Abrahamsen J, Nedergaard O A
Blood Vessels. 1985;22(1):32-46.
The accumulation of (-)-3H-adrenaline (3H-A) by rabbit isolated aorta was studied. In all experiments, monoamine oxidase and catechol-O-methyltransferase were inhibited by treatment with pargyline and 3',4'-dihydroxy-2-methyl-propiophenone (U-0521), respectively. The relationship between the accumulation of 3H derived from 3H-A (10(-8) M) and the duration of incubation (0-3 h) was linear. The 3H-accumulation after 3 h incubation was 22.5 ml X g-1. In reserpine-treated tissue, the 3H-accumulation levelled off after 30 min and was 8.5 ml X g-1 after 3 h. The concentration of 3H-A or (-)-3H-noradrenaline (3H-NA) and the 3H-accumulation (ml X g-1) were inversely related. At 10(-8) M, the 1-hour accumulation of 3H derived from 3H-A and 3H-NA was 7.8 and 15.2 ml X g-1, respectively. With increasing concentrations (3 X 10(-8)-10(-4) M), the accumulation values approached each other. At 10(-4) M, the accumulation was 2.3 and 2.8 ml X g-1 for 3H-A and 3H-NA, respectively. The accumulation of 3H derived from 3H-A (10(-8)-10(-4) M) by reserpine-treated tissue also showed an inverse relationship with concentration: 5.4 ml X g-1 (10(-8) M) and 2.6 ml X g-1 (10(-4) M). The accumulation of 3H derived from 3H-A (10(-8) M; 1 h) was dependent on the bath temperature (1-37 degrees C). The accumulation increased continuously from 1.1 ml X g-1 (1 degree C) to 11.1 ml X g-1 (37 degrees C). Storage of tissue (0-5 days in salt solution without equilibration with 95% O2/5% CO2; 4 degrees C) did not affect the accumulation of 3H derived from 3H-A (10(-8) M; 1 h). Thereafter (7-14 days), the accumulation decreased. The inhibitory potency (IC50;-log M) of desimipramine, cocaine, (-)-propranolol, (-)-isoprenaline, and (+/-)-normetanephrine on accumulation of 3H derived from 3H-A (10(-8) M; 1 h) was found to be 8.26; 6.50; 5.48, 4.88, and 4.02, respectively. The maximal degree of inhibition was almost the same for these drugs, while that of clonidine and corticosterone was 50 and 20%, respectively.(ABSTRACT TRUNCATED AT 400 WORDS)
研究了家兔离体主动脉对（-）-3H-肾上腺素（3H-A）的摄取。在所有实验中，分别用优降宁和3'，4'-二羟基-2-甲基苯丙酮（U-0521）处理以抑制单胺氧化酶和儿茶酚-O-甲基转移酶。来源于3H-A（10⁻⁸M）的3H摄取量与孵育时间（0 - 3小时）呈线性关系。孵育3小时后的3H摄取量为22.5 ml·g⁻¹。在利血平处理的组织中，3H摄取在30分钟后趋于平稳，3小时后为8.5 ml·g⁻¹。3H-A或（-）-3H-去甲肾上腺素（3H-NA）的浓度与3H摄取量（ml·g⁻¹）呈负相关。在10⁻⁸M时，来源于3H-A和3H-NA的3H 1小时摄取量分别为7.8和15.2 ml·g⁻¹。随着浓度增加（3×10⁻⁸ - 10⁻⁴M），摄取值逐渐接近。在10⁻⁴M时，3H-A和3H-NA的摄取量分别为2.3和2.8 ml·g⁻¹。利血平处理的组织对来源于3H-A（10⁻⁸ - 10⁻⁴M）的3H摄取也与浓度呈负相关：（10⁻⁸M时为5.4 ml·g⁻¹，10⁻⁴M时为2.6 ml·g⁻¹）。来源于3H-A（10⁻⁸M；1小时）的3H摄取量取决于浴温（1 - 37℃）。摄取量从1.1 ml·g⁻¹（1℃）持续增加到11.1 ml·g⁻¹（37℃）。组织储存（在无95% O₂/5% CO₂平衡的盐溶液中于4℃保存0 - 5天）不影响来源于3H-A（10⁻⁸M；1小时）的3H摄取。此后（7 - 14天），摄取量下降。发现地昔帕明、可卡因、（-）-普萘洛尔、（-）-异丙肾上腺素和（±）-去甲变肾上腺素对来源于3H-A（10⁻⁸M；1小时）的3H摄取的抑制效力（IC₅₀；-log M）分别为8.26；6.50；5.48、4.88和4.02。这些药物的最大抑制程度几乎相同，而可乐定和皮质酮的最大抑制程度分别为50%和20%。（摘要截短于400字）
