Sato Y, Kurose H, Isogaya M, Nagao T
Department of Toxicology and Pharmacology, Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
Eur J Pharmacol. 1996 Nov 21;315(3):363-7. doi: 10.1016/s0014-2999(96)00648-6.
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 [125I]iodocyanopindolol with COS-7 cell membranes that transiently expressed beta-adrenoceptor subtypes, T-0509 exhibited 11- and 97-fold greater Ki values for beta 2- and beta 3-adrenoceptors, respectively, compared with beta 1-adrenoceptors. Affinities of beta 2- and beta 3-adrenoceptors to isoproterenol were 1.4- and 28-fold lower than that of beta 1-adrenoceptors, respectively. The maximal stimulatory effects of T-0509 on adenylyl cyclase of CHO-K1 (chinese hamster ovary K1) cell membranes expressing beta 1- or beta 2-adrenoceptors were 85% or 96% of those produced by isoproterenol, respectively. These results indicate that T-0509 is a relatively specific beta 1-adrenoceptor agonist with a high intrinsic activity as compared with isoproterenol.
将(-)-(R)-1-(3,4-二羟基苯基)-2-[(3,4-二甲氧基苯乙基)氨基]乙醇（T-0509）的药理特性与异丙肾上腺素的药理特性进行了比较。在[125I]碘氰吲哚洛尔与瞬时表达β-肾上腺素能受体亚型的COS-7细胞膜的放射性配体结合研究中，与β1-肾上腺素能受体相比，T-0509对β2-和β3-肾上腺素能受体的Ki值分别高11倍和97倍。β2-和β3-肾上腺素能受体对异丙肾上腺素的亲和力分别比β1-肾上腺素能受体低1.4倍和28倍。T-0509对表达β1-或β2-肾上腺素能受体的CHO-K1（中国仓鼠卵巢K1）细胞膜腺苷酸环化酶的最大刺激作用分别为异丙肾上腺素产生作用的85%或96%。这些结果表明，与异丙肾上腺素相比，T-0509是一种具有高内在活性的相对特异性的β1-肾上腺素能受体激动剂。
