作者: E Buszman , A Orzechowska , A Beberok , R Rózańska
DOI:
关键词: In vitro 、 Trifluoperazine 、 Phenothiazine 、 Fluphenazine 、 Chlorpromazine 、 Binding site 、 Pharmacology 、 Melanin 、 Biophysics 、 In vivo 、 Chemistry
摘要: The aim of this study was to examine in vitro the binding capacity three phenothiazine derivatives--chlorpromazine, fluphenazine and trifluoperazine--causing adverse effects eye structures, natural melanin isolated from pig eyes as well synthetic DOPA-melanin used a model polymer. amount drug bound determined by UV spectrophotometry. analysis results for kinetics drug-melanin complex formation showed that increases with increasing initial concentration longer incubation time, attaining an equilibrium state after about 24 h. Binding parameters, i.e. number sites (n) association constants (K), were on basis Scatchard plots. For neuroleptic-ocular neuroleptic-DOPA-melanin complexes two classes independent found, K1 approximately 10(4) K2 10(2) M (-1) chlorpromazine complexes, 10(5) 10(3) M(-1) trifluoperazine complexes. numbers strong (n1) weak (n2) indicate lower affinity drugs examined ocular compared DOPA-melanin. ability chlorpromazine, interact melanin, especially is discussed relation toxicity these vivo.