Impairment of the low-affinity state β1-adrenoceptor-induced relaxation in spontaneously hypertensive rats
Impairment of the low-affinity state β1-adrenoceptor-induced relaxation in spontaneously hypertensive rats
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DOI：
10.1038/sj.bjp.0705990
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发表时间：
2004-11-01
影响因子：
7.3
通讯作者：
Gauthier, C
中科院分区：
文献类型：
--
作者：
Mallem, MY;Toumaniantz, G;Gauthier, C
[1]在高血压中，血管β-肾上腺素能舒张功能下降。然而，尚未评估每种β-肾上腺素受体（β-AR）亚型的特异性参与，特别是β（1）-AR的低亲和力状态。我们研究了自发性高血压大鼠（SHR）β（1）-AR诱导的舒张的低亲和力状态是否受损。2对CGP 12177和氰基吲哚洛尔的舒张反应，低亲和力状态β（1）-AR激动剂（具有β（1）-/β（2）-AR拮抗和部分β（3）-AR激动特性）在从12周龄Wistar京都大鼠（3在WKY中，CGP 12177和氰基吲哚酚产生内皮和一氧化氮（NO）非依赖性舒张。CGP 12177诱导的内皮非依赖性舒张作用不受β（1）-、β（2）-AR（纳多洛尔）或β（3）-AR（L-748337或SR 59230 A）拮抗剂的影响，但可被高浓度的CGP 20712 A显著降低（P
1 In hypertension, a decrease of the vascular beta-adrenergic relaxation has been described. However, the specific involvement of each beta-adrenoceptor (beta-AR) subtype, in particular the low-affinity state of beta(1)-AR, has not yet been evaluated. We investigated whether the low-affinity state of beta(1)-AR-induced relaxation was impaired in Spontaneously Hypertensive Rats (SHR).2 The relaxant responses to CGP 12177 and cyanopindolol, low-affinity state beta(1)-AR agonists ( with beta(1)-/beta(2)-AR antagonistic and partial beta(3)-AR agonistic properties) were evaluated on thoracic aortic rings isolated from 12-weeks-old Wistar Kyoto rats (WKY) and SHR.3 In WKY, CGP 12177 and cyanopindolol produced an endothelium and nitric oxide ( NO)independent relaxation. CGP 12177-induced endothelium-independent relaxation was not modified either by beta(1)-, beta(2)-AR (nadolol) or beta(3)-AR (L-748337 or SR 59230A) antagonists but was significantly reduced by high concentrations of CGP 20712A ( P