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Chemical Compound Review:

HK-2 1,2-diethyl-3-hydroxy- pyridin-4-one

Synonyms: CHEMBL72457, CP94, SureCN868431, CCRIS 9395, AG-D-37091, ...

Epemolu, R.O. et al., Singh, S. et al., Fredenburg, A.M. et al., Chang, S.C. et al., Wang, Q. et al., et al.

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Disease relevance of 115900-75-9

Desferrioxamine and CP94 (1,2-diethyl-3-hydroxypyridin-4-one) are metal chelators used or proposed for use in the clinical treatment of iron overload [1].

High impact information on 115900-75-9

2. The large depolarizing potentials were reversibly inhibited by the Zn2+ chelator 1,2-diethyl-3-hydroxypyridin-4-one (CP94) [2].
The urinary metabolic profiles of two novel orally active iron chelators, 1,2-dimethyl-3-hydroxypyridin-4-one (CP20 or L1) and 1,2-diethyl-3-hydroxypyridin-4-one (CP94), have been studied in rats [3].
The pharmacokinetics of 1,2-diethyl-3-hydroxypyridin-4-one (CP94) in rats [4].
In addition, the iron chelator 1,2-diethyl-3-hydroxypyridin-4-one (CP94) was used [5].

Biological context of 115900-75-9

Contrasting interspecies efficacy and toxicology of 1,2-diethyl-3-hydroxypyridin-4-one, CP94, relates to differing metabolism of the iron chelating site [6].
This paper assesses the in vivo effect of a new iron chelator, 1,2-diethyl-3-hydroxypyridin-4-one (CP94), on the kinetics of PpIX in different layers of the bladder wall [7].

Associations of HK-2 with other chemical compounds

The uptake of D-lactate and butyrate by HK-2 cells was inhibited by MCT analogues and the classical MCT inhibitors alpha-cyano-4-hydroxycinnamate, pCMB, and phloretin [8].

Analytical, diagnostic and therapeutic context of 115900-75-9

Each of 12 rabbits was administered 0.45 mmol/kg 1,2-dimethyl- (CP20; L1) and of 1,2-diethyl-3-hydroxypyridin-4-one (CP94; EL1NEt) by gastric lavage and by injection into a lateral ear vein [9].
A sensitive and selective high-performance liquid chromatographic (HPLC) method for the analysis of 1,2-diethyl-3-hydroxypyridin-4-one (CP94, I) and its 2-(1-hydroxyethyl) metabolite (II) in rat blood is described [10].

References

Cellular uptake and release of two contrasting iron chelators. Cable, H., Lloyd, J.B. J. Pharm. Pharmacol. (1999) [Pubmed]
Modulation of GABA-mediated synaptic transmission by endogenous zinc in the immature rat hippocampus in vitro. Xie, X., Hider, R.C., Smart, T.G. J. Physiol. (Lond.) (1994) [Pubmed]
Urinary metabolic profiles in human and rat of 1,2-dimethyl- and 1,2-diethyl-substituted 3-hydroxypyridin-4-ones. Singh, S., Epemolu, R.O., Dobbin, P.S., Tilbrook, G.S., Ellis, B.L., Damani, L.A., Hider, R.C. Drug Metab. Dispos. (1992) [Pubmed]
The pharmacokinetics of 1,2-diethyl-3-hydroxypyridin-4-one (CP94) in rats. Epemolu, O.R., Singh, S., Hider, R.C., Damani, L.A. Drug Metab. Dispos. (1992) [Pubmed]
A hydroxypyridinone (CP94) enhances protoporphyrin IX formation in 5-aminolaevulinic acid treated cells. Bech, O., Phillips, D., Moan, J., MacRobert, A.J. J. Photochem. Photobiol. B, Biol. (1997) [Pubmed]
Contrasting interspecies efficacy and toxicology of 1,2-diethyl-3-hydroxypyridin-4-one, CP94, relates to differing metabolism of the iron chelating site. Porter, J.B., Abeysinghe, R.D., Hoyes, K.P., Barra, C., Huehns, E.R., Brooks, P.N., Blackwell, M.P., Araneta, M., Brittenham, G., Singh, S. Br. J. Haematol. (1993) [Pubmed]
The efficacy of an iron chelator (CP94) in increasing cellular protoporphyrin IX following intravesical 5-aminolaevulinic acid administration: an in vivo study. Chang, S.C., MacRobert, A.J., Porter, J.B., Bown, S.G. J. Photochem. Photobiol. B, Biol. (1997) [Pubmed]
Characterization of monocarboxylate transport in human kidney HK-2 cells. Wang, Q., Lu, Y., Yuan, M., Darling, I.M., Repasky, E.A., Morris, M.E. Mol. Pharm. (2006) [Pubmed]
Pharmacokinetics of representative 3-hydroxypyridin-4-ones in rabbits: CP20 and CP94. Fredenburg, A.M., Wedlund, P.J., Skinner, T.L., Damani, L.A., Hider, R.C., Yokel, R.A. Drug Metab. Dispos. (1993) [Pubmed]
High-performance liquid chromatographic determination of 1,2-diethyl-3-hydroxypyridin-4-one and its 2-(1-hydroxyethyl) metabolite in rat blood. Epemolu, R.O., Singh, S., Hider, R.C., Damani, L.A. J. Chromatogr. (1992) [Pubmed]

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