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
StatePublished - 2000

Fingerprint

J 104132
Methylation
Radioactivity
Purification
pyridine
Endothelin Receptor Antagonists
methyl iodide

Keywords

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

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology

Cite this

Radiosynthesis of a potent endothelin receptor antagonist : [11C] L-753,037. / Ravert, Hayden T.; Mathews, William B; Hamill, Terence G.; Donald Burns, H.; Dannals, Robert F.

In: Journal of Labelled Compounds and Radiopharmaceuticals, Vol. 43, No. 12, 2000, p. 1205-1210.

Research output: Contribution to journalArticle

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AU - Donald Burns, H.

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