Binding studies of β-adrenoceptor agonists and antagonists in COS-7 cells expressing human β3-adrenoceptors by radioligand binding assay

Yoko Hanaoka, Takashi Nakamura, Maruf Ahmed, Hitoshi Kurose, Taku Nagao, Takafumi Nagatomo

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

The present study reports the assessment of the affinities of some β-adrenoceptor (β-AR) agonists and antagonists like isoproterenol, BRL 37344, bupranolol, SR-59230A, metoprolol, pindolol, propranolol, bopindolol and its two metabolites (18-502 and 20-785) to β3-AR using the membranes of cloned COS-7 cells by the radioligand binding assay. The β1- and β2-AR non-selective antagonists, propranolol and 18-502 showed high affinities to β3-ARs and the pKi values of propranolol, bopindolol and its two metabolites (18-502 and 20-785) to this subtype were, 7.70, 6.99, 8.03 and 6.48 respectively. The rank order of pKi values for these agents to β3-ARs in COS-7 cell membranes was, however, different from those to β1- and β2-ARs. Only BRL-37344 and SR-59230A tested here, being selective β3-AR agonist and antagonist respectively, showed higher binding affinity towards β3-AR of rat white adipose tissue (WAT). Thus. the present study suggests that the non-selective antagonists, propranolol and 18-502, possess the high ability of binding with β3-AR in cloned COS-7 cells as well as WAT, although different affinities of BRL-37344 and SR-59230A to β3-AR from those to WAT were observed.

Original languageEnglish
Pages (from-to)285-290
Number of pages6
JournalPharmacology Reviews and Communications
Volume11
Issue number4
Publication statusPublished - Dec 1 2001
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmacology

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