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Body Weight Regulation by Selective MC4 Receptor Agonists and Antagonists
Author(s) -
FOSTER ALAN C.,
JOPPA MARGARET,
MARKISON STACY,
GOGAS KATHY R.,
FLECK BETH A.,
MURPHY BRIAN J.,
WOLFF MEIRA,
CISMOWSKI MARY J.,
LING NICHOLAS,
GOODFELLOW VAL S.,
CHEN CHEN,
SAUNDERS JOHN,
CONLON PAUL J.
Publication year - 2003
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2003.tb03168.x
Subject(s) - melanocortin 4 receptor , melanocortin , agonist , receptor , orexigenic , pharmacology , melanocortin receptor , endocrinology , medicine , chemistry , neuropeptide y receptor , neuropeptide
A bstract : There has been great interest in melanocortin (MC) receptors as targets for the design of novel therapeutics to treat disorders of body weight, such as obesity and cachexia. Both genetic and pharmacological evidence points toward central MC4 receptors as the principal target. Using highly selective peptide tools for the MC4 receptor, which have become available recently, we have provided pharmacological confirmation that central MC4 receptors are the prime mediators of the anorexic and orexigenic effects reported for melanocortin agonists and antagonists, respectively. The current progress with receptor‐selective small molecule agonist and antagonist drugs should enable the therapeutic potential of MC4 receptor activation and inhibition to be assessed in the clinic in the near future.