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二氮嗪类似物对正常血压和自发性高血压大鼠主动脉反应性的作用。

The action of diazoxide analogs on aortic reactivity in normotensive and spontaneously hypertensive rats.

作者信息

Chona S, Triggle D J

出版信息

Can J Physiol Pharmacol. 1977 Apr;55(2):153-60. doi: 10.1139/y77-023.

Abstract

Diazoxide and four related 1,2,4-benzothiadiazines reduced the maximum responses to noradrenaline (NA) and KCl in aortic rings from normotensive and spontaneously hypertensive rats (SHR). These agents were more active against NA than against KCl responses, and more effective against either NA or KCl responses in aortae from hypertensive animals. Further studies with V (3-cyclopentenyl-6,7-dichloro-1,2,4-benzothiadiazine-1,1-dioxide), the most active member of the series, showed it to be significantly more effective against NA responses; when calcium was added to calcium-free solutions containing eith NA or KCl, V was more effective in inhibiting either response in SHR aortae and was about 100 times more effective in inhibiting the calcium-NA responses. These data are consistent with previous findings that vascular smooth muscle from normotensive and SHR differs in sensitivity to diazoxide. However, the site(s) at which this difference is exhibited remains to be elucidated.

摘要

二氮嗪及四种相关的1,2,4-苯并噻二嗪降低了正常血压大鼠和自发性高血压大鼠(SHR)主动脉环对去甲肾上腺素(NA)和氯化钾(KCl)的最大反应。这些药物对NA反应的作用比对KCl反应的作用更强,且对高血压动物主动脉中NA或KCl反应的作用更有效。对该系列中活性最强的成员V(3-环戊烯基-6,7-二氯-1,2,4-苯并噻二嗪-1,1-二氧化物)的进一步研究表明,它对NA反应的作用明显更有效;当向含有NA或KCl的无钙溶液中添加钙时,V在抑制SHR主动脉中的任何一种反应方面更有效,并且在抑制钙-NA反应方面的效力约高100倍。这些数据与先前的研究结果一致,即正常血压大鼠和SHR的血管平滑肌对二氮嗪的敏感性不同。然而,这种差异表现的位点仍有待阐明。

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