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用放射配体结合实验与离体血管收缩功能实验相结合的方法，研究了４种四氢原小檗碱（ｔｅｔｒａｈｙｄｒｏｐｒｏｂｅｒｂｅｒｉｎｅ，ＴＨＰＢ）同类物对α＿１－肾上腺素受体（α＿１－ＡＲ）的作用。结果显示左旋四氢巴马汀（ｌ－ＴＨＰ），左旋千金藤立陡碱（ｌ－ＳＰＤ），四氢原小檗碱－１８（ＴＨＰＢ－１８）和四氢小檗碱（ＴＨＢ）￣（１２５)ＩＢＥ２２５４￣（１２５)Ｉ－２－β（４－ｈｙｄｒｏｘｙｐｈｅｎｙｌ）－ｅｔｈｙａｍｉｎｏｍｅｔｈｙｌ－ｔｅｔｒａｌｏｎｅ，￣（１２５)ＩＢＥ）与大鼠脑皮质α＿１－ＡＲ的结合呈竞争性拮抗作用，ｐＫ１值分别为５．５４±０．３６，５．５６±０．４７，５．７５±０．５６和６．０１±０．６０，Ｈｉｌｌ系数接近于１．０。并拮抗苯肾上腺素（ｐｈｅｎｙｌｅｐｈｒｉｎｅ，ＰＥ）介导大鼠主动脉的收缩，ｐＡ＿２值分别为５．４８±０．５８，５．６６±０．５４，５．６４±０．３４和５．４５±０．７６，斜率与１．０无显著性差别。结果提示，４种四氢原小檗碱同类物对α＿１－ＡＲ均有非亚型选择性拮抗效应，且亲和性相同。
The effects of four tetrahydroproberberine (THPB) congeners on α 1 -adrenoceptor (α 1 -AR) were studied by a combination of radioligand binding assay and ex vivo vasoconstriction assay. The results showed that l-THP, l-SPD, THPB-18 and THB ~ 125 ) IBE2254 ~ (125) I-2-β (4-hydroxyphenyl) -ethyaminomethyl-tetralone, ~ (125) IBE) had a competitive antagonistic effect on the binding of rat brain cortex α 1-AR with pK1 values of 5.54 ± 0.36, 5.56 ± 0.47, 5.75 ± 0.56 and 6.01 ± 0.60, and the Hill coefficient was close to 1.0. And antagonized the phenylephrine (PE) -mediated aortic contractions in rats, with pA_2 values of 5.48 ± 0.58, 5.66 ± 0.54, 5.64 ± 0.34 and 5.45, respectively ± 0.76, slope and 1.0 no significant difference. The results suggest that the four tetrahydrobiopterin analogues have non-subtype selective antagonistic effects on α 1-AR with the same affinity.