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苯甲酸的甘氨酸结合活性及其在灌注大鼠肝脏中的腺泡定位。

Glycine conjugation activity of benzoic acid and its acinar localization in the perfused rat liver.

作者信息

Chiba M, Poon K, Hollands J, Pang K S

机构信息

Faculty of Pharmacy, University of Toronto, Ontario, Canada.

出版信息

J Pharmacol Exp Ther. 1994 Jan;268(1):409-16.

PMID:8301581
Abstract

Glycine conjugation activity toward benzoic acid (BA) was studied in the single-pass perfused rat liver preparation. The steady-state hepatic extraction ratio for the portal vein (PV) perfused liver (at 10 ml/min) was maximal (0.6) at input concentrations < 40 microM among perfusions varying from tracer to 700 microM. Glycine conjugation was the predominant pathway; the kinetic parameters estimated after appropriately correcting for plasma protein binding (KA = 8.37 x 10(3) M-1 and 1.9 sites) revealed a low Km (12 microM) and a moderately high Vmax (101 nmol.min-1.g-1 liver) system. Biliary excretion of BA and its glycine-conjugated metabolite, hippuric acid, was minimal. Under first-order conditions (input concentration < 2 microM), the method of HAPV and HAHV perfusion (trace [14C]benzoate delivered via the hepatic artery (HA) at 2 ml/min and blank perfusate via the portal vein (PV) or hepatic vein (HV) at 10 ml/min) was used to examine the localization of glycine conjugation activity toward BA. During steady state, a multiple indicator dose of 51Cr-labeled red blood cells (vascular marker), [58Co]EDTA (interstitial space marker, which behaves similar to labeled tracer sucrose) and 3H2O (cellular marker) was injected as a bolus into the HA. Values of the extraction ratio of BA for HAPV perfusion (0.59 +/- 0.09) were dramatically reduced during HAHV perfusion (0.061 +/- 0.033, P < .01).(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

在单通道灌注大鼠肝脏制剂中研究了甘氨酸对苯甲酸(BA)的结合活性。在从示踪剂到700微摩尔的不同灌注中,门静脉(PV)灌注肝脏(流速为10毫升/分钟)对BA的稳态肝提取率在输入浓度<40微摩尔时最大(0.6)。甘氨酸结合是主要途径;在适当校正血浆蛋白结合后估计的动力学参数(KA = 8.37 x 10(3) M-1和1.9个位点)显示该系统具有低Km(12微摩尔)和中等偏高的Vmax(101纳摩尔·分钟-1·克-1肝脏)。BA及其甘氨酸结合代谢产物马尿酸的胆汁排泄极少。在一级条件下(输入浓度<2微摩尔),采用肝动脉-门静脉(HAPV)和肝动脉-肝静脉(HAHV)灌注方法(通过肝动脉(HA)以2毫升/分钟的流速输注微量[14C]苯甲酸,通过门静脉(PV)或肝静脉(HV)以10毫升/分钟的流速输注空白灌注液)来研究甘氨酸对BA结合活性的定位。在稳态期间,将多指标剂量的51Cr标记红细胞(血管标记物)、[58Co]乙二胺四乙酸(间隙空间标记物,其行为类似于标记的示踪剂蔗糖)和3H2O(细胞标记物)作为团注注入HA。在HAHV灌注期间,HAPV灌注时BA的提取率值(0.59 +/- 0.09)显著降低(0.061 +/- 0.033,P <.01)。(摘要截断于250字)

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