Abstract：
:A bicarbonate-dependent organic cation transporter, unique from rOCT1 and rOCT2, primarily mediates amantadine uptake into renal proximal tubules. We examined whether intracellular pH regulates bicarbonate-dependent amantadine transporter function in these tubules. NH(4)Cl treatment resulted in immediate intracellular alkalinization of tubules for up to 30s followed by gradual acidification that was maximal at 5min. Proximal tubule amantadine uptake was similarly inhibited (60%) by NH(4)Cl during both the early intracellular alkalinization and later acidification phases. Sodium propionate treatment resulted in immediate intracellular acidification of proximal tubules without inhibiting amantadine uptake. NH(4)Cl inhibition of bicarbonate-dependent amantadine uptake was dose-dependent, competitive and sex-dependent. NH(4)Cl, NH(4)NO(3), (NH(4))(2)SO(4) and (NH(4))(2)HPO(4) inhibited amantadine uptake into proximal tubules similarly. NH(4)Cl also stimulated efflux of amantadine and tetraethylammonium from preloaded proximal tubules, suggesting mediation of a facilitated process. These data suggest the potential for direct modulation of organic cation transporters by NH(4)(+) in rat kidney proximal tubules.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Goralski KB,Bose R,Sitar DSdoi
10.1016/j.ejphar.2006.04.051subject
Has Abstractpub_date
2006-07-10 00:00:00pages
87-94issue
1-2eissn
0014-2999issn
1879-0712pii
S0014-2999(06)00460-2journal_volume
541pub_type
杂志文章abstract：:We evaluated the effects of ACEA (selective cannabinoid (CB)1 receptor agonist), WIN 55,212-2 mesylate (WIN; non-selective CB1 and CB2 receptor agonist) and N-palmitoylethanolamine (PEA; an endogenous fatty acid of ethanolamide) in DBA/2 mice, a genetic model of reflex audiogenic epilepsy. PEA, ACEA or WIN intraperito...
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journal_title：European journal of pharmacology
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