Mehta V D, Sivasubramanian A, Kulkarni P V, Mason R P, Antich P P
Department of Radiology, University of Texas Southwestern Medical Center, Dallas 75235, USA.
Bioconjug Chem. 1996 Sep-Oct;7(5):536-40. doi: 10.1021/bc9600527.
Fluorinated macromolecular probes (6-fluoropyridoxal-polymer conjugates) have been synthesized and characterized as potential pH indicators for magnetic resonance spectroscopy and imaging applications. The 19F pH sensor 2-fluoro-5-hydroxy-3-(hydroxymethyl)-6-methyl-4-pyridinecarboxal-+ ++dehyde (6-fluoropyridoxal; 2) has been conjugated to carrier molecules (polyamino dextran, polylysine, and albumin) by reductive alkylation for enhanced vascular retention and tissue targeting. The pH indicator polymer conjugates were purified by exhaustive dialysis and isolated in good yields (66-84%). The 6-fluoropyridoxal-polymer conjugates exhibit excellent 19F pH sensitivity and pKa suitable for in vivo studies. The potential application of these polymeric indicators has been demonstrated in whole blood. These novel macromolecular pH probes offer a new approach for studying tissue physiology.
含氟大分子探针（6-氟吡哆醛-聚合物缀合物）已被合成并表征为用于磁共振波谱和成像应用的潜在pH指示剂。19F pH传感器2-氟-5-羟基-3-（羟甲基）-6-甲基-4-吡啶甲醛（6-氟吡哆醛；2）已通过还原烷基化与载体分子（聚氨基葡聚糖、聚赖氨酸和白蛋白）缀合，以增强血管滞留和组织靶向性。pH指示剂聚合物缀合物通过彻底透析纯化，并以良好的产率（66-84%）分离得到。6-氟吡哆醛-聚合物缀合物表现出优异的19F pH敏感性和适合体内研究的pKa。这些聚合物指示剂的潜在应用已在全血中得到证明。这些新型大分子pH探针为研究组织生理学提供了一种新方法。
