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大鼠肾脏中咪唑啉优先结合位点与溶质排泄

Renal imidazoline preferring sites and solute excretion in the rat.

作者信息

Allan D R, Penner S B, Smyth D D

机构信息

Department of Internal Medicine, University of Manitoba, Winnipeg, Canada.

出版信息

Br J Pharmacol. 1993 Apr;108(4):870-5. doi: 10.1111/j.1476-5381.1993.tb13480.x.

Abstract
  1. Moxonidine has been found to have an approximately 600 fold greater affinity for I1 imidazoline preferring sites as compared to alpha 2-adrenoceptors in the rat kidney. The effects of an intrarenal infusion of moxonidine in an anaesthetized rat preparation were investigated and contrasted with the effects previously reported for alpha 2-adrenoceptor stimulation. 2. An intrarenal infusion of moxonidine (1, 3 and 10 nmol kg-1 min-1) produced an increase in urine flow rate and sodium excretion. Moxonidine increased urine volume through an increase in osmolar clearance rather than an increase in free water clearance as previously reported for alpha 2-adrenoceptor stimulation. 3. The effects of moxonidine also appeared to be unique from the effects of alpha 2-adrenoceptor stimulation. An imidazoline preferring site specific blocking dose of idazoxan (0.3 mg kg-1), but not an alpha 2-adrenoceptor specific blocking dose of rauwolscine (0.3 mg kg-1) attenuated the renal effects of moxonidine (3 nmol kg-1 min-1). Moreover, unlike alpha 2-adrenoceptor agonists, the effects of moxonidine were not altered by prior treatment with a V2 vasopressin receptor antagonist. 4. These results indicate differences between stimulation of alpha 2-adrenoceptors and I1 imidazoline preferring sites in the rat kidney and suggest a direct physiological function of renal imidazoline preferring sites.
摘要
  1. 已发现莫索尼定对大鼠肾脏中I1咪唑啉优先结合位点的亲和力比对α2肾上腺素能受体的亲和力高约600倍。研究了在麻醉大鼠制备物中肾内输注莫索尼定的作用,并与先前报道的α2肾上腺素能受体刺激的作用进行了对比。2. 肾内输注莫索尼定(1、3和10 nmol kg-1 min-1)可使尿流率和钠排泄增加。与先前报道的α2肾上腺素能受体刺激情况不同,莫索尼定通过增加渗透清除率而非自由水清除率来增加尿量。3. 莫索尼定的作用似乎也与α2肾上腺素能受体刺激的作用不同。咪唑啉优先结合位点特异性阻断剂量的伊达唑胺(0.3 mg kg-1)可减弱莫索尼定(3 nmol kg-1 min-1)的肾脏作用,而α2肾上腺素能受体特异性阻断剂量的萝芙木碱(0.3 mg kg-1)则无此作用。此外,与α2肾上腺素能受体激动剂不同,莫索尼定的作用不会因预先用V2血管加压素受体拮抗剂治疗而改变。4. 这些结果表明大鼠肾脏中α2肾上腺素能受体刺激与I1咪唑啉优先结合位点刺激之间存在差异,并提示肾脏咪唑啉优先结合位点具有直接的生理功能。

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Cardiovasc Drugs Ther. 1994 Mar;8 Suppl 1:43-8. doi: 10.1007/BF00877083.

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