CAJ | 학술논문

目的:研究消癃通闭对α1-肾上腺素受体(α-adrenoceptor, α1-AR)的拮抗作用,为寻找有治疗作用的先导化合物提供理论依据。方法:(1)采用放射配体结合实验，在犬脑细胞膜中分别加入标记后的125I-BE2254和15种浓度的消癃通闭，测定其放射性活度。通过Hill作图求出IC50值；(2)采用离体组织收缩功能实验，测定消癃通闭对去甲肾上腺素介导离体大鼠前列腺收缩的拮抗作用，求得pKB值。结果:消癃通闭对125I-BE2254与犬大脑皮层α1-AR的结合呈竞争性抑制作用,其半效抑制(质量)浓度IC50为（34.0±6.0） g*L－1，Hill系数为0.7。消癃通闭可使α1-AR介导的大鼠前列腺平滑肌收缩效应曲线平行右移，消癃通闭在两种不同浓度时,其拮抗的pKB值分别为（37.0±11.0） g*L－1和（30.0±8.0） g*L－1。结论：消癃通闭对α1-AR有竞争性拮抗作用。
목적:연구소륭통폐대α1-신상선소수체(α-adrenoceptor, α1-AR)적길항작용,위심조유치료작용적선도화합물제공이론의거。방법:(1)채용방사배체결합실험，재견뇌세포막중분별가입표기후적125I-BE2254화15충농도적소륭통폐，측정기방사성활도。통과Hill작도구출IC50치；(2)채용리체조직수축공능실험，측정소륭통폐대거갑신상선소개도리체대서전렬선수축적길항작용，구득pKB치。결과:소륭통폐대125I-BE2254여견대뇌피층α1-AR적결합정경쟁성억제작용,기반효억제(질량)농도IC50위（34.0±6.0） g*L－1，Hill계수위0.7。소륭통폐가사α1-AR개도적대서전렬선평활기수축효응곡선평행우이，소륭통폐재량충불동농도시,기길항적pKB치분별위（37.0±11.0） g*L－1화（30.0±8.0） g*L－1。결론：소륭통폐대α1-AR유경쟁성길항작용。
Objective: To better understand the antagonistic effect of Xiao Long Tong Bi (XLTB), a Chinese herb medicine, on α1-adrenoceptor (α1-AR). Methods: (1) Radio ligand binding assay . Specific　125I-BE2254(2-β(4-hdroxyphenyl)-ethyl amino-methyl-tetralone) binding was measured by incubating membrane of canine cerebral cortex with a single concentration of　125I-BE2254 in the presence of 15 concentrations of XLTB. Half-effectual concentration of inhibition (IC50) and Hill coefficients (nH) were determined by Hill plots. (2) Contractile responses of rat prostate strip in vitro were determined. pKB values for XLTB in competitively inhibiting NE-stimulated contraction of tissues were measured by the method of Ainlakshana. Results: XLTB competitively inhibited binding of　125I-BE2254 to α1-AR in a concentration -dependent manner. IC50 values for XLTB in canine cerebral cortex were (34.0±6.0)　g*L－1, the Hill efficiency value (0.7±0.1) was significantly decreased from unity. Contractile studies showed that XLTB competitively antagonized the NE concentration-response curve with pKB values of (37.0±11.0) g*L－1 or (30.0±8.0) g*L－1 when XLTB concentration was 70 g*L－1 or 170 g*L－1, respectively. The pKB values for XLTB in antagonizing NE-induced contraction of tissues were showed to fit in well with the IC50 values on rat prostate. Conclusion: These results suggest that XLTB appears to be a competitive antagonist for α1-AR.