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

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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

Fingerprint

Radioligand Assay
bopindolol
COS Cells
Propranolol
White Adipose Tissue
Adrenergic Receptors
Bupranolol
Pindolol
Metoprolol
Isoproterenol
Cell Membrane
Membranes
4-(2-hydroxy-3-tert-butylaminopropoxy)-2-methylindole
BRL 37344
3-(2-ethylphenoxy)-1-(1,2,3,4-tetrahydronaphth-1-ylamino)-2-propanol oxalate
4-(3-tert-butylamino-2-hydroxypropoxy)-2-carboxyindole

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Binding studies of β-adrenoceptor agonists and antagonists in COS-7 cells expressing human β3-adrenoceptors by radioligand binding assay. / Hanaoka, Yoko; Nakamura, Takashi; Ahmed, Maruf; Kurose, Hitoshi; Nagao, Taku; Nagatomo, Takafumi.

In: Pharmacology Reviews and Communications, Vol. 11, No. 4, 01.12.2001, p. 285-290.

Research output: Contribution to journalArticle

Hanaoka, Yoko ; Nakamura, Takashi ; Ahmed, Maruf ; Kurose, Hitoshi ; Nagao, Taku ; Nagatomo, Takafumi. / Binding studies of β-adrenoceptor agonists and antagonists in COS-7 cells expressing human β3-adrenoceptors by radioligand binding assay. In: Pharmacology Reviews and Communications. 2001 ; Vol. 11, No. 4. pp. 285-290.
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