通过血红蛋白饱和度变构抑制剂增强体内氧合作用。

Enhanced oxygenation in vivo by allosteric inhibitors of hemoglobin saturation.

作者信息

Khandelwal S R, Randad R S, Lin P S, Meng H, Pittman R N, Kontos H A, Choi S C, Abraham D J, Schmidt-Ullrich R

机构信息

Department of Radiation Oncology, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298.

出版信息

Am J Physiol. 1993 Oct;265(4 Pt 2):H1450-3. doi: 10.1152/ajpheart.1993.265.4.H1450.

DOI:10.1152/ajpheart.1993.265.4.H1450

PMID:8238433

Abstract

The in vivo effects on hemoglobin (Hb)-O2 affinity and tissue PO2 were investigated after intraperitoneal administration of 2-[4-(((dichloroanilino)-carbonyl)methyl)phenoxyl]-2-methyl propionic acid (RSR4; 150 mg/kg) or its 3,5-dimethyl derivative (RSR13; 300 mg/kg) in C3Hf/Sed mice. The Hb-O2 dissociation curve was plotted from tail vein blood samples using an O2 dissociation analyzer before and up to 160 min after compound administration. Twenty to 40 min after injection, the PO2 at 50% saturation of hemoglobin (Hb P50) increased by a mean of 25% (range 18-31%) after RSR4 and 53% (range 36-76%) after RSR13. Tissue PO2 was continuously measured using an O2 microelectrode in thigh muscle before and up to 40 min after RSR4 or RSR13 injection. Twenty to 40 min after administration, tissue PO2 increased by a mean of 78% (range 30-127%) after RSR4 and 66% (range 39-97%) after RSR13 administration in anesthetized mice. No change in tissue PO2 was seen in anesthetized controls.

摘要

在C3Hf/Sed小鼠腹腔注射2-[4-(((二氯苯胺基)-羰基)甲基)苯氧基]-2-甲基丙酸（RSR4；150毫克/千克）或其3,5-二甲基衍生物（RSR13；300毫克/千克）后，研究了其对血红蛋白（Hb）-O2亲和力和组织PO2的体内效应。在化合物给药前及给药后长达160分钟，使用O2解离分析仪从尾静脉血样绘制Hb-O2解离曲线。注射后20至40分钟，RSR4给药后血红蛋白50%饱和度时的PO2（Hb P50）平均增加25%（范围为18%-31%），RSR13给药后平均增加53%（范围为36%-76%）。在RSR4或RSR13注射前及注射后长达40分钟，使用O2微电极连续测量大腿肌肉中的组织PO2。给药后20至40分钟，麻醉小鼠中RSR4给药后组织PO2平均增加78%（范围为30%-127%），RSR13给药后平均增加66%（范围为39%-97%）。麻醉对照组中未观察到组织PO2的变化。