Development of a radiolabeled beta-human chorionic gonadotropin

Acta Pharm. 2009 Dec;59(4):421-9. doi: 10.2478/v10007-009-0035-6.

Abstract

beta-Human chorionic gonadotropin (beta-hCG) was successively labeled with [(67)Ga]-gallium chloride after conjugation with freshly prepared diethylenetriaminepentaacetic acid dianhydride (ccDTPA). After solid phase purification of the radiolabeled hormone, high performance liquid chromatography showed radiochemical purity higher than 95 % under optimized conditions (specific activity = 22-23 TBq mM(-1), labeling efficiency 80 %). Preliminary in vivo studies (ID g(-1), %) in male wild-type rats showed marked gonadal uptake of the tracer after 240 minutes in agreement with the biodistribution studies and reported beta-hCG receptors. Target to blood ratios were 5.1 and 15.2 after 3 and 24 hours, respectively, while target to muscle ratios were 35 and 40 after 3 and 24 hours, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport
  • Chorionic Gonadotropin, beta Subunit, Human / chemistry*
  • Chorionic Gonadotropin, beta Subunit, Human / pharmacokinetics
  • Gallium*
  • Humans
  • Isotope Labeling / methods*
  • Male
  • Pentetic Acid
  • Positron-Emission Tomography
  • Radiopharmaceuticals
  • Rats
  • Tissue Distribution

Substances

  • Chorionic Gonadotropin, beta Subunit, Human
  • Radiopharmaceuticals
  • gallium chloride
  • Pentetic Acid
  • Gallium