کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1877919 | 1042262 | 2010 | 8 صفحه PDF | دانلود رایگان |
Ga-AMBA (Ga-DO3A-CH2CO-G-[4-aminobenzoyl]-QWAVGHLM-NH2) is a bombesin-like agonist with high affinity for gastrin releasing peptide receptors (GRP-R). Syntheses for natGa-AMBA, [67Ga]Ga-AMBA and [68Ga]Ga-AMBA were developed. The preparation of HPLC-purified and Sep-Pak purified [68Ga]Ga-AMBA were fully automated, using the built-in radiodetector of the Tracerlab FX F-N synthesizer to monitor fractionated 68Ge/68Ga generator elution and purification. The total synthesis time, including the fractional elution of the generator, was 20 min for Sep-Pak purified material and 40 min for HPLC-purified [68Ga]Ga-AMBA. Both [67Ga]Ga-AMBA and [177Lu]Lu-AMBA showed comparable high affinity for GRP-R in the human prostate cancer cell line PC-3 in vitro (kD=0.46±0.07; 0.44±0.08 nM), high internalization (78; 77%) and low efflux from cells at 2 h (2.4±0.7; 2.9±1.8%). Biodistribution results in PC-3 tumor-bearing male nude mice showed comparable uptake for [177Lu]Lu-, [111In]In-, [67Ga]Ga- and [68Ga]Ga-AMBA.
Journal: Applied Radiation and Isotopes - Volume 68, Issue 12, December 2010, Pages 2285–2292