Preliminary evaluation of 2-[4-[3-tert-butylamino)-2-hydroxypropoxy]phenyl]-3-methyl-6-me thoxy-4(3H)-quinazolinone ([+/-]HX-CH 44) as a selective beta1-adrenoceptor ligand for PET

Nucl Med Biol. 1999 Jan;26(1):105-9. doi: 10.1016/s0969-8051(98)00073-0.

Abstract

(+/-)-3-[11C]Methyl-2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-6 -methoxy-4(3H) quinazolinone ([+/-]-[11C]HX-CH 44) was labeled with carbon-11 using [11C]iodomethane with the corresponding N-demethylated precursor. Then, 30-90 mCi (1.10-3.33 GBq) of pure [11C]HX-CH 44 were obtained 30 min after end of bombardment with specific radioactivities of 500-1,400 mCi/micromol (18.5-51.8 GBq/micromol). Myocardial uptake in dogs was 0.340+/-0.043 pmol/mL tissue per nanomole injected, 10-15 min postinjection. Heart-to-lung ratio was 3 from the 5th to the 30th minute. Only 35% of the myocardial radioactivity could be displaced. Tissue uptake could not be blocked with appropriate compounds. Therefore, (+/-)-[11C]HX-CH 44 does not appear to be a suitable ligand for the study of myocardial beta1-adrenoceptors in positron emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Antagonists* / blood
  • Adrenergic beta-Antagonists* / pharmacology
  • Animals
  • Carbon Radioisotopes
  • Dogs
  • Heart / diagnostic imaging*
  • Ligands
  • Lung / diagnostic imaging*
  • Propanolamines* / blood
  • Propanolamines* / pharmacology
  • Quinazolinones
  • Radiopharmaceuticals / chemical synthesis*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adrenergic, beta-1 / analysis*
  • Receptors, Adrenergic, beta-1 / drug effects
  • Tomography, Emission-Computed

Substances

  • Adrenergic beta-Antagonists
  • Carbon Radioisotopes
  • Ligands
  • Propanolamines
  • Quinazolinones
  • Radiopharmaceuticals
  • Receptors, Adrenergic, beta-1
  • HX-CH 44BS