Effects of a PPAR-gamma receptor agonist and an angiotensin receptor antagonist on aortic contractile responses to alpha receptor agonists in diabetic and/or hypertensive rats

Cardiovasc J Afr. 2016;27(3):164-169. doi: 10.5830/CVJA-2015-080. Epub 2016 May 4.

Abstract

Aim: The aim of this study was to investigate the effects of pioglitazone and losartan pre-treatment on the aortic contractile response to the alpha-1 agonist, phenylephrine, and the alpha-2 agonist, clonidine, in L-NAME-induced hypertensive, STZ-induced diabetic, and hypertensive diabetic rats.

Methods: Male Wistar rats were randomly allocated to four groups: control, diabetic (DM), hypertensive (HT) and hypertensive diabetic (HT + DM) groups. Three weeks after drug application, in vitro dose-response curves to phenylephrine (Phe) (10-9-10-5 M) and clonidine (Clo) (10-9-10-5 M) were recorded in aortic rings in the absence (control) and presence of pioglitazone (10 µM) and/or losartan (10 µM).

Results: Pioglitazone and losartan caused a shift to the right in contractile response to phenylephrine in all groups. The sensitivity of the aortic rings to phenylephrine was decreased in the presence of pioglitazone and/or losartan in all groups. The contractile response of clonidine decreased in the presence of pioglitazone and/or losartan in the control, HT and DM groups.

Conclusion: The sensitivity of aortic rings to alpha-1 and alpha-2 adrenoceptors was decreased in the presence of pioglitazone and/or losartan in diabetic and hypertensive rats. Concomitant use of PPAR-gamma agonists, thiazolidinediones, and angiotensin receptor blockers may be effective treatment for diabetes and hypertension.

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology*
  • Angiotensin II Type 1 Receptor Blockers / pharmacology*
  • Animals
  • Antihypertensive Agents / pharmacology*
  • Aorta / drug effects*
  • Aorta / metabolism
  • Aorta / physiopathology
  • Clonidine / pharmacology*
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetic Angiopathies / chemically induced
  • Diabetic Angiopathies / drug therapy*
  • Diabetic Angiopathies / metabolism
  • Diabetic Angiopathies / physiopathology
  • Dose-Response Relationship, Drug
  • Hypertension / chemically induced
  • Hypertension / drug therapy*
  • Hypertension / metabolism
  • Hypertension / physiopathology
  • Hypoglycemic Agents / pharmacology*
  • In Vitro Techniques
  • Losartan / pharmacology*
  • Male
  • NG-Nitroarginine Methyl Ester
  • PPAR gamma / agonists*
  • PPAR gamma / metabolism
  • Phenylephrine / pharmacology*
  • Pioglitazone
  • Rats, Wistar
  • Receptor, Angiotensin, Type 1 / drug effects*
  • Receptor, Angiotensin, Type 1 / metabolism
  • Thiazolidinediones / pharmacology*
  • Vasoconstriction / drug effects*
  • Vasoconstrictor Agents / pharmacology*

Substances

  • Adrenergic alpha-Agonists
  • Angiotensin II Type 1 Receptor Blockers
  • Antihypertensive Agents
  • Hypoglycemic Agents
  • PPAR gamma
  • Receptor, Angiotensin, Type 1
  • Thiazolidinediones
  • Vasoconstrictor Agents
  • Phenylephrine
  • Losartan
  • Clonidine
  • NG-Nitroarginine Methyl Ester
  • Pioglitazone