• Source: 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 each with differing specificities for melanocortins:

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 is associated with childhood growth, accrual of lean mass and onset of puberty.
MC4R. Defects in MC4R are a cause of autosomal dominant obesity, accounting for 6% of all cases of early-onset obesity.
MC5R. MC5R
These receptors are inhibited by endogenous inverse agonists agouti signalling peptide and agouti-related peptide, and activated by synthetic (i.e. afamelanotide) and endogenous agonist melanocyte-stimulating hormones.




Selective ligands


Several selective ligands for the melanocortin receptors are known, and some synthetic compounds have been investigated as potential tanning, anti-obesity and aphrodisiac drugs, with tanning effects mainly from stimulation of MC1, while anorectic and aphrodisiac effects appear to involve both MC3 and MC4. MC1, MC3 and MC4 are widely expressed in the brain, and are also thought to be responsible for effects on mood and cognition.




= Agonists

=
Non-selective
α-MSH
β-MSH
γ-MSH
Afamelanotide
Bremelanotide
Melanotan II
Modimelanotide
Setmelanotide
MC1-selective
BMS-470,539
MC4-selective
PF-00446687
PL-6983
THIQ
Unknown (but for certain MC2-acting)
Alsactide
Tetracosactide




= Antagonists and inverse agonists

=
Non-selective
Agouti-related peptide
Agouti signalling peptide
MC4-selective
HS-014
HS-024
MCL-0042
MCL-0129
MPB-10
SHU-9119 (agonist at MC1 and MC5, antagonist at MC3 and MC4)




= Unknown

=
Semax




References






External links


"Melanocortin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Melanocortin+Receptors at the U.S. 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

Kata Kunci Pencarian:

• Melanokortin
• Efelid
• Kuda
• SIM1
• Evolusi manusia terkini
• Kulit gelap
• Melanocortin receptor
• Melanocortin 1 receptor
• Melanocortin 4 receptor
• Melanocortin 3 receptor
• Melanocortin
• Melanocortin 5 receptor
• ACTH receptor
• Melanocortin 2 receptor accessory protein
• Adrenocorticotropic hormone
• Proopiomelanocortin