伐地那非的分子学研究

Molecular Studies of Vardenafil

PDE5抑制剂在治疗ED方面的巨大成功使人们将注意力集中在更好地探讨各种抑制剂和PDE5的特征上,这些结构特征是PDE5抑制剂与PDE5的催化位点之间高亲和力和相互作用的基础。新近的分子学研究发现,伐地那非与PDE5的亲和力高,结合后解离慢,这就解释了在临床上该药可以低剂量发挥疗效、起效快速、持久等特点。研究也揭示了伐地那非的这些分子特点主要是由其环状结构决定的。

The remarkable therapeutic success of PDE5 inhibitors in the treatment of male erectile dysfunction has focused the attention of the researchers on better defining the properties of the individual inhibitors and PDE5 that contribute to the high affinity of these inhibitors for interaction with the PDE5 catalytic site. Recent molecular studies have demonstrated that vardenafil has high affinity for PDE5 and low dissociation rate from PDE5, which serves to explain why vardenafil works with low dosage, onsets quickly and has durative action in clinical practice. Moreover, the potency of vardenafil depends on its ring structure that resembles the purine moiety in cGMP.