Reaction participants Show >> << Hide
- Name help_outline creatinine Identifier CHEBI:16737 (CAS: 60-27-5) help_outline Charge 0 Formula C4H7N3O InChIKeyhelp_outline DDRJAANPRJIHGJ-UHFFFAOYSA-N SMILEShelp_outline CN1CC(=O)NC1=N 2D coordinates Mol file for the small molecule Search links Involved in 4 reaction(s) Find molecules that contain or resemble this structure Find proteins in UniProtKB for this molecule
Cross-references
| RHEA:74539 | RHEA:74540 | RHEA:74541 | RHEA:74542 | |
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| Reaction direction help_outline | undefined | left-to-right | right-to-left | bidirectional |
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Publications
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Interactions of fluoroquinolone antibacterials, DX-619 and levofloxacin, with creatinine transport by renal organic cation transporter hOCT2.
Okuda M., Kimura N., Inui K.
Interactions of DX-619, a novel fluoroquinolone antibacterial, and levofloxacin (LVFX) with the human renal organic cation transporter hOCT2 were studied. The intracellular accumulation of [(14)C]creatinine in stable transfectants of HEK293 cells expressing hOCT2 (hOCT2-HEK293) as well as vector-t ... >> More
Interactions of DX-619, a novel fluoroquinolone antibacterial, and levofloxacin (LVFX) with the human renal organic cation transporter hOCT2 were studied. The intracellular accumulation of [(14)C]creatinine in stable transfectants of HEK293 cells expressing hOCT2 (hOCT2-HEK293) as well as vector-transfected HEK293 cells (VEC-HEK293) was evaluated in the presence of DX-619 and LVFX at various concentrations. When added extracellularly, both DX-619 and LVFX inhibited the uptake of [(14)C]creatinine (5 microM) by hOCT2-HEK293 cells in a dose-dependent manner. Unlike in hOCT2-HEK293 cells, the uptake in VEC-HEK293 cells was not inhibited by either fluoroquinolone suggesting that hOCT2 was specifically involved in the inhibition. The apparent IC(50) value for the inhibition of [(14)C]creatinine uptake in hOCT2-HEK293 cells was 1.29+/-0.23 microM for DX-619 and 127+/-27 microM for LVFX, indicating DX-619 to be approximately 100-fold more potent than LVFX at inhibiting the transport of [(14)C]creatinine by hOCT2. A Dixon plot revealed that the inhibition by DX-619 of the hOCT2-mediated transport of [(14)C]creatinine was competitive. Fluoroquinolone antibacterials have the ability to inhibit the transport of creatinine by hOCT2, with DX-619 being much more effective than LVFX. << Less
Drug Metab. Pharmacokinet. 21:432-436(2006) [PubMed] [EuropePMC]
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Creatinine transport by basolateral organic cation transporter hOCT2 in the human kidney.
Urakami Y., Kimura N., Okuda M., Inui K.
<h4>Purpose</h4>Creatinine is excreted into urine by tubular secretion in addition to glomerular filtration. The purpose of this study was to clarify molecular mechanisms underlying the tubular secretion of creatinine in the human kidney.<h4>Methods</h4>Transport of [14C]creatinine by human organi ... >> More
<h4>Purpose</h4>Creatinine is excreted into urine by tubular secretion in addition to glomerular filtration. The purpose of this study was to clarify molecular mechanisms underlying the tubular secretion of creatinine in the human kidney.<h4>Methods</h4>Transport of [14C]creatinine by human organic ion transporters (SLC22A) was assessed by HEK293 cells expressing hOCT1, hOCT2, hOCT2-A, hOAT1, and hOAT3.<h4>Results</h4>Among the organic ion transporters examined, only hOCT2 stimulated creatinine uptake when expressed in HEK293 cells. Creatinine uptake by hOCT2 was dependent on the membrane potential. The Michaelis constant (Km) for creatinine transport by hOCT2 was 4.0 mM, suggesting low affinity. Various cationic drugs including cimetidine and trimethoprim, but not anionic drugs, markedly inhibited creatinine uptake by hOCT2.<h4>Conclusion</h4>These results suggest that hOCT2, but not hOCT1, is responsible for the basolateral membrane transport of creatinine in the human kidney. << Less