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磷脂酰胆碱类似物对α-肾上腺素能受体的阻断作用

Blockade of alpha-adrenergic receptors by analogues of phosphatidylcholine.

作者信息

Smith K A, Cornett L E, Norris J S, Byers L W, Muirhead E E

出版信息

Life Sci. 1982 Nov 1;31(18):1891-902. doi: 10.1016/0024-3205(82)90027-3.

DOI:10.1016/0024-3205(82)90027-3
PMID:6129556
Abstract

The experimental evidence reviewed in this article suggests that the kidneys may have an additional function in regulating blood pressure besides their role in controlling both blood volume by urine formation and the relative state of vasoconstriction by the renin-angiotensin system. That is, the kidneys may have an additional influence upon the vasculature of a hormonal vasodilating system. The interstitial cells of the renal medulla appear to be mediating this activity and lipid compounds have been extracted from the renal medulla which display depressor activity. One such compound, the antihypertensive polar renomedullary lipid (APRL), has been demonstrated to consist of specific alkyl ether analogues of phosphatidylcholine. The vascular responses to these compounds include vasodilation of both arterioles and venules, rapid lowering of arterial blood pressure with little or no tachycardia, increased depressor activity in hypertensive animals, and blockade of vascular smooth muscle alpha 1-adrenergic receptors. Most recently, APRL and a synthetic analogue, 1-0-octadecyl-2-acetyl-sn-glycero-3-phosphorylcholine, have been used to demonstrate alpha-adrenergic receptor blockade on a smooth muscle cell line (DDT1) by radioligand assays. This action may be due to the insertion of these compounds into cell membranes causing subsequent steric interactions and blockade of the alpha-adrenergic receptor.

摘要

本文所综述的实验证据表明,肾脏除了通过尿液生成控制血容量以及通过肾素 - 血管紧张素系统控制血管收缩的相对状态来调节血压外,可能还具有其他功能。也就是说,肾脏可能对一种激素性血管舒张系统的脉管系统有额外影响。肾髓质的间质细胞似乎在介导这一活动,并且已从肾髓质中提取出具有降压活性的脂质化合物。其中一种化合物,即抗高血压极性肾髓质脂质(APRL),已被证明由磷脂酰胆碱的特定烷基醚类似物组成。这些化合物引起的血管反应包括小动脉和小静脉的血管舒张、动脉血压快速下降且几乎没有心动过速、高血压动物的降压活性增加以及血管平滑肌α1 - 肾上腺素能受体的阻断。最近,APRL和一种合成类似物,1 - O - 十八烷基 - 2 - 乙酰 - sn - 甘油 - 3 - 磷酸胆碱,已被用于通过放射性配体测定法在平滑肌细胞系(DDT1)上证明α - 肾上腺素能受体阻断。这种作用可能是由于这些化合物插入细胞膜导致随后的空间相互作用以及α - 肾上腺素能受体的阻断。

相似文献

1
Blockade of alpha-adrenergic receptors by analogues of phosphatidylcholine.磷脂酰胆碱类似物对α-肾上腺素能受体的阻断作用
Life Sci. 1982 Nov 1;31(18):1891-902. doi: 10.1016/0024-3205(82)90027-3.
2
Analogs of phosphatidylcholine: alpha-adrenergic antagonists from the renal medulla.
Hypertension. 1981 Jul-Aug;3(4):460-70. doi: 10.1161/01.hyp.3.4.460.
3
Antihypertensive lipids from the kidney: alkyl ether analogs of phosphatidylcholine.来自肾脏的抗高血压脂质:磷脂酰胆碱的烷基醚类似物。
Fed Proc. 1981 Jun;40(8):2285-90.
4
The role of antihypertensive polar renomedullary lipid in the pathogenesis of hypertension.抗高血压极性肾髓质脂质在高血压发病机制中的作用。
Jpn Circ J. 1984 Feb;48(2):196-200. doi: 10.1253/jcj.48.196.
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Atropine lowers blood pressure in normotensive rats through blockade of alpha-adrenergic receptors.阿托品通过阻断α-肾上腺素能受体降低正常血压大鼠的血压。
Life Sci. 1981 Jan 19;28(3):315-22. doi: 10.1016/0024-3205(81)90739-6.
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Vasodilatation elicited by 5-HT1A receptor agonists in constant-pressure-perfused rat kidney is mediated by blockade of alpha 1A-adrenoceptors.
Eur J Pharmacol. 1991 Sep 4;202(1):33-44. doi: 10.1016/0014-2999(91)90250-t.
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Effect of alpha adrenergic receptor stimulation on integrated systemic venous bed.
Pflugers Arch. 1977 Sep 16;370(3):241-6. doi: 10.1007/BF00585533.
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Alpha 2-adrenergic receptors and calcium: alpha 2-receptor blockade in vascular smooth muscle as an approach to the treatment of hypertension.α2-肾上腺素能受体与钙:血管平滑肌中的α2受体阻断作为治疗高血压的一种方法。
Methods Find Exp Clin Pharmacol. 1990 Apr;12(3):213-25.
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[3H]Dihydroergocryptine binding to alpha adrenergic receptors in canine aortic membranes.[3H]双氢麦角隐亭与犬主动脉膜中α肾上腺素能受体的结合
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Interaction between alpha adrenergic and serotonergic activation of canine saphenous veins.犬隐静脉中α肾上腺素能与5-羟色胺能激活之间的相互作用。
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