Bisubstrates:物质与肾contraluminal有机阴离子和有机阳离子运输系统。azepines胺,哌啶,哌嗪类,吡啶、喹啉类药物,咪唑类、噻唑、胍和肼。

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乌尔里希KJ, Rumrich G,大卫·C Fritzsch G

Bisubstrates:物质与肾contraluminal有机阴离子和有机阳离子运输系统。azepines胺,哌啶,哌嗪类,吡啶、喹啉类药物,咪唑类、噻唑、胍和肼。

弗鲁格拱门。1993年11月,425 (3 - 4):280 - 99。

PubMed ID

8309790 (在PubMed

]

文摘

为了评估是否N-containing基质相互作用的有机“负离子”(p-aminohippurate PAH)或只与有机阳离子”(N1-methylnicotinamide NMeN)传输系统或与,的截流管周毛细血管microperfusion方法应用于大鼠原位肾和明显的吻值的几类或有机基质对contraluminal NMeN和PAH交通测定。有机阴离子和有机阳离子“运输单引号,因为无论是散装运输车将电离度的解决方案,他们也接受nonionizable基质(乌尔里希KJ, Rumrich G(1992)弗鲁格拱421:286 - 288]。必须充分疏水性胺(苯基乙胺、哌啶、哌嗪)为了与NMeN运输。额外的Cl, Br, NO2或其他电负性群体呈现抑制对多环芳烃运输。这样bisubstrate胺被确定如下:胃复安,bromopride,苯海拉明,溴苯醇胺,维拉帕米,西酞普兰,氯胺酮,甲氟喹合成,ipsapirone,丁螺环酮,曲唑酮,H7和三氟啦嗪。咪唑类似物与两种转运蛋白(如果它们承担充分疏水烷基或芳基组或电负性sidegroups。Bisubstrate咪唑磺甲硝咪唑类似物,毛果芸香碱、氯压定azidoclonidine和西咪替丁。吡啶和噻唑与NMeN运输车如果他们有一个额外的ring-attached氨基集团。再次与额外的Cl, Br,或NO2组氨基比林和氨噻唑也成为PAH运输车的抑制剂。在胍只有物质等电负性side-groups胍法辛,阿米洛利,benzylamiloride和雷尼替丁,转运蛋白相互作用。 Amongst the phenylhydrazines only 4-bromophenylhydrazine interacts with the NMeN transporter and 4-nitrophenylhydrazine with both transporters. Quinoline (isoquinoline) and its amino and hydroxy analogues interact with both transporters, their pKa values correlate directly with the affinity to the NMeN transporter and reciprocally with their affinity to the PAH transporter. In experiments with labelled substrates only the sufficiently hydrophilic cimetidine, amiloride and ranitidine show a saturable transport, which can be inhibited by probenecid (apalcillin) and tetraethylammonium in an additive manner. The highly hydrophobic substrates verapamil, citalopram, imipramine, diltiazem and clonidine enter the cell very fast in an unsaturable and uninhibitable manner, apparently in the undissociated form, since N-methyl-4-phenylpyridinium, which--disregarding its ionization--is similarly hydrophobic, shows a transport behaviour similar to that of tetraethylammonium [Ullrich et al. (1991) Pflugers Arch 419:84-92]. Ethidium bromide and dimidium bromide, which have a permanent cationic quaternary nitrogen and two sufficiently electronegative NH2 groups, also interact with both transporters.(ABSTRACT TRUNCATED AT 400 WORDS)

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药物转运蛋白

药物	转运体	类	生物	药理作用	行动
溴苯醇胺	溶质载体家庭22个成员6	蛋白质	人类	未知的	不可用	细节