锝标记长链脂肪酸衍生物(BAT-FA)的初步研究

锝标记长链脂肪酸衍生物(BAT-FA)的初步研究

PRELIMINARY STUDIES OF ~(99m)T_c LABELED FATTY ACID ANALOGS FOR MYOCARDIAL IMAGING

摘要

摘要: 放射性药物研究中,用~(123)I标记长链脂肪酸及其衍生物已有很多报道。本文报道了三种锝标记的长链脂肪酸衍生物:Tc-BAT-TDA,Tc-BAT-PDA和Tc-BAT-HxDA。三者的~(99m)Tc标记物均可用配体交换反应制备,产额分别为87％,70％和49％。产物经萃取纯化,放化纯高于98％。以~(99)Tc为载体,制备了~(99)Tc标记物,红外、紫外光谱的Tc=O特征峰与已知~(99)Tc-BAT络合物的光谱数据相符。动物实验数据表明:~(99m)Tc标记的上述长链脂肪酸衍生物在心脏中的浓集程度较碘代苯基十五酸(IPPDA)低。静脉给药后5min,在大鼠心肌中分别为0.20％,0.32％和0.46％剂量/组织。药物大部分浓集于肝脏。所提出的三种Tc-BAT-FA尚不能满足做为心肌显像剂的要求,需要通过改善配体的结构等途径来获得更好的结果。

Abstract: Radio iodine labelled fatty acid analogs are potential myocardial imaging agents for SPECT. In this paper are reported three new99mTc labelled fatty acid analogs. 99mTc-BAT-TDA, 99mTc-BAT-PDA and 99mTc-BAT-HxDA. Ligand exchange reaction with99mTc stannous glucoheptonate in 50% aqueous ethanol is used for labelling. With a yield of 87%, 70%, 49% respectively. 99mTc-fatty acid is purified by extraction into chloroform and the purity as determined by reverse phase HPLC is 98%. In order to determine the structure of Tc-BAT-fatty acid, 99Tc-BAT-PDA is synthesized with 99Tc ammonium pertechnetate in 50% citric acid buffer (pH=6) /ethanol using stannous chloride as the reducing agent. 99Tc-BAT-PDA displays the expected Tc = O UV absorption at 420nm and strong peak at 900cm-1 in the FTIR spectrum.Biodistribution studies of three 99mTc-fatty acid analogs are conducted in rats using 125I-ω- (p-iodophenyl) -penta-decanoic acid (IPPDA) as internal standard. The initial heart uptake of them is significantly lower than that of 125I-IPPDA.

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