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 (100âμM). Upon generation of stable phasic contractions, PDE-4 and PDE-5 inhibitors were added cumulatively to separate tissues. PDE-4 inhibitors, such as rolipram (10ânM and greater) and roflumilast (100ânM and greater), resulted in significant attenuation of ureteral contractile responses, while a higher concentration of piclamilast (1âμM and greater) was required to induce a significant depressant effect. The attenuation effect by rolipram was abolished by SQ22536 (100âμM). 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 1âμM. 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.
Inhibition of PDE-4 isoenzyme attenuates frequency and overall contractility of agonist-evoked ureteral phasic contractions.
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作者:Lim Iris, Masutani Taishi, Hashitani Hikaru, Chess-Williams Russ, Sellers Donna
| 期刊: | Pharmacology Research & Perspectives | 影响因子: | 2.300 |
| 时间: | 2024 | 起止号: | 2024 Feb;12(1):e1175 |
| doi: | 10.1002/prp2.1175 | ||
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