本工作分别在稳定表达α１Ａ，α１Ｂ和α１Ｄ肾上腺素受体（ａｄｒｅｎｏｃｅｐｔｏｒ，ＡＲ）的人胚胎肾脏细胞（ｈｕｍａｎｅｍｂｒｙｏｎｉｃｋｉｄｎｅｙ２９３，ＨＥＫ２９３）和大鼠离体血管上，用放射配体结合实验和离体血管收缩功能实验方法以确定ｓｅｒｔｉｎｄｏｌｅ对α１ＡＲ亚型的选择性拮抗作用。结果显示ｓｅｒｔｉｎｄｏｌｅ与克隆α１ＡＡＲ的亲和性分别是与克隆α１ＢＡＲ和克隆α１ＤＡＲ的６９倍和１３２倍。Ｓｅｒｔｉｎｄｏｌｅ拮抗去甲肾上腺素引起的主动脉和肾动脉收缩反应的ｐＡ２值分别与其对α１Ｄ和α１Ａ亚型的ｐＫＩ值相符。分别稳定表达３种亚型受体的ＨＥＫ２９３细胞膜标本经与ｓｅｒｔｉｎｄｏｌｅ预温育３０ｍｉｎ后，受体与１２５ＩＢＥ２２５４结合的Ｂｍａｘ值显著降低，ＫＤ值无显著变化；而在ｓｅｒｔｉｎｄｏｌｅ存在条件下，α１ＡＲ３种亚型与１２５ＩＢＥ２２５４结合的ＫＤ值显著增大，但Ｂｍａｘ值无显著改变。上述结果表明ｓｅｒｔｉｎｄｏｌｅ为不可逆性竞争性α１ＡＲ拮抗剂，并有α１Ａ亚型选择性 This study was carried out on humanembryonickidney293 (HEK293) and rat isolated blood vessels stably expressing α1A, α1B and α1D adrenoceptors (AR) using radioligand binding assay and ex vivo vasoconstriction Experimental methods to determine the sertindole α1  AR subtype of selective antagonism. The results showed that the affinity of sertindole with the clone α1AAR was 69 times and 132 times that of the clone α1BAR and the clone α1DAR, respectively. The pA2 value of Sertindole against noradrenaline-induced aortic and renal artery contractile responses was consistent with its pKI value for alpha1D and alpha1A subtypes, respectively. After pre-incubation with sertindole for 30min, HEK293 cells stably expressing three subtype receptors were significantly decreased in Bmax and bound to 125IBE2254, respectively. There was no significant change in KD values; however, in the presence of sertindole, α1-AR3 The KD value of subtype binding to 125IBE2254 increased significantly, but the Bmax value had no significant change. The above results indicate that sertindole is an irreversible and competitive α1-AR antagonist with α1A subtype selectivity