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ANTAGONISTIC CHARACTRIZATION OF 1-(2,6-DIMETHYLPHENOXYL)-2-(3,4-DIMETHYLPHENYL ETHYLAMINO) PROPANE HYDROCHLORIDE ON α1-ADRENOCEPTOR
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 10
- DOI:
- 10.3321/j.issn:0513-4870.2000.10.005
- Key Word:
- α1肾上腺素受体;拮抗剂;1-(2,6-二甲氧基)-2-(3,4-二甲基苯乙氨基)丙烷盐酸盐
Abstract： 目的研究DDPH对α1-肾上腺素受体(α1-AR)及其亚型的拮抗作用.方法放射配体结合实验和离体血管收缩功能实验.结果 DDPH对125I-BE2254与大鼠脑皮质和脾脏α1-AR结合呈竞争性拮抗作用.pKI值在两者间无显著性差别, Hill系数均接近于1.0.在分别稳定表达α1A,α1B或α1D-AR的克隆HEK293细胞中,其拮抗的pKI值α1A和α1D比α1B-AR高约2倍,Hill系数均接近于1.0.并拮抗去甲肾上腺素(NE)介导大鼠主动脉,肾动脉和脾脏收缩的pA2值,在三者间无显著差别,斜率接近1.0.结论 DDPH对α1-AR有竞争性拮抗作用,但其作用对α1-AR亚型无选择性.
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