Szökö E, Kalász H, Kerecsen L, Magyar K
Department of Pharmacodynamics, Semmelweis University of Medicine, Budapest, Hungary.
Pol J Pharmacol Pharm. 1987 Mar-Apr;39(2):177-83.
Binding of three potential antidepressive compounds, EGYT-3615, EGYT-475 (trelibet) and EGYT-2760 to human serum was investigated by equilibrium dialysis method using radiolabelled drugs. All three compounds bound to serum proteins and the binding was sensitive to pH and salt concentration. The binding of trelibet and EGYT-3615 was not saturable at a wide range of drug concentration. The results show that EGYT-3615 has both specific and non-specific, while trelibet has only non-specific binding sites on serum proteins.
采用放射性标记药物的平衡透析法,研究了三种潜在抗抑郁化合物EGYT - 3615、EGYT - 475(曲利贝特)和EGYT - 2760与人血清的结合情况。这三种化合物均与血清蛋白结合,且这种结合对pH值和盐浓度敏感。在较宽的药物浓度范围内,曲利贝特和EGYT - 3615的结合不饱和。结果表明,EGYT - 3615在血清蛋白上既有特异性结合位点,也有非特异性结合位点,而曲利贝特只有非特异性结合位点。