Synthesis,labelling and animal experiments of the derivative of phenylpentadecanoic acid(CACPPA)

Ｓｙｎｔｈｅｓｉｓ，ｌａｂｅｌｉｎｇａｎｄａｎｉｍａｌｅｘｐｅｒｉｍｅｎｔｓｏｆｔｈｅｄｅｒｉｖａｔｉｖｅｏｆｐｈｅｎｙｌｐｅｎｔａｄｅｃａｎｏｉｃａｃｉｄ（ＣＡＣＰＰＡ）ＷｕＣｈｕｎＹｉｎｇ，ＪｉＳｈｕＲｅｎ，ＦａｎｇＰｉｎｇ，ＺｈｏｕＸｉａ...

The synthesis and biodistribution were discribed for 99m Tc labelled fatty acid, p [(N,N ′ di carboxymethyl) aminomethyl carboxyamino] phenylpentadecanoic acid (CACPPA). 99m Tc CACPPA was prepared by the reduction of Na 99m TcO 4 with stannous chloride in aqueous solution at pH 8.5～9.5, the labelling yield and chemical purity were over 90% determined by TLC and HPLC. Biodistribution of 99m Tc CACPPA in mice demonstrated that the highest myocardial uptake of 99m Tc CACPPA was 18.17±2.67% ID/g. When blood disappearance of 99m Tc CACPPA was analysed with a biexponential model, an initial half time of 1.11 min and a late half time of 20.08 min were obtained. 99m Tc CACPPA exhibited high binding to HSA in vitro, and partition coefficients were 10.98 and 11.45 at pH7.00 and pH7.40, respectively.