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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 myome-trium specimens. Methods Contractile responses to Ariflo and SB242126A were recorded cumulatively on isola-ted human longitudinal myometrium specimens obtained through surgical operations. Results Ariflo andSB242126A could inhibit both the frequency and amplitude of spontaneous contractions of myometrium (pD2 =8. 6and 7. 6,n =4) and ET-1 -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 effecton endothelin-1-induced contractility of isolated human myometrium. The finding suggested that PDE4 inhibitorsmight have clinical potential in treating preterm labour and dysmenorrhoea.
Objective To investigate the effects of novel selective phosphodiesterase 4 (PDE4) inhibitors, Ariflo and SB242126A, on the endothelin-1 (ET-1) -induced contractility occurring in nonpregnant human myome-trium specimens. Methods Contractile responses to Ariflo and SB242126A were recorded cumulatively 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-1 -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-1-induced contractility of isolated human myometrium. The finding suggested that PDE4 inhibitorsmight have clinical potential in treating preterm labor and dysmenorrhea.