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Pharmacological and biochemical study on the effects of selective phosphodiesterase inhibitors on human term myometrium

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Abstract.

This study was aimed at evaluating the in vitro effects of phosphodiesterase inhibitors and β2-adrenoceptor agonists on spontaneous contractions of human term myometrium. Rolipram, RP 73401 (3-cyclopentyloxy-N-(3,5(-dichloro-4-pyridil)-4-methoxybenzamide) and Ro 20-1724 (1-4-(3-butoxy-4-methoxybenzyl)-2-imidozolidinone) (phosphodiesterase 4 inhibitors) inhibited spontaneous myometrial contractions (Emax ~100%; pD2 of 6.80±0.28, 6.84±0.32 and 6.31±0.03, respectively). Salbutamol and formoterol were less effective (Emax=40±6% and 35±12%, respectively) than phosphodiesterase 4 inhibitors to reduce myometrial contractility. Inhibitors of phosphodiesterase 3 (milrinone and siguazodan) and 5 (zaprinast) were marginally effective. Rolipram (10–30 nM) and siguazodan (0.1 µM) potentiated the response to salbutamol (Emax=75±12%, 88±8% and 73±12% and pD2=6.51±0.20, 6.93±0.29 and 6.48±0.16, respectively). Sodium nitroprusside (pD2=6.76±0.29) and theophylline (pD2=5.15±0.22) were effective inhibitors of myometrial contractions. Chromatographic separation of phosphodiesterase isoenzymes demonstrated that phosphodiesterase 4 is predominant but other phosphodiesterase isoenzymes were also identified. In conclusion, phosphodiesterase 4 inhibitors alone or combined with β2-adrenoceptor agonists have potential interest as tocolytic agents.

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Bardou, M., Cortijo, J., Loustalot, C. et al. Pharmacological and biochemical study on the effects of selective phosphodiesterase inhibitors on human term myometrium. Naunyn-Schmiedeberg's Arch Pharmacol 360, 457–463 (1999). https://doi.org/10.1007/s002109900092

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  • DOI: https://doi.org/10.1007/s002109900092

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