Molecular Characterization of Pharmacological Properties and Selectivity of SWR-0315NA for β_3-Adrenoceptors (Pharmacology)

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概要

• 論文の詳細を見る

• The pharmacological properties of SWR-0315NA, (E,Z)-[4[[1-[2-[(3-phenoxy-2-hydroxy propyl)]amino]-ethyl]-1-propenyl]phenoxy]acetic acid sodium, were compared with those of (-)-isoproterenol. In the radioligand binding studies of [^<125>I]iodocyanopindolol with COS-7 cell membranes that transiently expressed human β-adrenoceptor (β-AR) subtypes, SWR-0315NA exhibited 1-fold and 2-fold greater binding affinities for β_3-AR than those for β_1- and β_2-ARs, respectively. The maximal stimulatory effects of SWR-0315NA on cAMP accumulation in CHO cells expressing all the β-AR subtypes were 79%, 3% and 93% for β_1-, β_2- and β_3-ARs of those produced by (-)-isoproterenol, respectively. SWR-0315NA has 26.3-fold and more than 630-fold greater selectivity for β_3-AR than those for β_1- and β_2-ARs in potency, respectively. These results indicate that although SWR-0315NA has lower binding selectivity towards β-AR subtypes, it is a selective agonist with high intrinsic activity for β_3-AR as compared with (-)-isoproterenol.

• 公益社団法人日本薬学会の論文
• 2004-05-01

著者

• NAGATOMO Takafumi

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

• Ahmed Maruf

  Pharmacy Department University Of Rajshahi

• Ahmed Maruf

  バングラデシュ

• Nagatomo T

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

• AHMED Maruf

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

• KISO Tatsuya

  Research Department, Sawai Pharmaceutical Co., Ltd.,

• KAKITA Takao

  Research Department, Sawai Pharmaceutical Co., Ltd.,

• OHTSUBO Yoshikazu

  Research Department, Sawai Pharmaceutical Co., Ltd.,

• Kiso Tatsuya

  Research Department Sawai Pharmaceutical Co. Ltd.

• HANAOKA Yoko

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

• Kakita T

  Research Department Sawai Pharmaceutical Co. Ltd.

• Hanaoka Yoko

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

• Nagatomo Takafumi

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

• Ohtsubo Yoshikazu

  Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.

• Namikawa Tomoko

  Biological Res. Dep. Sawai Pharmaceutical Co. Ltd.

• OHTSUBO Yoshikazu

  Research Department, Sawai Pharmaceutical Co. Ltd.

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