Hieble J P, Sarau H M, Foley J J, Demarinis R M, Pendleton R G
Naunyn Schmiedebergs Arch Pharmacol. 1982 Mar;318(4):267-73. doi: 10.1007/BF00501164.
A series of alpha-adrenergic agonists and antagonists having diverse chemical structure was examined for both central and peripheral alpha 1-adrenoceptor activity. The agonists tested included several novel aminotetralin derivatives which were potent and selective alpha 1-agonists. Peripheral alpha 1-activity was determined in the isolated rabbit ear artery; central alpha 1-receptor affinity was measured as the ability to inhibit 3H-WB 4101 binding to rat brain homogenates. In the agonist series, an excellent correlation between peripheral alpha 1-activity and central alpha 1-affinity was obtained, providing that partial agonists were excluded. Likewise, the receptor dissociation constant for blockade of the peripheral alpha 1-adrenoceptor correlated well with affinity for the central receptor for all of the alpha-antagonists. These data support the conclusion that central and peripheral alpha 1-adrenoceptors are similar or identical.
对一系列具有不同化学结构的α-肾上腺素能激动剂和拮抗剂进行了中枢和外周α1-肾上腺素能受体活性检测。所测试的激动剂包括几种新型氨基四氢萘衍生物，它们是强效且选择性的α1-激动剂。外周α1-活性在离体兔耳动脉中测定；中枢α1-受体亲和力通过抑制3H-WB 4101与大鼠脑匀浆结合的能力来测量。在激动剂系列中，排除部分激动剂后，外周α1-活性与中枢α1-亲和力之间存在良好的相关性。同样，对于所有α-拮抗剂，外周α1-肾上腺素能受体阻断的受体解离常数与对中枢受体的亲和力相关性良好。这些数据支持中枢和外周α1-肾上腺素能受体相似或相同的结论。
