The kinetics and metabolism ofl-α-glycerylphosphoryl-choline (α-GPC) were investigated in male and female rats after i.v. (10 mg/kg) and oral doses (100–300 mg/kg). α-GPC was labelled with [14C]-glycerol ([14C]-GPC) or [14C]-choline ([14C]-GPC). Different kinetic and metabolic profiles were observed after i.v. and oral administration. It is assumed that α-GPC is hydrolyzed by phosphodiesterases in the gut mucosa. The different labelled metabolites have different kinetic properties of absorption, distribution and clearance, leading to different blood concentration-time curves of total radioactivity. Both labelled compounds gave a wide distribution of radioactivity, particularly concentrated in the liver, kidney, lung and spleen compared to blood. Brain concentrations of [14C]-GPC were comparable to ([14G]-GPC) or lower than ([14C]-GPC) total blood radioactivity. The metabolite profile in the perfused brain showed a small amount of choline and two unknown metabolites, probably the same as in blood. In addition, choline was incorporated into brain phospholipids in increasing amounts within 24 h of dosing. In all cases renal and fecal excretion of radioactivity was low and comparable for [14G]-GPC and [14C]-GPC. Mostly the administered radioactivity was exhaled as14CO2, this degradation being faster and more pronounced for the glycerol-labelled metabolites than for the choline-labelled metabolites for both routes of administration. In all cases the results were the same for male and female rats.
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Abbiati, G., Fossati, T., Lachmann, G. et al. Absorption, tissue distribution and excretion of radiolabelled compounds in rats after administration of [14C]-l-α-glycerylphosphorylcholine. Eur. J. Drug Metab. Pharmacokinet. 18, 173–180 (1993). https://doi.org/10.1007/BF03188793
- disposition and metabolism