Cassis L, Ludwig J, Grohmann M, Trendelenburg U
Naunyn Schmiedebergs Arch Pharmacol. 1986 Jul;333(3):253-61. doi: 10.1007/BF00512938.
Two different "deaminating systems" were compared (i.e., intact tissues in which an uptake process translocates the 3H-catecholamine from the extracellular space to the intracellular MAO): the adrenergic nerve endings of the rat vas deferens exposed to 10 nmol/l 3H-(-)-noradrenaline, and the extraneuronal deaminating system of the rat heart perfused with 50 nmol/l 3H-(-)-adrenaline. Vesicular uptake and COMT were inhibited. In both systems MAO was partially inhibited by pargyline, and the steady-state tissue content of the 3H-catecholamine was determined as well as the steady-state rate of deamination. Rat vas deferens (preincubated with 10-40 nmol/l pargyline for 30 min). Inhibition of neuronal MAO caused not more than a moderate decrease of the steady-state rate of deamination of 3H-(-)-noradrenaline, but the steady-state tissue content was greatly increased. Determinations of the activity of MAO in homogenates of vasa deferentia showed that preincubation with 10 and 20 nmol/l pargyline inhibited the enzyme by 80 to 95%. Rat heart (of animals pretreated with 1 to 30 mg/kg pargyline). Inhibition of extraneuronal MAO caused a steep decline of the steady-state rate of deamination of 3H-(-)-adrenaline, but only a small rise in the steady-state tissue content. The decisive difference between the two deaminating systems lies in the fact that the ratio "kmao/kout" (where the two k-values characterize the activity of the unsaturated intracellular MAO and the ability of the 3H-catecholamine to leave the relevant cells, respectively) is much higher for the neuronal deaminating system exposed to 3H-(-)-noradrenaline than for the extraneuronal deaminating system exposed to 3H-(-)-adrenaline.(ABSTRACT TRUNCATED AT 250 WORDS)
对两种不同的“脱氨基系统”进行了比较(即完整组织,其中摄取过程将3H-儿茶酚胺从细胞外空间转运至细胞内单胺氧化酶):将大鼠输精管的肾上腺素能神经末梢暴露于10 nmol/L的3H-(-)-去甲肾上腺素中,以及用50 nmol/L的3H-(-)-肾上腺素灌注大鼠心脏的神经外脱氨基系统。抑制囊泡摄取和儿茶酚-O-甲基转移酶。在这两种系统中,单胺氧化酶均被帕吉林部分抑制,并测定了3H-儿茶酚胺的稳态组织含量以及脱氨基的稳态速率。大鼠输精管(用10 - 40 nmol/L帕吉林预孵育30分钟)。抑制神经元单胺氧化酶导致3H-(-)-去甲肾上腺素脱氨基的稳态速率仅适度降低,但稳态组织含量大幅增加。对输精管匀浆中单胺氧化酶活性的测定表明,用10和20 nmol/L帕吉林预孵育可使该酶抑制80%至95%。大鼠心脏(用1至30 mg/kg帕吉林预处理的动物)。抑制神经外单胺氧化酶导致3H-(-)-肾上腺素脱氨基的稳态速率急剧下降,但稳态组织含量仅小幅上升。这两种脱氨基系统的决定性差异在于,对于暴露于3H-(-)-去甲肾上腺素的神经元脱氨基系统,“kmao/kout”比值(其中两个k值分别表征不饱和细胞内单胺氧化酶的活性和3H-儿茶酚胺离开相关细胞的能力)比暴露于3H-(-)-肾上腺素的神经外脱氨基系统高得多。(摘要截断于250字)