Melanin-concentrating hormone receptor explained
Two Melanin-concentrating hormone receptors (MCHR) have recently been characterized: MCH-R1 and MCH-R2. These two receptors share approximately 38% homology.
- MCH-R1 is expressed in all mammals.
- MCH-R2 is only found in some primates and carnivores including dogs, ferrets and humans.
Clinical significance
Antagonists might be useful in the treatment of obesity[1] [2] and anxiety and depression.[3] An agonist might have possible utility as a treatment for osteoporosis[4] and insomnia[5]
Research is ongoing for antagonists affecting MCH receptors R1 and R2.[6] [7]
See also
External links
- Web site: Melanin-Concentrating Hormone Receptors . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2007-10-25 . 2016-03-03 . https://web.archive.org/web/20160303165426/http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1339 . dead .
Notes and References
- Handlon AL, Zhou H . Melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity . J. Med. Chem. . 49 . 14 . 4017–22 . 2006 . 16821761 . 10.1021/jm058239j .
- Luthin DR . Anti-obesity effects of small molecule melanin-concentrating hormone receptor 1 (MCHR1) antagonists . Life Sci. . 81 . 6 . 423–40 . 2007 . 17655875 . 10.1016/j.lfs.2007.05.029 .
- Shimazaki T, Yoshimizu T, Chaki S . Melanin-concentrating hormone MCH1 receptor antagonists: a potential new approach to the treatment of depression and anxiety disorders . CNS Drugs . 20 . 10 . 801–11 . 2006 . 16999451 . 10.2165/00023210-200620100-00002. 32524553 .
- Bohlooly-Y M, Mahlapuu M, Andersén H, Astrand A, Hjorth S, Svensson L, Törnell J, Snaith MR, Morgan DG, Ohlsson C . Osteoporosis in MCHR1-deficient mice . Biochem. Biophys. Res. Commun. . 318 . 4 . 964–9 . 2004 . 15147966 . 10.1016/j.bbrc.2004.04.122 .
- Melanin-concentrating hormone control of sleep-wake behavior.. 23477948 . 10.1016/j.smrv.2012.10.002 . 17. 4. August 2013. Sleep Med Rev. 293–8. Monti JM, Torterolo P, Lagos P .
- Saito Y, Maruyama K . Identification of melanin-concentrating hormone receptor and its impact on drug discovery . Journal of Experimental Zoology Part A: Comparative Experimental Biology . 305 . 9 . 761–8 . 2006 . 16902961 . 10.1002/jez.a.311 . 2006JEZA..305..761S .
- McBriar MD . Recent advances in the discovery of melanin-concentrating hormone receptor antagonists . Current Opinion in Drug Discovery & Development . 9 . 4 . 496–508 . 2006 . 16889232 .