Cardiovascular and electrocardiographic effects of the dopamine receptor agonists ropinirole, apomorphine, and PNU-142774E in conscious beagle dogs

J Cardiovasc Pharmacol. 2006 Mar;47(3):337-47. doi: 10.1097/01.fjc.0000205983.05771.f5.

Abstract

To confirm recent in vitro findings, we examined the cardiovascular and electrocardiographic (ECG) effects of the dopamine receptor agonists ropinirole, apomorphine, and PNU-142774E in conscious dogs. Intravenous (i.v.) infusions of ropinirole totaling 20 microg/kg maximally reduced mean arterial pressure (MAP; -16 mm Hg) and the ECG PR interval (-13 milliseconds) and increased heart rate (HR; +29 b/min) and QTc length (+33 ms) at a peak plasma drug concentration (p[drug]) of 3.5 ng/ml. I.V. PNU-142774E was better tolerated through 66 microg/kg and a maximal p[drug] of 5.9 ng/ml with negligible cardiovascular changes and mild QTc reduction (13 ms). Apomorphine (25 microg/kg i.v.) was intermediate to ropinirole and PNU-142774E for emesis and peak changes in MAP (-6 mm Hg), HR (+24 b/min), and QTc (+15 milliseconds) at a mean p[drug] of 3.4 ng/ml. By comparison, the class III antiarrhythmic trecetilide (2.0 mg/kg bolus) increased QTc (+58 ms) without affecting mean arterial pressure or heart rate. This study establishes that in conscious dogs, the selective dopamine receptor agonist PNU-142774E has fewer cardiovascular and emetic effects than ropinirole and apomorphine and supports prior in vitro findings that ropinirole and apomorphine but not the PNU-142774E imidazoquinolin analog sumanirole reduces the delayed rectifier current in HERG transfected cells.

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Apomorphine / blood
  • Apomorphine / pharmacology*
  • Blood Pressure / drug effects*
  • Dogs
  • Dopamine Agonists / pharmacology*
  • Drug Tolerance
  • Electrocardiography / drug effects*
  • Female
  • Heart Rate / drug effects*
  • Imidazoles / blood
  • Imidazoles / pharmacology*
  • Indoles / blood
  • Indoles / pharmacology*
  • Quinolines / blood
  • Quinolines / pharmacology*
  • Receptors, Dopamine D2 / agonists*
  • Receptors, Dopamine D2 / physiology
  • Receptors, Dopamine D3 / physiology

Substances

  • Dopamine Agonists
  • Imidazoles
  • Indoles
  • PNU-142774E
  • Quinolines
  • Receptors, Dopamine D2
  • Receptors, Dopamine D3
  • ropinirole
  • Apomorphine