Radiosynthesis of a potent endothelin receptor antagonist: [11C] L-753,037

Hayden T. Ravert, William B. Mathews, Terence G. Hamill, H. Donald Burns, Robert F. Dannals

Research output: Contribution to journalArticle

Abstract

[11C]-L-753,037, [(+)-(5S,6R,7R)-2-butyl-7-[2-((2S)-2-carboxypropyl)-4-[11C]-methoxyphenyl]- 5-(3,4-methylenedioxyphenyl)-cyclopenteno-[1,2-b]pyridine-6-carboxylate], a potent mixed antagonist of endothelin receptor subtypes ET(A) and ET(B), was synthesized by [11C]-methylation of a phenolic precursor. The time for synthesis, purification, and formulation was 17 minutes with an average specific radioactivity of 2535 mCi/μmol (EOS) and average decay corrected radiochemical yield of 3% based on [11C]-methyl iodide.

Original languageEnglish (US)
Pages (from-to)1205-1210
Number of pages6
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume43
Issue number12
DOIs
StatePublished - Jan 1 2000

Keywords

  • Carbon-11
  • Endothelin
  • L-753,037
  • Positron emission tomography

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Radiosynthesis of a potent endothelin receptor antagonist: [<sup>11</sup>C] L-753,037'. Together they form a unique fingerprint.

  • Cite this