大鼠脑中的血管紧张素II受体亚型。
Angiotensin II receptor subtypes in the rat brain.
作者信息
Rowe B P, Grove K L, Saylor D L, Speth R C
机构信息
Department of Physiology, Quillen College of Medicine, East Tennessee State University, Johnson City 37614.
出版信息
Eur J Pharmacol. 1990 Sep 21;186(2-3):339-42. doi: 10.1016/0014-2999(90)90457-h.
The non-peptide angiotensin II (AII) receptor subtype selective antagonist, DuP 753, was used to characterize AII receptor binding sites in the rat brain. DuP 753 competed for specific 125I-[Sar1,Ile8]AII (125I-SIAII) binding in many brain nuclei (IC50 = 20-30 nM), but was a weak competitor at remaining sites (IC50 greater than 10(-4) M). DuP 753 sensitive binding sites (designated AII alpha subtype) correspond with areas where binding is inhibited by sulfhydryl reducing agents, whereas DuP 753 insensitive sites (AII beta) correspond with areas where binding is not inhibited by sulfhydryl reducing agents.
非肽类血管紧张素II（AII）受体亚型选择性拮抗剂DuP 753被用于鉴定大鼠脑中的AII受体结合位点。DuP 753在许多脑核中竞争性抑制特异性125I-[Sar1，Ile8]AII（125I-SIAII）结合（IC50 = 20 - 30 nM），但在其余位点是弱竞争性抑制剂（IC50大于10^(-4) M）。DuP 753敏感结合位点（称为AIIα亚型）与巯基还原剂抑制结合的区域相对应，而DuP 753不敏感位点（AIIβ）与巯基还原剂不抑制结合的区域相对应。
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