Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Eur J Pharmacol. 2003 Aug 15;475(1-3):37-47. doi: 10.1016/s0014-2999(03)02146-0.

Abstract

Central administration of the neuropeptide melanin-concentrating hormone (MCH) stimulates feeding in rodents. We studied the effects of intracerebroventricular (i.c.v.) administration of an MCH-1 receptor agonist (Compound A) and an MCH-1 receptor antagonist (Compound B) on feeding in satiated rats. Compound B (10 microg, i.c.v.) blocked the acute orexigenic effect of Compound A (5 microg, i.c.v.). In an experiment designed to either stimulate or inhibit MCH-1 receptor signaling over an extended period, rats received continuous i.c.v. infusions of vehicle (saline), Compound A (30 microg/day), Compound B (30 or 48 microg/day) or neuropeptide Y (24 microg/day, as positive control) via implantable infusion pumps. Continuous MCH-1 receptor activation recapitulated the obese phenotype of MCH-over-expressor mice, manifest as enhanced feeding (+23%, P<0.001), caloric efficiency and body weight gain (+38%, P<0.005) over the 14-day period relative to controls. Chronic MCH-1 receptor activation also elevated plasma insulin and leptin levels significantly. Conversely, continuous MCH-1 receptor antagonism led to sustained reductions in food intake (-16%, P<0.001), body weight gain (-35%, P<0.01), and body fat gain relative to controls, without an effect on lean mass. Antagonism of the MCH-1 receptor may be an effective approach for the treatment of obesity.

Publication types

  • Comparative Study

MeSH terms

  • Adipose Tissue / drug effects
  • Adipose Tissue / physiology*
  • Amino Acid Sequence / physiology
  • Animals
  • Appetite / drug effects
  • Appetite / physiology*
  • Body Weight / drug effects
  • Body Weight / physiology*
  • Dose-Response Relationship, Drug
  • Eating / drug effects
  • Eating / physiology
  • Ethers / administration & dosage
  • Ethers / chemistry
  • Hydrocarbons, Fluorinated / administration & dosage
  • Hydrocarbons, Fluorinated / chemistry
  • Male
  • Molecular Sequence Data
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Pituitary Hormone / agonists
  • Receptors, Pituitary Hormone / antagonists & inhibitors
  • Receptors, Pituitary Hormone / chemistry
  • Receptors, Pituitary Hormone / physiology*

Substances

  • CH3OCF2CH(CF3)OCH2F
  • Ethers
  • Hydrocarbons, Fluorinated
  • Receptors, Pituitary Hormone
  • melanin-concentrating hormone receptor
  • fluoromethyl 2,2-difluoro-1-(trifluoromethyl)vinyl ether