Melanocortin receptors

Overview

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
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Species
Receptor
Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Endocrinology/Metabolism
Neurology
Ophthalmology
Dermatology
Musculoskeletal
à la carte
Reference agonist:
α‐MSH
EC50:
850 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Endocrinology/Metabolism
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
ACTH
EC50:
4.1 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
180 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Endocrinology/Metabolism
à la carte
Reference agonist:
α‐MSH
EC50:
600 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
8.5 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
3.2 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
ACTH
EC50:
27 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
370 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
5.2 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
α‐MSH
EC50:
19 nM