EMAIL THIS PAGE TO A FRIEND

Methods in enzymology

Constitutive activity of neural melanocortin receptors.


PMID 21036237

Abstract

The two neural melanocortin receptors (MCRs), melanocortin-3 and -4 receptors (MC3R and MC4R), are G protein-coupled receptors expressed primarily in the brain that regulate different aspects of energy homeostasis. The MCRs are unique in having endogenous antagonists, agouti and agouti-related protein (AgRP). These antagonists were later shown to be inverse agonists. The MC3R has little or no constitutive activity, whereas the MC4R has significant constitutive activity that can easily be detected. We describe herein methods for detecting constitutive activities in these receptors and small molecule ligands as inverse agonists. AgRP is an inverse agonist for both MC3R and MC4R. We also provide models for the constitutively active MC4R mutants.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

A9501
Adenosine 3′,5′-cyclic monophosphate, ≥98.5% (HPLC), powder
C10H12N5O6P