Human MC1R

Figure. Concentration-dependent activation of MC1R by α‐MSH

Reporter cells were transfected with either the expression plasmid for human melanocortin 1 receptor (MC1R) or the mock plasmid and treated with various concentrations of α‐MSH. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 850 pM.

Nomenclature
melanocortin 1 receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
Panels
à la carte, Oncology, Endocrinology/Metabolism, Neurology, Ophthalmology, Dermatology, Musculoskeletal, Human non-orphan GPCRs

Melanocortin receptors

Melanocortin receptors are activated by members of the melanocortin family (α-MSH, β-MSH and γ-MSH forms; δ form is not found in mammals) and adrenocorticotrophin (ACTH). Endogenous antagonists include agouti and agouti-related protein. ACTH(1-24) was approved by the US FDA as a diagnostic agent for adrenal function test, whilst NDP-MSH was approved by EMA for the treatment of erythropoietic protoporphyria. Several synthetic melanocortin receptor agonists are under clinical development.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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