抑制 PDE-4 同工酶可减弱激动剂诱发的输尿管阶段性收缩的频率和总体收缩力。

IF 2.9 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Iris Lim, Taishi Masutani, Hikaru Hashitani, Russ Chess-Williams, Donna Sellers
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引用次数: 0

摘要

本研究旨在探讨磷酸二酯酶(PDE)在离体猪输尿管中的功能作用。将输尿管远端条带安装在器官槽中,并预先用 5-HT (100 μM)进行收缩。在产生稳定的阶段性收缩后,将 PDE-4 和 PDE-5 抑制剂累积添加到分离的组织中。PDE-4抑制剂,如罗立普仑(10 nM及以上)和罗氟司特(100 nM及以上),可显著减弱输尿管收缩反应,而更高浓度的吡拉米司特(1 μM及以上)则需要诱导显著的抑制作用。SQ22536(100 μM)可消除罗利普仑的衰减效应。PDE-5抑制剂,如西地那非和他达拉非,效果并不明显,只能在1μM的较高浓度下抑制5-HT诱导的收缩。罗利普仑能明显增强福斯可林的抑制作用,而硝普钠诱导的收缩反应减弱作用在他达拉非存在时保持不变。总之,我们的研究表明,PDE-4 抑制剂能有效减弱猪输尿管远端组织中 5-HT 诱导的收缩性,而 PDE-5 抑制剂的效果较差。这些研究结果表明,PDE-4 抑制剂(如罗利普仑)有望成为治疗输尿管内压增高引起的输尿管疾病的潜在治疗药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Inhibition of PDE-4 isoenzyme attenuates frequency and overall contractility of agonist-evoked ureteral phasic contractions.

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.

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来源期刊
Pharmacology Research & Perspectives
Pharmacology Research & Perspectives Pharmacology, Toxicology and Pharmaceutics-General Pharmacology, Toxicology and Pharmaceutics
CiteScore
5.30
自引率
3.80%
发文量
120
审稿时长
20 weeks
期刊介绍: PR&P is jointly published by the American Society for Pharmacology and Experimental Therapeutics (ASPET), the British Pharmacological Society (BPS), and Wiley. PR&P is a bi-monthly open access journal that publishes a range of article types, including: target validation (preclinical papers that show a hypothesis is incorrect or papers on drugs that have failed in early clinical development); drug discovery reviews (strategy, hypotheses, and data resulting in a successful therapeutic drug); frontiers in translational medicine (drug and target validation for an unmet therapeutic need); pharmacological hypotheses (reviews that are oriented to inform a novel hypothesis); and replication studies (work that refutes key findings [failed replication] and work that validates key findings). PR&P publishes papers submitted directly to the journal and those referred from the journals of ASPET and the BPS
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