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鲨肝醇作为一种口服抗高血压药物:初步报告。

Selachyl alcohol as an oral antihypertensive agent: a preliminary note.

作者信息

Muirhead E E, Byers L W, Brooks B, Pitcock J A, Brown P, Dowell R

机构信息

Department of Pathology, University of Tennessee, Memphis.

出版信息

Am J Med Sci. 1987 Nov;294(5):384-7. doi: 10.1097/00000441-198711000-00014.

Abstract

Selachyl alcohol (SA) is a mono-oleyl glyceryl ether. It has certain biologic activities similar to those of the antihypertensive neutral renomedullary lipid (ANRL) derived from the renal papilla and its renomedullary interstitial cells (RIC). These include a vaso-depressor effect following bolus injection and a requirement for hepatic activation for the development of biological activity. In view of this similarity to ANRL, it appeared worthwhile to test the antihypertensive action of SA when given via the GI tract. Accordingly, pure SA was given either by gavage or by tube into the stomach or duodenum of one-kidney, one-clip hypertensive rats (5-10 mg per dose). The role of hepatic activation was demonstrated by comparing the BP response to bolus injection of SA and ANRL with and without the presence of an intact circulation to the liver. Administration of SA via the GI tract resulted in a significant decline in BP without tachycardia or weight loss. In the absence of a circulation to the liver, neither SA nor ANRL was active. SA appears to be an effective antihypertensive agent when given via the GI tract.

摘要

鲨肝醇(SA)是一种单油酰甘油醚。它具有某些与源自肾乳头及其肾髓质间质细胞(RIC)的降压中性肾髓质脂质(ANRL)相似的生物活性。这些活性包括推注注射后的血管降压作用以及生物活性的发挥需要肝脏激活。鉴于与ANRL的这种相似性,测试经胃肠道给予SA时的降压作用似乎是值得的。因此,将纯SA通过灌胃或经导管注入一侧肾、单夹高血压大鼠的胃或十二指肠(每剂量5 - 10毫克)。通过比较在有和没有完整肝循环的情况下推注SA和ANRL后的血压反应,证明了肝脏激活的作用。经胃肠道给予SA导致血压显著下降,且无心动过速或体重减轻。在没有肝循环的情况下,SA和ANRL均无活性。经胃肠道给予时,SA似乎是一种有效的降压药。

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