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抑制 PDE-4 同工酶可减弱激动剂诱导的输尿管相收缩的频率和整体收缩性。

Inhibition of PDE-4 isoenzyme attenuates frequency and overall contractility of agonist-evoked ureteral phasic contractions.

机构信息

Centre for Urology, Faculty of Health Sciences & Medicine, Bond University, Gold Coast, Queensland, Australia.

Department of Cell Physiology, Nagoya City University Graduate School of Medical Sciences, Nagoya, Japan.

出版信息

Pharmacol Res Perspect. 2024 Feb;12(1):e1175. doi: 10.1002/prp2.1175.

Abstract

The aim of this study was to investigate the functional role of phosphodiesterase enzymes (PDE) in the isolated porcine ureter. Distal ureteral strips were mounted in organ baths and pre-contracted with 5-HT (100 μM). Upon generation of stable phasic contractions, PDE-4 and PDE-5 inhibitors were added cumulatively to separate tissues. PDE-4 inhibitors, such as rolipram (10 nM and greater) and roflumilast (100 nM and greater), resulted in significant attenuation of ureteral contractile responses, while a higher concentration of piclamilast (1 μM and greater) was required to induce a significant depressant effect. The attenuation effect by rolipram was abolished by SQ22536 (100 μM). PDE-5 inhibitors, such as sildenafil and tadalafil, were not nearly as effective and were only able to suppress the 5-HT-induced contractions at higher concentrations of 1 μM. Rolipram significantly enhanced the depressant effect of forskolin, while sodium nitroprusside-induced attenuation of contractile responses remained unchanged in the presence of tadalafil. In summary, our study demonstrates that PDE-4 inhibitors are effective in attenuating 5-HT-induced contractility in porcine distal ureteral tissues, while PDE-5 inhibitors are less effective. These findings suggest that PDE-4 inhibitors, such as rolipram, may hold promise as potential therapeutic agents for the treatment of ureteral disorders attributable to increased intra-ureteral pressure.

摘要

本研究旨在探讨磷酸二酯酶(PDE)在猪离体输尿管中的功能作用。将远端输尿管条段置于器官浴中,并以 5-HT(100μM)预收缩。当产生稳定的阶段性收缩时,以累积方式向分离的组织中添加 PDE-4 和 PDE-5 抑制剂。PDE-4 抑制剂,如罗利普兰(10nM 及以上)和罗氟司特(100nM 及以上),可显著抑制输尿管收缩反应,而需要更高浓度的匹立米隆(1μM 及以上)才能产生显著的抑制作用。SQ22536(100μM)可消除罗利普兰的抑制作用。PDE-5 抑制剂,如西地那非和他达拉非,效果则不那么显著,仅能在更高浓度 1μM 时抑制 5-HT 诱导的收缩。罗利普兰显著增强了 forskolin 的抑制作用,而在存在他达拉非的情况下,硝普钠诱导的收缩反应抑制作用保持不变。总之,我们的研究表明,PDE-4 抑制剂可有效抑制猪远端输尿管组织中 5-HT 诱导的收缩,而 PDE-5 抑制剂效果则较差。这些发现表明,PDE-4 抑制剂,如罗利普兰,可能作为治疗因输尿管内压升高引起的输尿管疾病的潜在治疗剂具有应用前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05fa/10858371/c17710e779b8/PRP2-12-e1175-g002.jpg

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