Stephenson J A, Summers R J
J Auton Pharmacol. 1986 Jun;6(2):109-16. doi: 10.1111/j.1474-8673.1986.tb00637.x.
The selective alpha1-adrenoreceptor antagonist radioligand [3H] prazosin has been used to localize alpha1-adrenoreceptors in slide mounted sections of rat, dog and human kidney. The biochemical characteristics of [3H] prazosin binding to rat kidney sections were examined and found to be saturable, reversible, stereoselective, with a KD of 0.12 nM and Bmax of 6.72 +/- 0.2 fmoles/section. 3H Ultrofilm images of [3H] prazosin binding to rat, dog, and human kidney revealed binding to the vasculature but in the rat additional receptors were confined to the renal cortex. In the rat kidney autoradiography using emulsion coated coverslips showed that binding in the renal cortex was largely to proximal tubules. In all three species the autoradiographic studies support a role for alpha1-adrenoreceptors in control of renal blood flow. In the rat the location of alpha1-adrenoreceptors suggests that they can also have an important influence on fluid and electrolyte balance, gluconeogenesis and production of prostanoids.
选择性α1-肾上腺素能受体拮抗剂放射性配体[3H]哌唑嗪已被用于在大鼠、狗和人类肾脏的载玻片切片中定位α1-肾上腺素能受体。研究了[3H]哌唑嗪与大鼠肾脏切片结合的生化特性，发现其具有饱和性、可逆性、立体选择性，解离常数（KD）为0.12 nM，最大结合容量（Bmax）为6.72±0.2飞摩尔/切片。[3H]哌唑嗪与大鼠、狗和人类肾脏结合的3H超薄膜图像显示其与脉管系统结合，但在大鼠中，额外的受体局限于肾皮质。在大鼠肾脏中，使用涂有乳剂的盖玻片进行放射自显影显示，肾皮质中的结合主要发生在近端小管。在所有三个物种中，放射自显影研究均支持α1-肾上腺素能受体在肾血流控制中的作用。在大鼠中，α1-肾上腺素能受体的位置表明它们也可能对液体和电解质平衡、糖异生以及前列腺素的产生产生重要影响。
