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丙泊酚衍生物:治疗勃起功能障碍的潜在药物?

Propofol's derivative: a potential drug for erectile dysfunction?

机构信息

Department of General Medicine, Chennai Medical College Hospital and Research Centre, Irungalur, Trichy, India.

出版信息

Med Hypotheses. 2011 Oct;77(4):668-70. doi: 10.1016/j.mehy.2011.07.011. Epub 2011 Jul 29.

Abstract

Propofol, an intravenous anesthetic agent induces priapism in humans. We hypothesize the probable central nervous system and local mechanisms through which a similar molecule can be used as a therapy in erectile dysfunction. Previous literatures published over a period of 35 years (1976-2010) were searched using the key words, mechanisms were identified and discussed. In the central nervous system, propofol has an inhibitory effect on serotonin receptors and on gamma-aminobutyric acid A (GABA-A) receptors as well as a facilitatory action on N-methyl-D-aspartate (NMDA) mediated calcium response and agonistic action on dopaminergic D2 receptors, which might contribute towards maintaining erections. While in the penile tissue, propofol's action may be due to increased synthesis of nitric oxide (NO), the principal mediator of penile erection. In addition, it may also have inhibitory effect on thromboxane A2, a potent vasoconstrictor and stimulatory action on penile adenosine triphosphate (ATP) dependent potassium (K-ATP) channels, a potent vasodilator. In view of the above mechanisms, use of propofol or similar molecule in erectile dysfunction needs to be ascertained and evaluated.

摘要

异丙酚,一种静脉麻醉剂,可导致人类阴茎异常勃起。我们假设通过类似的分子可能作为一种治疗勃起功能障碍的治疗方法,其可能的中枢神经系统和局部机制。使用关键字搜索了过去 35 年(1976-2010 年)发表的文献,确定并讨论了机制。在中枢神经系统中,异丙酚对 5-羟色胺受体和γ-氨基丁酸 A(GABA-A)受体具有抑制作用,对 N-甲基-D-天冬氨酸(NMDA)介导的钙反应具有促进作用,并对多巴胺 D2 受体具有激动作用,这可能有助于维持勃起。而在阴茎组织中,异丙酚的作用可能是由于一氧化氮(NO)的合成增加,NO 是阴茎勃起的主要介质。此外,它还可能对血栓素 A2 有抑制作用,血栓素 A2 是一种强效的血管收缩剂,对阴茎三磷酸腺苷(ATP)依赖性钾(K-ATP)通道有刺激作用,K-ATP 通道是一种强效的血管扩张剂。鉴于上述机制,需要确定和评估异丙酚或类似分子在勃起功能障碍中的应用。

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