α-adrenergic blockade: A possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo

I. Zupkó, Kinga Jánossy, Katalin Maul, A. Márki, G. Falkay

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Benzodiazepines are frequently used for the treatment of maternal psychiatric disorders during pregnancy. Besides their anxiolytic effect, they are reported to exert a direct relaxing action on several smooth muscle preparations, including the uterus. In the present study, the possibility of the involvement of α1-adrenergic receptors in this peripheral effect is investigated. The tocolytic potencies of diazepam, midazolam and nitrazepam are assessed in vivo in a postpartum rat model, together with other drugs known to bind to α-adrenoceptors (e.g. α1-antagonists, tricyclic compounds and droperidol). The interactions of some benzodiazepines and norepinephrine were also examined in an isolated in vitro system. The affinities of these agents for the receptor in question were additionally tested by radioligand displacement assay. A correlation was found between the tocolytic potencies and inhibition constants of the tested drugs, suggesting that the smooth muscle-relaxing effect of these benzodiazepines is mediated through modulation of the α1-adrenergic receptors.

Original languageEnglish
Pages (from-to)1093-1102
Number of pages10
JournalLife Sciences
Volume72
Issue number10
DOIs
Publication statusPublished - Jan 24 2003

Fingerprint

Tocolytic Agents
Benzodiazepines
Adrenergic Agents
Adrenergic Receptors
Postpartum Period
Rats
Smooth Muscle
Muscle
Nitrazepam
Droperidol
Radioligand Assay
Midazolam
Anti-Anxiety Agents
Diazepam
Pharmaceutical Preparations
Uterus
Psychiatry
Assays
Norepinephrine
Mothers

Keywords

  • Benzodiazepine
  • Postpartum rat
  • Premature delivery
  • Tocolysis

ASJC Scopus subject areas

  • Pharmacology

Cite this

α-adrenergic blockade : A possible mechanism of tocolytic action of certain benzodiazepines in a postpartum rat model in vivo. / Zupkó, I.; Jánossy, Kinga; Maul, Katalin; Márki, A.; Falkay, G.

In: Life Sciences, Vol. 72, No. 10, 24.01.2003, p. 1093-1102.

Research output: Contribution to journalArticle

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