Nunes J P, Vaz-Da-Silva M J, Brandão F, Guimarães S
Department of Pharmacology, Faculty of Medicine, Porto, Portugal.
Arch Int Pharmacodyn Ther. 1987 Oct;289(2):189-97.
Using the oil immersion technique, the role of neuronal uptake, monoamine oxidase and COMT in the inactivation of 2 concentrations (0.23 and 2.3 mumol/l) of noradrenaline and adrenaline was determined by the prolongation of the inactivation time caused by cocaine (12 mumol/l), pargyline (1 mmol/l) and U-0521 (50 mumol/l), respectively. The results obtained allow us to conclude that: 1) as previously shown, for the saphenous vein and mesenteric artery, noradrenaline is inactivated more rapidly than adrenaline; 2) in all tissues and for both concentrations of noradrenaline and adrenaline, neuronal uptake is more important for the inactivation of noradrenaline than for that of adrenaline, while O-methylation is more important for the inactivation of adrenaline than for that of noradrenaline. The only exception is that in the renal artery, O-methylation is very clearly the most important pathway of inactivation for both concentrations of both amines.
采用油浸技术,通过分别使用可卡因(12 μmol/L)、帕吉林(1 mmol/L)和U - 0521(50 μmol/L)导致失活时间延长,来确定神经元摄取、单胺氧化酶和儿茶酚 - O - 甲基转移酶在两种浓度(0.23和2.3 μmol/L)去甲肾上腺素和肾上腺素失活中的作用。所得结果使我们得出以下结论:1)如先前在隐静脉和肠系膜动脉中所显示的那样,去甲肾上腺素比肾上腺素失活更快;2)在所有组织中,对于两种浓度的去甲肾上腺素和肾上腺素而言,神经元摄取在去甲肾上腺素失活中比在肾上腺素失活中更重要,而O - 甲基化在肾上腺素失活中比在去甲肾上腺素失活中更重要。唯一的例外是在肾动脉中,对于两种胺的两种浓度而言,O - 甲基化非常明显是最重要的失活途径。