2-[(3, 4-dimethoxyphenethyl)amino]ethanol hydrochloride], with regard to its inotropic effect in vivo and cardiac βAR density. The results were compared with those for isoproterenol. Continuous infusion of isoproterenol at doses of 2.5-40 μg/kg/hr, s.c. for 6 days shifted the dose-response curves of isoproterenol (i.v.) for LVdP/dt<SUB>max</SUB> to the right and increased the ED<SUB>50</SUB> values up to fourfold. Isoproterenol infusion at 40 μg/kg/hr reduced the density of both β<SUB>1</SUB>- and β<SUB>2</SUB>ARs by 36010 and 43070 respectively, in left ventricular membranes. Following 6-day infusion of T-0509 at doses sufficient to induce a positive inotropic effect (5-40 μg/kg/hr), the ED<SUB>50</SUB> value of T-0509 (i.v.) for LVdP/dt<SUB>max</SUB> was also increased up to fourfold. In contrast to isoproterenol, infusion of T-0509 caused selective down-regulation of β<SUB>1</SUB>ARs by 30% without changing the number of β<SUB>2</SUB>ARs. These results indicate that long-term application of a selective β<SUB>1</SUB>AR full agonist causes desensitization to its inotropy in vivo, with subtype-selective down-regulation of β<SUB>1</SUB>ARs in cardiac ventricles.

• 社団法人 日本薬理学会の論文
• 1995-12-01

著者

• 佐藤 陽治

  国立医薬品食品衛生研究所 遺伝子細胞医薬部

• 佐藤 陽治

  国立医薬品食品衛生研究所

• Nagao Taku

  Division Of Cellular And Gene Therapy Products National Institute Of Health Sciences

• Nagao Taku

  Department Of Toxicology And Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo

• Imai Kazuhiro

  Department Of Aeronautics And Astronautics School Of Engineering University Of Tokyo:(present Addres

• Prados Pablo

  Department Of Analytical Chemistry Faculty Of Pharmaceutical Sciences University Of Tokyo

• Sato Yoji

  Division Of Cellular And Gene Therapy Products National Institute Of Health Sciences

• Sato Yoji

  National Institute Of Health Sciences

• SATO Yoji

  Department of Toxicology and Pharmacology,Faculty of Pharmaceutical Sciences, University of Tokyo

• ADACHI-AKAHANE Satomi

  Department of Taxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo

• Imai Kazuhiro

  Department Of Analytical Chemistry Faculty Of Pharmaceutical Sciences University Of Tokyo

• 佐藤 陽治

  Division Of Cellular And Gene Therapy Products National Institute Of Health Sciences

• Adachi-akahane Satomi

  Department Of Taxicology And Pharmacology Faculty Of Pharmaceutical Sciences University Of Tokyo

• Adachi-Akahane Satomi

  Department of Pharmacology, School of Medicine, Faculty of Medicine, Graduate School of Medical Sciences, Toho University

• Adachi-Akahane Satomi

  Department of Pharmacology, Faculty of Medicine, Toho University

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