The variation of drug concentration in blood samples with time can be assayed by different spectroscopic and chromatographic methods. A better understanding of pharmacokinetics could be achieved by on-line, within-animal drug monitoring. The first application of X-band electron paramagnetic resonance (EPR) spectroscopy for <i>in vivo</i> pharmacokinetics was reported by Mader et al., who monitored a spin probe in mouse tail after its percutaneous administration. We recently utilized X-band EPR to monitor the nitroxyl free radical 2,2,5,5-tetramethylpyrrolidine-1-oxy1-3-carboxylic acid (PCA) directly in the circulating blood of artificially ventilated and blood-pressure-controlled rats. In this report we examined the applicability of EPR spectroscopy for <i>in vivo</i> online determination of spin-labeled drugs. Monosialic ganglioside GM1 is a normal component of mammalian cell plasma membranes with relevant therapeutic potential. The effects of GM1 have been investigated on severe neurological syndromes, such as acute ischemic stroke and acute spinal cord injury. In this study, GM1 was spin-labeled with PCA, intravenously administered, and monitored directly in circulating rat blood.
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