β-Adrenoceptor blocking properties of dl-nebivolol and its enantiomers in the pithed normotensive rat

J. Schneider, C. Fruh, B. Wilffert, Thies Peters

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Abstract

In the pithed normotensive rat, the effects of dl-nebivolol and its enantiomers on the (-)-adrenaline (epinephrine)- and electrical stimulation-induced increases in heart rate (HR) and diastolic blood pressure (DBP) were investigated. dl-Nebivolol dose-dependently (10-7to 10-5mol/kg intravenously) antagonised the (-)-adrenaline-induced as well as the electrical stimulation-induced increases in HR, whereas the accompanying increases in DBP were not affected by dl-nebivolol in doses up to 10-5mol/kg. d-Nebivolol dose-dependently (10-8to 10-5mol/kg intravenously) attenuated the (-)-adrenaline-mediated increase in HR. The increase in DBP in the lower dose range of (-)-adrenaline was slightly but significantly (p <0.05) enhanced by d-nebivolol 10-6and 10-5mol/kg. This effect was not dose-dependent and was much smaller than expected for a β2-adrenoceptor blocking drug. The increase in HR elicited by electrical stimulation of the spinal cord was completely blocked by d-nebivolol 10-6mol/kg, whereas the accompanying increase in DBP was not influenced. l-Nebivolol in doses
Original languageEnglish
Pages (from-to)123-128
Number of pages6
JournalClinical Drug investigation
Volume3
Issue numberSUPPL. 1
Publication statusPublished - 22-Oct-1991

Keywords

  • adrenalin
  • beta adrenergic receptor
  • beta adrenergic receptor blocking agent
  • dextro nebivolol
  • nebivolol
  • unclassified drug
  • animal experiment
  • blood pressure
  • conference paper
  • drug effect
  • drug mixture
  • enantiomer
  • heart rate
  • intravenous drug administration
  • male
  • nonhuman
  • rat
  • stereoisomerism

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