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仔猪窦房结5-羟色胺受体类似于人类心房5-HT4样受体。

Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors.

作者信息

Kaumann A J

机构信息

Smith Kline Beecham Pharmaceuticals, Frythe, Welwyn, Hertfordshire, UK.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1990 Nov;342(5):619-22. doi: 10.1007/BF00169055.

Abstract

5-Hydroxytryptamine (5-HT), 5-carboxamidotryptamine (5-CT) and the gastrointestinal kinetic benzamides renzapride and cisapride caused tachycardia in spontaneously beating right atria of piglet in the presence of 400 nmol/l (+/-)-propranolol and 6 mumol/l cocaine. The maximum tachycardia caused by agonists, compared to that evoked by 200 mumol/l (-)-isoprenaline, was 63% for 5-HT, 50% for 5-CT, 50% for renzapride and 28% for cisapride. The rank order of potency was 5-HT greater than renzapride greater than cisapride greater than 5-CT. The effects of the agonists, but not those of (-)-isoprenaline, were antagonised by 3 alpha-tropanyl-1H-indole-3-carboxylic acid (ICS 205930); the pKB of ICS 205930 (vs 5-HT) was 6.9. These characteristics suggest that piglet sinoatrial 5-HT receptors are similar to "so-called" 5-HT4 receptors previously described in mouse colliculi neurons. Piglet sinoatrial 5-HT4-like receptors resemble the human atrial 5-HT receptors that mediate positive inotropic effects of 5-HT.

摘要

在存在400 nmol/l(±)-普萘洛尔和6 μmol/l可卡因的情况下,5-羟色胺(5-HT)、5-羧酰胺色胺(5-CT)以及胃肠动力性苯甲酰胺类药物伦扎必利和顺阿普唑仑在仔猪自主跳动的右心房中引起心动过速。与200 μmol/l(-)-异丙肾上腺素诱发的心动过速相比,激动剂引起的最大心动过速,5-HT为63%,5-CT为50%,伦扎必利为50%,顺阿普唑仑为28%。效价顺序为5-HT>伦扎必利>顺阿普唑仑>5-CT。激动剂的作用,而非(-)-异丙肾上腺素的作用,被3α-托烷-1H-吲哚-3-羧酸(ICS 205930)拮抗;ICS 205930(相对于5-HT)的pKB为6.9。这些特征表明,仔猪窦房结5-HT受体类似于先前在小鼠丘脑中神经元中描述的“所谓”5-HT4受体。仔猪窦房结5-HT4样受体类似于介导5-HT正性肌力作用的人心房5-HT受体。

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