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苯乙醇胺N-甲基转移酶抑制剂对大鼠肾上腺儿茶酚胺释放及排泄的影响。

The effects of an inhibitor of phenylethanolamine N-methyltransferase upon stimulated adrenal catecholamine release and excretion in the rat.

作者信息

Pendleton R G, Weiner G, Jenkins B, Gessner G

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1977 Apr;297(3):245-50. doi: 10.1007/BF00509268.

Abstract

SK&F 64139, an inhibitor of adrenal phenylethanolamine N-methyltransferase (PNMT), was found to significantly decrease 2-deoxy-D-glucose (2-DG) induced epinephrine excretion in the conscious rat under conditions where the former agent was administered chromically at 50 and 200 mg/kg/day over a 12-day period and 2-DG was administered after 3, 7 and 11 days of treatment. The reduced epinephrine output caused by SK&F 64139 in response to 2-DG was accompanied by an increased norepinephrine excretion pattern at 200 mg/kg/day of the compound. The reductions in epinephrine excretion were also associated with significant decreases in adrenal epinephrine and increases in the norepinephrine content.

摘要

SK&F 64139是一种肾上腺苯乙醇胺N-甲基转移酶(PNMT)抑制剂,发现在清醒大鼠中,当以50和200毫克/千克/天的剂量连续12天长期给予该药物,并在治疗3、7和11天后给予2-脱氧-D-葡萄糖(2-DG)时,它能显著降低2-DG诱导的肾上腺素排泄。在给予该化合物200毫克/千克/天的情况下,SK&F 64139对2-DG反应导致的肾上腺素输出减少,伴随着去甲肾上腺素排泄模式的增加。肾上腺素排泄的减少也与肾上腺肾上腺素的显著减少和去甲肾上腺素含量的增加有关。

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