Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.1.4.1 (phosphodiesterase)
 18,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The human myometrium contains two different forms of phosphodiesterase (PDE). One form is characterized by its lack of substrate specificity and its calcium-calmodulin dependence. The other one is selective for cyclic adenosine monophosphate (cAMP). Rolipram (4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone, ZK 62711) is a specific cAMP-PDE inhibitor. The physiological significance of the two forms of PDE is still unknown, particularly the role of the cAMP-specific form in the control of uterine motility. The latter form largely occurs in myometrium of pregnant women near term and is also present during the third trimester of pregnancy. Using isolated guinea-pig uteri it has been shown that rolipram in the concentration of 9 x 10(-4) mol/l caused the organ to remain insensitive to the stimulatory action of oxytocin. 9 x 10(-6) mol/l rolipram led to immediate relaxation of the uterus when it was added to the organ bath after the maximum concentration was reached following oxytocin stimulation. A new drug like rolipram effecting uterine motility in a not receptor-mediated manner might have advantages in comparison to beta-mimetics for the treatment of premature labor.
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PMID:Inhibition of uterine contractions by rolipram in vitro. 324 53

Since terbutaline treatment in premature labor has been shown to increase phosphodiesterase activity in the myometrium, the phosphodiesterase-inhibiting effect of theophylline and papaverine on myometrial preparations from pregnant women has been studied. The patients were either treated with terbutaline during the last 3 weeks of pregnancy or not treated. The results showed that papaverine is about 100 times more potent than theophylline in both phosphodiesterase-inhibiting effect and muscle-relaxing effect. No differences in effects were found in myometrial strips from terbutaline-treated or untreated women. A possible improvement in the tocolytic therapy with a combination of a beta-sympathomimetic and a phosphodiesterase-inhibiting drug is suggested.
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PMID:In vitro study of phosphodiesterase-inhibiting drugs: a complement to beta-sympathomimetic drug therapy in premature labor? 630 Dec 81