Role of hypothalamic melanocortin 3/4-receptors in mediating chronic cardiovascular, renal, and metabolic actions of leptin

Hypertension. 2004 Jun;43(6):1312-7. doi: 10.1161/01.HYP.0000128421.23499.b9. Epub 2004 May 3.

Abstract

The present study examined whether blockade of melanocortin receptors subtypes 3 and 4 (MC3/4-R) inhibits chronic cardiovascular and dietary responses to leptin infusion. A cannula was placed in the lateral ventricle of male Sprague-Dawley rats for chronic intracerebroventricular (ICV) infusion via osmotic minipump, and arterial and venous catheters were implanted for measurement of mean arterial pressure (MAP) and heart rate (HR) 24 h/d and IV infusions. After a 5-day control period, rats received (1) 0.9% saline vehicle ICV for 12 days plus leptin (1 microg/kg per minute IV, n=5) during the final 7 days; (2) MC3/4-R antagonist SHU-9119 (1 nmol/h ICV) for 12 days plus leptin (1 microg/kg per minute IV, n=6) during the final 7 days; and (3) SHU-9119 (1 nmol/h ICV, n=8) for 12 days. Leptin infusion in vehicle-treated rats caused a small increase in MAP (5+/-1 mm Hg) despite reduced food intake (23+/-1 to 10+/-1 g/d) and decreased body weight (-6%+/-1%). SHU-9119 infusion completely prevented the cardiovascular and dietary actions of leptin, leading to increased food intake (23+/-1 to 49+/-4 g/d) and body weight (+30%+/-2%), markedly decreased HR (-77+/-9 bpm), and caused a decrease in MAP (-6+/-1 mm Hg). Similar results were observed when SHU-9119 was infused alone in vehicle-treated rats. Leptin decreased plasma insulin to 30% of control values, an effect that was also abolished by SHU-9119 treatment, which caused a 5-fold increase in plasma insulin concentration. Thus, MC3/4-R antagonism completely blocked the chronic cardiovascular, satiety, and metabolic effects of leptin, suggesting that the hypothalamic melanocortin system plays an important role in mediating these actions of leptin.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Diuresis / drug effects
  • Diuresis / physiology
  • Eating / drug effects*
  • Eating / physiology
  • Heart Rate / drug effects
  • Heart Rate / physiology
  • Hemodynamics / drug effects*
  • Hemodynamics / physiology
  • Hypothalamus / drug effects
  • Hypothalamus / physiology*
  • Infusion Pumps, Implantable
  • Insulin / blood
  • Kidney / drug effects*
  • Kidney / physiology
  • Leptin / administration & dosage
  • Leptin / pharmacology*
  • Leptin / physiology
  • Male
  • Melanocyte-Stimulating Hormones / pharmacology
  • Natriuresis / drug effects
  • Natriuresis / physiology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Melanocortin, Type 3 / antagonists & inhibitors
  • Receptor, Melanocortin, Type 3 / physiology*
  • Receptor, Melanocortin, Type 4 / antagonists & inhibitors
  • Receptor, Melanocortin, Type 4 / physiology*
  • Renin / blood
  • Satiety Response / drug effects
  • Satiety Response / physiology
  • Weight Gain / drug effects*
  • Weight Gain / physiology

Substances

  • Insulin
  • Leptin
  • Receptor, Melanocortin, Type 3
  • Receptor, Melanocortin, Type 4
  • SHU 9119
  • Melanocyte-Stimulating Hormones
  • Renin