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异丙肾上腺素在犬类和人类体内的代谢。

Metabolism of isoprenaline in dog and man.

作者信息

Conolly M E, Davies D S, Dollery C T, Morgan C D, Paterson J W, Sandler M

出版信息

Br J Pharmacol. 1972 Nov;46(3):458-72. doi: 10.1111/j.1476-5381.1972.tb08143.x.

DOI:10.1111/j.1476-5381.1972.tb08143.x
PMID:4656607
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1666503/
Abstract
  1. The metabolism of isoprenaline has been studied in man and dog following intravenous and oral or intra-duodenal administration.2. Intravenous isoprenaline was excreted largely unchanged in urine in both species. Only one-third of the radioactivity in urine was in the form of the O-methyl metabolite.3. After oral doses in man or intraduodenal doses in dogs, plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine.4. Catechol-O-methyl transferase may be less important than Uptake(2) in limiting the pharmacological action of isoprenaline.5. Pharmacological response (heart-rate increase) was related to plasma concentration of isoprenaline only after rapid intravenous injections. In dogs, following prolonged infusion or intraduodenal doses, heart rate returned to base-line values when plasma concentrations of isoprenaline were high.
摘要
  1. 已在人和狗身上研究了静脉注射以及口服或十二指肠内给药后异丙肾上腺素的代谢情况。

  2. 静脉注射的异丙肾上腺素在这两个物种的尿液中大多以原形排出。尿液中只有三分之一的放射性是以O - 甲基代谢物的形式存在。

  3. 在人经口服给药或狗经十二指肠内给药后,血浆放射性几乎完全以结合型异丙肾上腺素的形式存在,且这种代谢物占尿液中放射性的80%以上。

  4. 在限制异丙肾上腺素的药理作用方面,儿茶酚 - O - 甲基转移酶可能不如摄取(2)重要。

  5. 仅在快速静脉注射后,药理反应(心率增加)才与血浆异丙肾上腺素浓度相关。在狗身上,长时间输注或十二指肠内给药后,当血浆异丙肾上腺素浓度很高时,心率会恢复到基线值。

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Metabolism of isoprenaline in dog and man.异丙肾上腺素在犬类和人类体内的代谢。
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Eur J Drug Metab Pharmacokinet. 1980;5(3):135-43. doi: 10.1007/BF03189457.

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本文引用的文献

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THE FATE OF 3H-ISO-PROTERENOL IN THE RAT.大鼠体内3H-异丙肾上腺素的代谢情况
Biochem Pharmacol. 1964 Aug;13:1119-28. doi: 10.1016/0006-2952(64)90112-1.
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Studies on the metabolism of catecholamines.儿茶酚胺代谢的研究。
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Separation of steroid sulfokinases.类固醇硫酸激酶的分离
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Studies on the metabolism of norepinephrine, epinephrine and their o-methyl analogs by partially purified enzyme preparations.用部分纯化的酶制剂对去甲肾上腺素、肾上腺素及其邻甲基类似物的代谢研究。
Arch Biochem Biophys. 1958 Oct;77(2):417-27. doi: 10.1016/0003-9861(58)90089-4.
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The chemical estimation of adrenaline-like substances in blood.血液中肾上腺素样物质的化学测定。
Biochem J. 1952 Jun;51(3):311-8. doi: 10.1042/bj0510311.
6
Separation of catecholamines and metanephrine and normetanephrine using a weak cation-exchange resin.使用弱阳离子交换树脂分离儿茶酚胺、变肾上腺素和去甲变肾上腺素。
Anal Biochem. 1965 Jun;11(3):575-9. doi: 10.1016/0003-2697(65)90075-8.
7
Absorption and elimination profile of isoproterenol. 3. The metabolic fate of dl-isoproterenol-7-3H in the dog.异丙肾上腺素的吸收与消除情况。3. 犬体内消旋异丙肾上腺素-7-³H的代谢命运。
J Pharm Sci. 1968 Jul;57(7):1135-41. doi: 10.1002/jps.2600570710.
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Digital heart rate meter.数字心率计。
Cardiovasc Res. 1971 Jan;5(1):157-60. doi: 10.1093/cvr/5.1.157.
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The inactivation of noradrenaline and isoprenaline in dogs.狗体内去甲肾上腺素和异丙肾上腺素的失活
Br J Pharmacol. 1970 Jul;39(3):573-84. doi: 10.1111/j.1476-5381.1970.tb10365.x.
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The role of uptake2 in the extraneuronal metabolism of catecholamines in the isolated rat heart.摄取2在离体大鼠心脏儿茶酚胺的非神经元代谢中的作用。
Br J Pharmacol. 1969 Nov;37(3):638-49. doi: 10.1111/j.1476-5381.1969.tb08502.x.