Synthesis and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[ 11C]methylpiperidin-3-yl)methyl)-2-o-tolylquinazolin-4(3H)-one, a potential PET tracer for growth hormone secretagogue receptor (GHSR)

Rachel Potter, Andrew G. Horti, Hayden T. Ravert, Daniel P. Holt, Paige Finley, Ursula Scheffel, Robert F. Dannals, Richard L. Wahl

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

The peptide hormone ghrelin mediates through action on its receptor, the growth hormone secretagogue receptor (GHSR), and is known to play an important role in a variety of metabolic functions including appetite stimulation, weight gain, and suppression of insulin secretion. In light of the fact that obesity is one of the major health problems plaguing the modern society, the ghrelin signaling system continues to remain an important and attractive pharmacological target for the treatment of obesity. In vivo imaging of the GHSR could shed light on the mechanism by which ghrelin affects feeding behavior and thus offers a new therapeutic perspective for the development of effective treatments. Recently, a series of piperidine-substituted quinazolinone derivatives was reported to be selective and potent GHSR antagonists with high binding affinities. Described herein is the synthesis, in vitro, and in vivo evaluation of (S)-6-(4-fluorophenoxy)-3-((1-[11C]methylpiperidin-3-yl)methyl)-2- o-tolylquinazolin-4(3H)-one ([11C]1), a potential PET radioligand for imaging GHSR.

Original languageEnglish
Pages (from-to)2368-2372
Number of pages5
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number7
DOIs
StatePublished - Apr 1 2011
Externally publishedYes

Keywords

  • C
  • GHSR
  • Ghrelin
  • Growth hormone secretagogue receptor
  • PET

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