ATP-sensitive potassium channels modulate in vitro tocolytic effects of β₂-adrenergic receptor agonists on uterine muscle rings in rats in early but not in late pregnancy.

Abstract:

AIM:To investigate whether ATP-sensitive potassium (K(ATP)) channels modulate the tocolytic effect of β2-adrenergic receptor (β2-AR) agonists (ritodrine and salmeterol) in early-pregnant (day 6) and late-pregnant (day 22) rat uterus in vitro, in order to examine the relation between the K(ATP) channel sulphonylurea-binding regulatory subunit (SUR) expression and pharmacological reactivity of β2-AR agonists. METHODS:The tocolytic effects of ritodrine and salmeterol (10(-10)-10(-5) M) on spontaneous rhythmic contractions were investigated cumulatively, alone, or in the presence of the K(ATP) channel blocker glibenclamide (10(-6) M) and the K(ATP) channel opener pinacidil (10(-9)-10(-7) M) after 5-min preincubation. RESULTS:β2-AR agonist induced myometrial relaxation was inhibited by glibenclamide and enhanced by pinacidil on day 6, when SUR1 expression levels were high. Neither glibenclamide nor pinacidil mediated tocolytic effect was measured on day 22. CONCLUSION:Low expression of the K(ATP) channels at the end of gestation may facilitate enhanced excitability and contractility in the rat myometrium. The combination of a betamimetic and a K(ATP) channel opener will therefore not be of therapeutic relevance in the treatment of preterm delivery.

journal_name

Croat Med J

journal_title

Croatian medical journal

authors

Lovasz N,Koncz A,Domokos D,Gaspar R,Falkay G

doi

10.3325/cmj.2015.56.114

subject

Has Abstract

pub_date

2015-04-01 00:00:00

pages

114-8

issue

2

eissn

0353-9504

issn

1332-8166

journal_volume

56

pub_type

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