Effects of novel phosphodiesterase 4 inhibitors, ariflo and SB242126A,on endothelin-l-induced contractility of isolated human myometrium

摘要

Objective: To investigate the effects of novel selective phosphodiesterase4 (PDE4) inhibitors, Ariflo and SB242126A, on the endothelin-1 (ET-1)- induced contractility occurring in nonpregnant human myometrium specimens. Methods: Contractile responses to Ariflo and SB242126A were recorded cumulatively on isolated human longitudinal myometrium specimens obtained through surgical operations. Results: Ariflo and SB242126A could inhibit both the frequency and amplitude of spontaneous contractions of myometrium (pD2= 8.6 and 7.6 ,n = 4) and ET-l-induced contractions in a concentration-dependent manner (pD2 = 7.7 and 8.1 , n = 5 ) , with a potency similar to that of Rolipram. Conclusion: Ariflo and SB242126A have an obvious inhibitory effect on endothelin-l-induced contractility of isolated human myometrium. The finding suggested that PDE4 inhibitors might have clinical potential in treating preterm labour and dysmenorrhoea.