Koike K, Takayanagi I
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Arch Int Pharmacodyn Ther. 1988 Nov-Dec;296:184-91.
Single smooth muscle cells were prepared from guinea-pig taenia caecum. To study the beta-adrenoceptors in the single cells, we observed mechanical responses of the single cells to beta-adrenergic drugs and also tested the binding of a [3H]-labelled drug to the single cells. The single cells showed a graded relaxing response to isoprenaline. The concentration-response curve was shifted in a parallel fashion by propranolol, indicating a competitive antagonism. The pA2 value of propranolol was in agreement with that estimated using the intact tissue. The dissociation constant of [3H]-dihydroalprenolol was similar to the value estimated in the microsomal fractions. The apparent dissociation constants of isoprenaline and propranolol estimated from inhibition of the specific binding of [3H]-dihydroalprenolol to the single cells were also in agreement with the values in the microsomal fractions. The results suggest that there is no change in the beta-adrenoceptor mechanism in single smooth muscle cells by isolating the cells.
从豚鼠盲肠带制备单个平滑肌细胞。为研究单细胞中的β-肾上腺素能受体,我们观察了单细胞对β-肾上腺素能药物的机械反应,并检测了一种[3H]标记药物与单细胞的结合情况。单细胞对异丙肾上腺素呈现出分级舒张反应。普萘洛尔使浓度-反应曲线平行移动,表明存在竞争性拮抗作用。普萘洛尔的pA2值与使用完整组织估算的值一致。[3H]-二氢阿普洛尔的解离常数与微粒体部分估算的值相似。从[3H]-二氢阿普洛尔与单细胞特异性结合的抑制情况估算的异丙肾上腺素和普萘洛尔的表观解离常数也与微粒体部分的值一致。结果表明,通过分离细胞,单个平滑肌细胞中的β-肾上腺素能受体机制没有变化。