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[3H]-(±)-异丙肾上腺素在新生小猫离体心房和冠状动脉中的代谢

Metabolism of [3H]-(+/-)-isoprenaline by isolated atria and coronary arteries of the kitten.

作者信息

Cornish E J, Goldie R G

出版信息

Br J Pharmacol. 1980 Mar;68(3):499-504. doi: 10.1111/j.1476-5381.1980.tb14564.x.

Abstract

1 Isolated coronary arteries of the kitten accumulated more unchanged isoprenaline and metabolized more amine than atria following incubation for 1 to 20 min with [3H]-(+/-)-isoprenaline (25 ng/ml or 5 micrograms/ml). 2 Cortisol (10 or 80 microM), U-0521 (120 microM) and oxytetracycline (100 microM) all reduced metabolite formation. 3 Cortisol inhibited 'Iso InfluxMin' (cellular isoprenaline accumulation plus total metabolite production). In contrast, it increased, decreased or did not alter accumulation of unmetabolized isoprenaline, depending upon the experimental conditions. 4 Isoprenaline accumulation was increased in atria and reduced in coronary arteries by U-0521, while oxytetracycline reduced accumulation in coronary arteries at the high amine concentration. 5 It is concluded that in atria, cortisol inhibits metabolism and has differential effects on a number of extraneuronal compartments which accumulate isoprenaline. Both cortisol and U-0521 appear to be extraneuronal uptake inhibitors and inhibitors of catechol-O-methyltransferase in coronary arteries. Oxytetracycline may have effects additional to inhibition of isoprenaline binding to connective tissue fibres.

摘要
  1. 将小猫的离体冠状动脉与[3H] -(±)-异丙肾上腺素(25纳克/毫升或5微克/毫升)孵育1至20分钟后,其积累的未变化异丙肾上腺素比心房更多,且代谢的胺也更多。2. 皮质醇(10或80微摩尔)、U - 0521(120微摩尔)和土霉素(100微摩尔)均减少了代谢产物的形成。3. 皮质醇抑制“异丙肾上腺素流入最小值”(细胞内异丙肾上腺素积累加上总代谢产物生成)。相比之下,根据实验条件,它会增加、减少或不改变未代谢异丙肾上腺素的积累。4. U - 0521使心房中的异丙肾上腺素积累增加,冠状动脉中的积累减少,而在高胺浓度下,土霉素减少冠状动脉中的积累。5. 得出的结论是,在心房中,皮质醇抑制代谢,并对积累异丙肾上腺素的多个非神经细胞区室有不同影响。皮质醇和U - 0521似乎都是冠状动脉中非神经细胞摄取抑制剂和儿茶酚 - O - 甲基转移酶抑制剂。土霉素除了抑制异丙肾上腺素与结缔组织纤维的结合外,可能还有其他作用。

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本文引用的文献

8
Analysis of the compartments involved in the extraneuronal storage and metabolism of isoprenaline in the perfused heart.
Naunyn Schmiedebergs Arch Pharmacol. 1974;283(3):223-44. doi: 10.1007/BF00499185.
10

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