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邻、间、对章鱼胺的肾上腺素能活性。

Adrenergic activity of ortho-, meta-, and para-octopamine.

作者信息

Fregly M J, Kelleher D L, Williams C M

出版信息

Pharmacology. 1979;18(4):180-7. doi: 10.1159/000137250.

Abstract

DL-o-, and p-octopamine were tested for beta- and alpha-adrenergic activity in rats. When compared to DL-isoproterenol, a beta-adrenergic agonist, all three isomers failed to show significant beta-adrenergic activity as assessed by intiation of thirst and by increase in tail skin temperature. All three isomers increased mean blood pressure in pentolinium-blocked rats. Of the three isomers, m-octopamine possessed the greatest alpha-adrenergic activity. When the responses were compared with those induced by L-norepinephrine, the order of activities was: 1:0.01 :0.0005 :0.0007 for norepinephrine, m-, p- and o-octopamine, respectively. Thus, DL-m-octopamine has about 1/100th the alpha-adrenergic activity of L-norepinephrine.

摘要

对大鼠测试了DL - 邻 - 、间 - 和对 - 章鱼胺的β - 和α - 肾上腺素能活性。与β - 肾上腺素能激动剂DL - 异丙肾上腺素相比,通过引发口渴和尾部皮肤温度升高评估,所有三种异构体均未显示出显著的β - 肾上腺素能活性。所有三种异构体均使泮库溴铵阻断的大鼠平均血压升高。在这三种异构体中,间 - 章鱼胺具有最强的α - 肾上腺素能活性。当将这些反应与L - 去甲肾上腺素诱导的反应进行比较时,活性顺序分别为:去甲肾上腺素、间 - 、对 - 和邻 - 章鱼胺为1:0.01 :0.0005 :0.0007。因此,DL - 间 - 章鱼胺的α - 肾上腺素能活性约为L - 去甲肾上腺素的1/100。

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