Molecular characterization of pharmacological properties of T-0509 for β-adrenoceptors

Yoji Sato, Hitoshi Kurose, Masafumi Isogaya, Taku Nagao

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

The pharmacological properties of T-0509, (-)-(R)-1-(3,4-dihydroxyphenyl)-2-[(3,4- dimethoxyphenethyl)amino]ethanol, were compared with those of isoproterenol. In the radioligand binding studies of [ 125 I]iodocyanopindolol with COS-7 cell membranes that transiently expressed β-adrenoceptor subtypes, T-0509 exhibited 11- and 97-fold greater K(i) values for β 2 - and β 3 -adrenoceptors, respectively, compared with β 1 -adrenoceptors. Affinities of β 2 - and β 3 -adrenoceptors to isoproterenol were 1.4- and 28-fold lower than that of β 1 -adrenoceptors, respectively. The maximal stimulatory effects of T-0509 on adenylyl cyclase of CHO-K1 (Chinese hamster ovary K1) cell membranes expressing β 1 - or β 2 -adrenoceptors were 85% or 96% of those produced by isoproterenol, respectively. These results indicate that T-0509 is a relatively specific β 1 -adrenoceptor agonist with a high intrinsic activity as compared with isoproterenol.

Original languageEnglish
Pages (from-to)363-367
Number of pages5
JournalEuropean Journal of Pharmacology
Volume315
Issue number3
DOIs
Publication statusPublished - Nov 21 1996
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Pharmacology

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