Moriearty P L, Kenny W, Kumar V
Department of Psychiatry, Southern Illinois University School of Medicine, Springfield 62794-9230.
Alzheimer Dis Assoc Disord. 1989 Fall;3(3):143-7. doi: 10.1097/00002093-198903030-00003.
THA (9-amino, 1,2,3,4-tetrahydroacridine; tacrine) is currently under study as a cholinesterase (ChE) inhibitor in Alzheimer disease. In this study, a sensitive radiometric assay for THA inhibition of human plasma ChE, suitable for detection of effects of orally administered drug, is described. The assay is sensitive in a range of 4-50 ng/ml plasma. Reversibility of the inhibition permits distinguishing of drug effects on ChE from changes in amount of enzyme synthesized during treatment.
他克林（9-氨基-1,2,3,4-四氢吖啶；THA）目前作为一种胆碱酯酶（ChE）抑制剂正在用于阿尔茨海默病的研究。在本研究中，描述了一种用于检测口服给药药物效果的、灵敏的放射性测定法，该方法用于检测他克林对人血浆胆碱酯酶的抑制作用。该测定法在血浆浓度范围为4-50 ng/ml时具有灵敏性。抑制作用的可逆性使得能够区分药物对胆碱酯酶的作用与治疗期间合成的酶量的变化。
