Melanocortin receptor
Melanocortin receptors are members of the rhodopsin family of 7-transmembrane G protein-coupled receptors.
There are five known members of the melanocortin receptor system[1] each with differing specificities for melanocortins:[2][3][4]
- MC1R. MC1R is associated with pigmentation genetics.
- MC2R. MC2R is also known as the ACTH receptor or corticotropin receptor because it is specific for ACTH alone.
- MC3R. MC3R
- MC4R. Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity.[5]
- MC5R. MC5R
These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide,[6] and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones.[7]
Contents
Selective ligands
Several selective ligands for the melanocortin receptors are known,[8][9][10][11] and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1,[12] while anorectic and aphrodisiac effects appear to involve both MC3 and MC4.[13] MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.[14][15][16][17]
Agonists
- Non-selective
- MC1-selective
- MC4-selective
- Unknown (but for certain MC2-acting)
Antagonists and inverse agonists
- Non-selective
- MC4-selective
- HS-014
- HS-024
- MCL-0042[18]
- MCL-0129[19]
- MPB-10
- SHU-9119 (agonist at MC1 and MC5, antagonist at MC3 and MC4)
Unknown
References
- ↑ Melanocortins and the Melanocortin Receptor
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External links
- Lua error in package.lua at line 80: module 'strict' not found.
- Melanocortin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
- Calculated spatial position of melanocortin-4 receptor in the lipid bilayer, inactive state with antagonist and active state with agonist
