Assessment of β_2- and β_3-Adrenoceptors in Rat White Adipose Tissues by Radioligand Binding Assay

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概要

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• We investigated the characteristics of β-adrenoceptors (β-ARs) in rat white adipose tissues (WAT) with a radioligand receptor binding assay using (-)-[^3H]-CGP12177. Scatchard analysis revealed that there are high- and low-affinity sites for (-)-[^3H]-CGP12177 in WAT. The (-)-[^3H]-CGP12177 bound to a high-affinity site was displaced by 1 μM propranolol. The rank of pK_i values of catecholamines for the site was isoproterenol>epinephrine>norepinephrine. By contrast, BRL37344A, BRL35135A and SR59230A, β_3-selective agonists had high affinity for the low-affinity site of (-)-[^3H]-CGP12177,whereas (-)-[^3H]-CGP12177 bound to a low-affinity site was completely displaced by 100 μM bupranolol but not 1 μM propranolol. The pK_i values of the catecholamines (isoproterenol, norepinephrine, epinephrine) for this site were very low. In addition, the correlation between the pK_i values of various β-agonists for the low-affinity site of rat WAT and those obtained from rat cloned β_3-ARs was significant, but those of human cloned β_3-ARs were not. Consequently, the results suggested that the high- and low-affinity sites were β_2-ARs and β_3-ARs in rat WAT, respectively.

• 公益社団法人日本薬学会の論文
• 1997-02-15

著者

• NAGATOMO Takafumi

  Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences

• 杉山 憲司

  Faculty Of Pharmaceutical Sciences Osaka University

• Hattori K

  Niigata Coll. Pharmacy Niigata Jpn

• Hattori Kaoru

  Department Of Cardiology Miki City Hospital

• Hattori Kaoru

  新潟薬科大学 薬理

• KUBO Satoshi

  Department of Neurosurgery, Kyoto Second Red Cross Hospital

• Kubo Satoshi

  Department Of Biomass Chemistry Forestry And Forest Products Research Institute

• Nagatomo T

  Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Niigata Univ. Of Pharmacy And Applied Life Scie

• OHNUKI Toshio

  Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and A

• 大貫 敏男

  新潟薬科大学薬理学教室

• Ohnuki Toshio

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Ohnuki Toshio

  Department Of Pharmacology Nilgata College Of Pharmacy

• MATSUDA Aritomo

  Department of Pharmacology, Niigata College of Pharmacy

• SUZUKI Jun

  Therapeutic Product Development, Amgen, Limited

• Matsuda Aritomo

  Department Of Pharmacology Niigata College Of Pharmacy

• Suzuki J

  Department Of Electrical And Electronic Engineering Tokyo Institute Of Technology

• Hattori K

  Tohoku Univ. Sendai Jpn

• Nagatomo Takafumi

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Sugiyama K

  Department Of Pharmacology Niigata College Of Pharmacy

• 大貫 敏男

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App

• Ohnuki Toshio

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Hokkaido University

• Kubo S

  Department Of Pharmacology Niigata College Of Pharmacy

• Namikawa Tomoko

  Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.

• Kubo Satoshi

  Department Of Biological And Environmental Science Faculty Of Agriculture Graduate School Of Agricul

• Hattori Kaoru

  Department of Pharmacology, Niigata College of Pharmacy

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