Vaidyanathan G, Zalutsky M R
Department of Radiology, Duke University Medical Center, Durham, NC, USA.
Nucl Med Biol. 1995 Aug;22(6):759-64. doi: 10.1016/0969-8051(95)00028-v.
A potent chemotactic peptide, formyl-norleucyl-leucyl-phenylalanyl-norleucyl-tyrosyl-lysine was derivatized by reaction with N-succinimidyl 4-fluorobenzoate. This derivatized peptide bound to human polymorphonuclear leukocytes in vitro and exhibited biological activity in a superoxide production assay. Peptide labeling using N-succinimidyl 4-[18F]fluorobenzoate was accomplished in reasonable yields with 10-15 mCi of labeled peptide available per 100 Ci of [18F]fluoride. With the exception of the gastrointestinal tract, clearance of activity from tissues following injection of this peptide in normal mice was rapid. Although preliminary in nature, these results suggest that 18F-labeled chemotactic peptides should be investigated as potential agents for positron emission tomographic imaging of bacterial infections.
一种强效趋化肽，甲酰基 - 去甲亮氨酰 - 亮氨酰 - 苯丙氨酰 - 去甲亮氨酰 - 酪氨酰 - 赖氨酸通过与N - 琥珀酰亚胺基4 - 氟苯甲酸酯反应进行衍生化。这种衍生化肽在体外与人多形核白细胞结合，并在超氧化物产生测定中表现出生物活性。使用N - 琥珀酰亚胺基4 - [¹⁸F]氟苯甲酸酯进行肽标记的产率合理，每100居里的[¹⁸F]氟化物可获得10 - 15毫居里的标记肽。除胃肠道外，在正常小鼠中注射该肽后，组织中活性的清除速度很快。尽管这些结果本质上是初步的，但它们表明¹⁸F标记的趋化肽应作为细菌感染正电子发射断层成像的潜在试剂进行研究。
