Redzić Z B, Marković I D, Jovanović S S, Zloković B V, Rakić L M
Institute of Biochemistry, Faculty of Medicine, Belgrade.
Eur J Ophthalmol. 1995 Apr-Jun;5(2):131-5. doi: 10.1177/112067219500500211.
This study investigated the transport of tiazofurin (2-beta-D-ribofuranosyl thiazole-4-carboxamide) across the blood-aqueous humor barrier, using the vascular perfusion method in the guinea pig. Volume of distribution (Vd) of [3H] tiazofurin increased almost linearly in time, from 4% of its plasma concentration at 3 min to 10% after 12 min of perfusion. Unidirectional transport constant, K(in) was 7.01 +/- 1.06 x 10(-3) ml/min/g. These results indicate that tiazofurin penetrates the aqueous humor to a considerable extent. Addition of unlabelled tiazofurin to the perfusing medium caused a significant decrease in the uptake of [3H] labelled tiazofurin (K(in) = 2.60 +/- 0.91 x 10(-3) ml/min/g). Therefore, penetration of tiazofurin from blood into aqueous humor seems to be a saturable process with a diffusional component that cannot be disregarded. Such findings could be of considerable importance since this molecule is known to affect tissue metabolism.
本研究采用豚鼠血管灌注法，研究了替唑呋林（2-β-D-呋喃核糖基噻唑-4-甲酰胺）跨血-房水屏障的转运。[3H]替唑呋林的分布容积（Vd）随时间几乎呈线性增加，从灌注3分钟时血浆浓度的4%增加到灌注12分钟后的10%。单向转运常数K(in)为7.01±1.06×10(-3) ml/min/g。这些结果表明替唑呋林能在相当程度上穿透房水。向灌注介质中加入未标记的替唑呋林会导致[3H]标记的替唑呋林摄取量显著降低（K(in)=2.60±0.91×10(-3) ml/min/g）。因此，替唑呋林从血液进入房水的渗透似乎是一个具有不可忽视的扩散成分的可饱和过程。由于已知该分子会影响组织代谢，这些发现可能具有相当重要的意义。
