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本文对四种不同长度碳链烷基酯ECD[N,N′-乙撑-双(L-半胱胺酸乙酯)]衍生物的生物效应进行了比较,研究结果表明,烷基碳链的长度与它们各自的脂溶性、血浆蛋白(HSA)的结合率、脑摄取量呈正相关,但与脑清除速度呈负相关。注射后10s,~(99m)Tc-MCD、~(99m)Tc-ECD、~(99m)Tc-PCD和~(99m)Tc-BCD在大鼠脑的浓度(％I.D/g)分别为0.45、0.59、0.96和0.68。由猴的全身显像所见,注药后1.5h脑药物浓度分别为1.3、3.1、3.2和2.2(％I.D),肝内的放射性浓聚最高,经代谢有较大部分由肾排出。
In this paper, the biological effects of four derivatives of carbon chain alkyl esters ECD [N, N’-ethylene-bis (L-cysteine ethyl ester)] were compared. The results showed that alkyl carbon chains Were positively correlated with their respective liposolubility, plasma protein (HSA) binding rate and brain uptake, but negatively correlated with brain clearance rate. Concentrations (% ID / g) of 99m Tc-MCD, 99m Tc-ECD, 99m Tc-PCD and 99m Tc-BCD in rat brain at 10s after injection were 0.45 , 0.59, 0.96 and 0.68. From the monkeys’ whole body imaging, the brain drug concentration at 1.5h after injection was 1.3, 3.1, 3.2 and 2.2 (% I.D), respectively. The radioactive concentration in the liver was the highest, and most of the metabolism was excreted by the kidneys.