[3H] -哌唑嗪和[3H] -二氢麦角隐亭与大鼠心脏α-肾上腺素能受体的结合
Binding of [3H]-prazosin and [3H]-dihydroergocryptine to rat cardiac alpha-adrenoceptors.
作者信息
Guicheney P, Meyer P
出版信息
Br J Pharmacol. 1981 May;73(1):33-9. doi: 10.1111/j.1476-5381.1981.tb16768.x.
Abstract
1 [3H]-prazosin binds specifically to a single class of alpha-adrenoceptors in rat cardiac membranes (KD25 degrees C = 0.2 nM). 2 That these receptors are of the alpha 1-type was indicated by competition studies, i.e. alpha 1-antagonists such as prazosin and (2-(2,6-dimethoxyphenoxyethyl) aminomethyl-1, 4-benzodioxane (WB 4101) were more potent than the alpha 2-antagonists, yohimbine and piperoxan in inhibiting [3H]-prazosin binding. 3 A comparative study of [3H]-prazosin binding and [3H]-dihydroergocryptine binding to cardiac membranes showed that both [3H]-prazosin and [3H]-dihydroergocryptine (at low concentrations) bind to alpha 2-adrenoceptors, while [3H]-dihydroergocryptine (at higher concentrations) also binds to another class of sites.
摘要
- [3H] - 哌唑嗪特异性结合大鼠心肌膜上的单一类别的α - 肾上腺素能受体（25℃时解离常数KD = 0.2 nM）。2. 竞争研究表明这些受体属于α1型，即哌唑嗪和（2 - （2,6 - 二甲氧基苯氧基乙基）氨基甲基 - 1,4 - 苯并二恶烷（WB 4101）等α1拮抗剂在抑制[3H] - 哌唑嗪结合方面比α2拮抗剂育亨宾和哌罗克生更有效。3. 对[3H] - 哌唑嗪结合与[3H] - 二氢麦角隐亭结合心肌膜的比较研究表明，[3H] - 哌唑嗪和[3H] - 二氢麦角隐亭（低浓度时）均结合α2 - 肾上腺素能受体，而[3H] - 二氢麦角隐亭（高浓度时）还结合另一类位点。
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