Effects of different phosphodiesterase-inhibiting drugs on human pregnant myometrium: an in vitro study.
The phosphodiesterase (PDE)-inhibiting and smooth muscle relaxing effects of theophylline, enprofylline, papaverine and moxaverine have been studied in vitro on spontaneous contracting human, pregnant myometrium. All drugs showed a close correlation between the PDE-inhibiting and smooth muscle relaxing effect. The order of smooth muscle relaxing potency was papaverine greater than moxaverine greater than enprofylline greater than theophylline. The most potent PDE-inhibitors were moxaverine and papaverine with a 50% PDE-inhibiting concentration (IC50) of 3.3 and 3.8 microM as compared to the least potent PDE-inhibitor, theophylline, with an IC50 of 665 microM. It is concluded that PDE-inhibiting drugs show a close correlation between PDE-inhibiting and relaxing effect on spontaneously contracting pregnant myometrium and that the newly developed drug enprofylline might be of interest in the treatment of premature uterine contractions.
Berg
G
G
Department of Gynecology/Obstetrics, University Hospital, Linköping, Sweden.
Andersson
R G
RG
Ryden
G
G
D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D009126:Muscle Relaxation / Q000187:drug effects; D009215:Myometrium / Q000187:drug effects* / Q000201:enzymology; D010208:Papaverine / Q000031:analogs & derivatives / Q000494:pharmacology; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D011247:Pregnancy / Q000187:drug effects / Q000502:physiology*; D013806:Theophylline / Q000494:pharmacology; D014590:Uterine Contraction / Q000187:drug effects*; D014970:Xanthines / Q000494:pharmacology
D010726:Phosphodiesterase Inhibitors; D014970:Xanthines; D013806:Theophylline; D010208:Papaverine; C034347:enprofylline; C004490:moxaverine