Small-molecule melanin-concentrating hormone-1 receptor antagonists require brain penetration for inhibition of food intake and reduction in body weight.

@article{Hu2008SmallmoleculeMH,
  title={Small-molecule melanin-concentrating hormone-1 receptor antagonists require brain penetration for inhibition of food intake and reduction in body weight.},
  author={X Eric Hu and John August Wos and Martin E. Dowty and Paula M. Suchanek and Wei Ji and James Brad Chambers and Stephen C. Benoit and Deborah J. Clegg and Ofer Reizes},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2008},
  volume={324 1},
  pages={206-13}
}
The melanin-concentrating hormone-1 receptor (MCH1R) is a G-protein-coupled receptor expressed in the brain and peripheral tissues that regulates energy storage and body weight. Here, we focused on discovery of the mechanism and site of action for a small-molecule MCH1R antagonist, which yields weight loss in a mouse model of human obesity. MCH1R is expressed throughout the brain but also found in peripheral tissues known to regulate fat storage and utilization, e.g., skeletal muscle and… CONTINUE READING