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 specimen...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.展开更多
基金Supported by the grant of Sino-France Cooperation of INSERM and SSMU.
文摘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.
