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应用放射受体结合法研究了近30种四氢异喹啉类(TIQs)生物碱对大鼠脑内α肾上腺素受体的作用。其中l-CBN,l-THC和l-STP对α_1受体亲和力最高,K_i值为～2.0×10~(-7)mol/L。其次是DHS,XLP和l-DCT,K_i值分别为4.7×10~(-7),6.5×10~(-7)和7.6×10~(-7)mol/L。DHS对α_2受体亲和力最高(K_i=1.25×10~(-6)mol/L),l-REM次之。对α受体亚型亲和力选择比K_i(alpha-2)/Ki(alpha-1)最高的是l-STP(357) 和XLP(154),它们对α_2受体几无亲和力(K_i>10~(-4)mnl/L)。提示l-STP和XLP对α_1受体有较高的选择性。l-SPD和l-THP对α_1和α_2受体亲和力相近,均为中等强度。THJ,DRC及l-TTD等6种TIQs对α_1和α_2受体均无亲和力(K_i>10~(-4)mnl/L)。
The effects of nearly 30 tetrahydroisoquinolines (TIQs) alkaloids on α-adrenergic receptors in rat brain were studied by radioimmunoassay. Among them, l-CBN, l-THC and l-STP had the highest affinity for α_1 receptor with a K_i value of ~ 2.0 × 10 -7 mol / L. Followed by DHS, XLP and l-DCT. The values of K_i were 4.7 × 10 -7, 6.5 × 10 -7 and 7.6 × 10 -7 mol / L, respectively. DHS had the highest affinity for α_2 receptor (K_i = 1.25 × 10 -6 mol / L), followed by 1-REM. L-STP (357) and XLP (154), which have the highest affinity for α receptor subtypes than K_i (alpha-2) / Ki (alpha-1), have little affinity for α_2 receptors (K_i> (-4) mnl / L). Tip l-STP and XLP α_1 receptor for a high selectivity. l-SPD and l-THP on α_1 and α_2 receptor affinity similar, are moderate intensity. Six kinds of TIQs, such as THJ, DRC and l-TTD, had no affinity for α_1 and α_2 receptors (K_i> 10 ~ (-4) mnl / L).