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Molecular Human Reproduction, Vol. 9, No. 8, 475-480, August 2003
© 2003 European Society of Human Reproduction and Embryology

Article

Investigation of the role of the serotonergic activity of certain subtype-selective {alpha}1A antagonists in the relaxant effect on the pregnant rat uterus in vitro

Submitted on March 13, 2003; accepted on April 23, 2003

Attila Mihályi, Eszter Ducza, Robert Gáspár and George Falkay1

University of Szeged, Faculty of Pharmacy, Department of Pharmacodynamics and Biopharmacy, H-6720 Szeged, Eötvös u. 6, Hungary

1 To whom correspondence should be addressed. e-mail: falkay{at}pharma.szote.u-szeged.hu

Results from recent studies have shown that {alpha}1A-adrenergic receptor ({alpha}1A-AR) antagonists could offer a new alternative in the treatment of preterm delivery. However, members of this group [2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane hydrochloride (WB4101), 5-methylurapidil (5-MU)] are known to influence serotonin (5-hydroxy-tryptamine) (5-HT1A) receptors, too. Our objective was to clarify the role of their 5-HT1A activities in the uterus relaxant effect. RT–PCR was used to determine mRNA expression of the receptor subtypes in 22 day pregnant rat uteri. Isolated uteri were stimulated by 5-HT or electrical field to investigate the contraction-inhibiting effect and the 5-HT1A activity of the {alpha}1A antagonists. Both receptor subtypes are present in rat myometrium. 5-HT induced contractions were inhibited by the {alpha}1A antagonists. Besides shifting the dose–response curve of 5-HT to the right, 5-MU decreased its maximal effect. The {alpha}1A antagonists inhibited electrical field stimulation-induced contractions. 5-HT1A blockade increased the maximal effect of 5-MU but did not change that of WB4101. These results suggest that the contraction increase caused by 5-HT is mediated by {alpha}1A receptors. Serotonergic activity of {alpha}1 antagonists and especially {alpha}1A antagonists should be investigated as it may alter their efficacy and could interfere with their side-effects. It is proposed that novel {alpha}1A antagonists should be designed with no 5-HT1A activity to achieve maximal relaxant effect.

Key words: alpha1A-adrenoceptors/5-HT1A receptors/rat/tocolysis/uterus


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