Turnheim K, Lauterbach F
Naunyn Schmiedebergs Arch Pharmacol. 1977 Oct;299(3):201-5. doi: 10.1007/BF00500311.
In anesthetized guinea pigs N-(3H)methylscopolamine (NMScop), N1-(14C)methylnicotinamide (NMN), and (14C)tetraethylammonium (TEA), administered intravenously, were secreted against a concentration gradient into the lumen of the small intestine. The concentration ratio of unmetabolized ammonium base in the intestinal lumen to that in the plasma was 4.3 and 6.5 for NMScop and NMN, respectively, 75 min after the intravenous injection of 1 nmole/g body weight of the individual compounds. The corresponding value for TEA after 180 min was 2.0. The establishment of the concentration gradient between intestinal lumen and plasma was diminished with increasing doses. An excess of NMN inhibited the uphill transport of NMScop. Since the electrical potential difference across the intestinal epithelium and a 'fluid circuit' mechanism cannot solely account for the observed accumulation of the monoquaternary ammonium compounds in the intestinal lumen, the evidence presented supports previous in vitro findings that the small intestine is capable of actively secreting organic cations.
在麻醉的豚鼠中,静脉注射的N-(3H)甲基东莨菪碱(NMScop)、N1-(14C)甲基烟酰胺(NMN)和(14C)四乙铵(TEA)会逆浓度梯度分泌到小肠肠腔中。静脉注射1纳摩尔/克体重的各化合物75分钟后,肠腔中未代谢铵碱与血浆中未代谢铵碱的浓度比,NMScop和NMN分别为4.3和6.5。180分钟后TEA的相应值为2.0。随着剂量增加,肠腔与血浆之间浓度梯度的建立会减弱。过量的NMN会抑制NMScop的上坡转运。由于跨肠上皮的电位差和“流体回路”机制不能单独解释观察到的单季铵化合物在肠腔中的积累,所提供的证据支持了先前的体外研究结果,即小肠能够主动分泌有机阳离子。