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혈청 농도가 다제내성 억제제 BIBW 22 의 nucleoside 수송에 미치는 영향
이동권(Dong Kwon Rhee),(Hong Xing Chen),(Uwe Bamberger),(Yung Chi Cheng) 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.2
Some multidrug resistance inhibitors have been known to be influenced by the serum concentration. In this study, effect of serum concentration on inhibition of nucleoside transport by BIBW22, a new multidrug resistance inhibitor derived from dipyridamole (DPM), was studied. When 5% or 100% (v/v) of fetal bovine serum (FBS) was contained in the culture, DPM dose for which nucleoside transport was inhibited by 50% (ID_(50)) was 0.42μM or 1.17μM, respectively. BIBW22 also showed the same trend as DPM did in response to increase of FBS concentration. However, ID_(50) value for DPM in the absence or presence of human plasma was 0.007μM or 1.02μM respectively showing 145times increase of ID_(50) value. ID_(50) value for BIBW22 in the presence of human plasma was 0.028μM showing only 5times increase in ID_(50) value. This result suggests that potency of BIBW22 was much less affected by the plasma concentration and BIBW22 could be a good candidate for a clinical use in multidrug resistance treatment.