Rozanov A Ia, Tishchenko D V, Zaporozhchenko A V
Ukr Biokhim Zh (1978). 1993 Jul-Aug;65(4):87-94.
Pharmacokinetics and catabolism to CO2 in the mice organism and metabolic transformation by the tissues homogenates of [1-14C] GABA and its conjugates with nicotinate, pyridoxal phosphate and biotin have been studied. The permeability of nicotinoyl-GABA through the hemato-encephalic barrier was 10 times as much as the corresponding value for GABA and its conjugates with other vitamins. PLP-GABA is eliminated more rapidly from the brain in comparison with GABA, biotinyl-GABA is retained to a higher degree in kidneys, the entero-hepatic recycling takes place more actively for nicotinoyl-GABA. The latter, in contrast to biotinyl-GABA, remains unaffected by the liver, intestine mucose membrane and brain proteases and is catabolized to CO2 to a considerably lower extent as compared with GABA, perhaps due to the intestine bacterial microflora.
研究了[1-14C]γ-氨基丁酸(GABA)及其与烟酸、磷酸吡哆醛和生物素的结合物在小鼠体内的药代动力学、分解为二氧化碳的过程以及组织匀浆中的代谢转化。烟酰-GABA透过血脑屏障的通透性是GABA及其与其他维生素结合物相应值的10倍。与GABA相比,磷酸吡哆醛-GABA从脑中消除得更快,生物素基-GABA在肾脏中保留程度更高,烟酰-GABA的肠肝循环更活跃。与生物素基-GABA相比,后者不受肝脏、肠黏膜和脑蛋白酶的影响,与GABA相比,其分解为二氧化碳的程度要低得多,这可能是由于肠道细菌微生物群的作用。