Takayanagi I, Satoh M, Kokubu N, Kato T
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.
Can J Physiol Pharmacol. 1992 Apr;70(4):458-61. doi: 10.1139/y92-059.
An age-related change in potency of L-isoprenaline in the presence of ascorbic acid, desmethylimipramine, corticosterone, pargyline, and phentolamine was obtained in tracheal strips from guinea pigs of differing ages between 6 and 40 weeks. The potency in the strips from 100-week-old guinea pigs did not significantly differ from that in strips from 40-week-old animals. Single cells were prepared from the tracheal muscles of 6-, 10-, 40-, and 100-week-old guinea pigs. The specific binding of [3H]dihydroalprenolol to the single cells was saturable. The dissociation constants of [3H]dihydroalprenolol were in good agreement with those of the membrane fractions from the guinea-pig tracheal muscles, and did not change with age. An excellent relationship between the potency of L-isoprenaline and the maximum binding of [3H]dihydroalprenolol estimated in the preparations from 6- to 40-week-old guinea pigs was found, suggesting that the increase in the potency of L-isoprenaline is due to the increase in the maximum binding or receptor density. The value in the preparations from 100-week-old guinea pigs deviated significantly from the regression line. This suggests the possibility that the decrease in potency in the strips from 100-week-old animals is due to a change in post beta-receptor processes in responsiveness.
在6至40周龄不同的豚鼠气管条中,研究了在抗坏血酸、去甲丙咪嗪、皮质酮、帕吉林和酚妥拉明存在的情况下,L-异丙肾上腺素效价与年龄相关的变化。100周龄豚鼠气管条中的效价与40周龄动物气管条中的效价无显著差异。从6周龄、10周龄、40周龄和100周龄豚鼠的气管肌肉制备单细胞。[3H]二氢烯丙洛尔与单细胞的特异性结合是可饱和的。[3H]二氢烯丙洛尔的解离常数与豚鼠气管肌肉膜组分的解离常数高度一致,且不随年龄变化。在6至40周龄豚鼠制备物中,发现L-异丙肾上腺素效价与[3H]二氢烯丙洛尔最大结合量之间存在良好的关系,这表明L-异丙肾上腺素效价的增加是由于最大结合量或受体密度的增加。100周龄豚鼠制备物中的值明显偏离回归线。这表明100周龄动物气管条中效价降低可能是由于β受体后反应过程的变化。