Lanman R C, Schanker L S
J Pharmacol Exp Ther. 1980 Dec;215(3):563-8.
The role which carrier-mediated transport and passive diffusion play in the clearance of quaternary ammonium compounds from cerebrospinal fluid was evaluated by ventriculocisternal perfusion in rabbits by using [14C]choline as the primary test compound. Choline was transported out of cerebrospinal fluid by two processes: a saturable, carrier-mediated process with a Tmax of 70.5 ng/min and Kt of 2.2 microgram/min; and, a passive nonsaturable process with a cerebrospinal fluid perfusate clearance of 11.5 microliter/min. N1-methylnicotinamide depressed the clearance of choline as well as that of hexamethonium, suggesting that these cations share a common transport process. Ouabain reduced the clearance of choline and hexamethonium. Passage of choline into brain occurred by passive diffusion.
通过使用[14C]胆碱作为主要测试化合物,对家兔进行脑室池灌注,评估了载体介导转运和被动扩散在脑脊液中季铵化合物清除过程中所起的作用。胆碱通过两种过程从脑脊液中转运出来:一种是可饱和的、载体介导的过程,其最大转运速率(Tmax)为70.5纳克/分钟,转运常数(Kt)为2.2微克/分钟;另一种是被动的、非饱和的过程,脑脊液灌流清除率为11.5微升/分钟。N1-甲基烟酰胺降低了胆碱以及六甲铵的清除率,这表明这些阳离子共享一个共同的转运过程。哇巴因降低了胆碱和六甲铵的清除率。胆碱通过被动扩散进入大脑。