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目的 研究洛土辛 (Lot)对磷酸二酯酶 (PDE)Ⅲ或Ⅴ亚型的抑制作用及选择性。方法 采用放射免疫测定法及收缩张力记录。结果 Lot和氨力农(Amr)剂量依赖性地增加大鼠心肌cAMP含量 ,且Lot的作用强于Amr。在家兔阴茎海绵体 ,Lot和扎普司特 (Zap)可剂量依赖性地增加海绵体cGMP含量 ,Lot的作用远弱于Zap。Lot,罂粟碱 (Pap)、Zap及Amr可显著抑制预先用苯肾上腺素诱发的阴茎海绵体血管收缩 ,其EC50 分别依次为Zap >Pap >Amr >Lot。结论 提示洛土辛的作用机理可能与选择性的抑制PDEⅢ有关。
Objective To investigate the inhibitory effect and selectivity of Lotion on phospholipid esterase (PDE) Ⅲ or Ⅴ subtypes. Methods Radioimmunoassay and contractive tension recording were used. Results Lot and Amr dose-dependently increased cAMP content in rat myocardium, and Lot had a stronger effect than Amr. In the rabbit penis, Lot and Zap can dose-dependently increase cGMP content in the corpus cavernosum, with Lot being much weaker than Zap. Lot, Papaverine (Pap), Zap and Amr significantly inhibited the contraction of corpus cavernosum induced by phenylephrine, with EC50 values of Zap> Pap> Amr> Lot respectively. Conclusions suggest that the mechanism of action of lobesartan may be related to the selective inhibition of PDE Ⅲ.