Radiolabeling of bombesin-like peptide with 99mTc: 99mTc-litorin and biodistribution in rats

Abstract

Bombesin-like peptides are related to several human cancer receptors, including small cell lung, prostate, breast, colon, and pancreatic cancers. Litorin, an amphibian bombesin peptide derivative, is found to stimulate the contraction of smooth muscle, to stimulate gastrin, gastric acid, and pancreatic secretion, and to suppress the nutriment in in vivo experiments. In the present study, litorin was labeled with 99mTc by the stannous chloride procedure. Labeling yield is 95 +/- 1.4%, as determined by radio thin layer chromatography (RTLC) and radio high performance chromatography (RHPLC). Results of in vitro studies demonstrated a high stability in serum and cysteine solutions. In vivo biodistribution was investigated with normal male Albino Wistar rats. Biodistribution data showed fast clearance, low intestinal accumulation, and significant uptake in bombesin/gastrin releasing peptide (BN/GRP) receptor rich tissues such as the pancreas (23.56 +/- 0.01 %ID/g 30 min pi). It can be blocked partially by previous administration of 'cold' litorin. The results showed specificity of the uptake. As 99mTc-litorin displays good radiolabeling and biodistribution, it is a potentially useful radiopharmaceutical for detection of bombesin receptor-expressing cancers.