A derivative of the melanocortin receptor antagonist SHU9119 (PG932) increases food intake when administered peripherally

Gregory M. Sutton, M. Josephine Babin, Xuyuan Gu, Victor J Hruby, Andrew A. Butler

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Melanocortin receptors are considered promising candidates for the treatment of behavioral and metabolic disorders ranging from obesity to anorexia and cachexia. These experiments examined the response of mice to peripheral injections of two compounds. PG932 is a derivative of SHU9119 which is non-selective antagonist of melanocortin-3 and melanocortin-4 receptors (Mc3r and Mc4r). PG946 is a derivative of a hybrid of α- and β-MSH, and is a moderately selective Mc3r antagonist. SHU9119 increases food intake when administered intracerebroventricularly but is without effect when injected into the periphery. In contrast, PG932 was found to be highly effective at stimulating food intake when administered peripherally by intraperitoneal injection. The orexigenic effect of PG932 required functional Mc4r, suggesting that inhibition of this receptor is involved in the stimulation of food intake. PG946 did not significantly affect on feeding behavior. PG932 is thus a useful new compound for studies examining the regulation of appetite and energy balance, and may also prove useful for the treatment of cachectic conditions.

Original languageEnglish (US)
Pages (from-to)104-111
Number of pages8
JournalPeptides
Volume29
Issue number1
DOIs
StatePublished - Jan 2008

Fingerprint

Melanocortin Receptors
Eating
Derivatives
Receptor, Melanocortin, Type 4
Melanocortins
Melanocyte-Stimulating Hormones
Appetite Regulation
Cachexia
Anorexia
Feeding Behavior
Energy balance
Intraperitoneal Injections
Obesity
Injections
Therapeutics
SHU 9119
Experiments

Keywords

  • Anorexia
  • Antagonist
  • Appetite
  • Endotoxin
  • Melanocortin receptor
  • Proopiomelanocortin

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

A derivative of the melanocortin receptor antagonist SHU9119 (PG932) increases food intake when administered peripherally. / Sutton, Gregory M.; Josephine Babin, M.; Gu, Xuyuan; Hruby, Victor J; Butler, Andrew A.

In: Peptides, Vol. 29, No. 1, 01.2008, p. 104-111.

Research output: Contribution to journalArticle

Sutton, Gregory M. ; Josephine Babin, M. ; Gu, Xuyuan ; Hruby, Victor J ; Butler, Andrew A. / A derivative of the melanocortin receptor antagonist SHU9119 (PG932) increases food intake when administered peripherally. In: Peptides. 2008 ; Vol. 29, No. 1. pp. 104-111.
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