Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1071-4. doi: 10.1016/j.bmcl.2009.01.014. Epub 2009 Jan 10.

Abstract

Inhibitors of phenylethanolamine N-methyltransferase [PNMT, the enzyme that catalyzes the final step in the biosynthesis of epinephrine (Epi)] may be of use in determining the role of Epi in the central nervous system. Here we describe the synthesis and characterization of 7-SCN tetrahydroisoquinoline as an affinity label for human PNMT.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Epinephrine / metabolism
  • Epinephrine / physiology
  • Humans
  • Phenylethanolamine N-Methyltransferase / antagonists & inhibitors
  • Phenylethanolamine N-Methyltransferase / metabolism*
  • Rats
  • Tetrahydroisoquinolines / chemical synthesis*
  • Tetrahydroisoquinolines / chemistry
  • Tetrahydroisoquinolines / pharmacology*
  • Time Factors

Substances

  • 7-isothiocyanatotetrahydroisoquinoline
  • Tetrahydroisoquinolines
  • Phenylethanolamine N-Methyltransferase
  • Epinephrine