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Chemical Compound Review:

DEPX 1,3-diethyl-8-phenyl-7H- purine-2,6-dione

Synonyms: Lopac-A-003, CHEMBL11348, AG-J-63364, SureCN1321894, CHEBI:108548, ...

Ukena, D. et al., Jarvis, M.F. et al., Coulson, R. et al., Rauca, C. et al.

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Disease relevance of NCGC00014999-01

The adenosine A1 receptor antagonist 1,3-diethyl-8-phenylxanthine (DPX), administered at a dose of 0.1 mg/kg s.c. before hypoxia, blocked the decrease in the susceptibility to the convulsive effect of PTZ [1].

High impact information on NCGC00014999-01

The potency order for adenosine antagonists was CGS 15943 (IC50 = 5 nM) greater than 8-phenyltheophylline greater than 1,3-dipropyl-8-(4-amino-2-chloro)phenylxanthine greater than 1,3-diethyl-8-phenylxanthine greater than theophylline = caffeine (IC50 greater than 10,000 nM) [2].
1,3-Diethyl-8-phenylxanthine (DPX) a potent adenosine receptor antagonist, increased urine volume, glomerular filtration rate, vascular resistance and the fractional excretions of Na, K, Ca and Pi in the IPRK [3].

Associations of NCGC00014999-01 with other chemical compounds

However, the A1 receptor selective antagonists 1,3-diethyl-8-phenylxanthine and 1,3-dipropyl-8-cyclopentylxanthine are comparatively potent inhibitors of PDE IV activity with IC50 values in the 10 microM range and are, therefore, nearly as potent as the PDE IV selective inhibitor, rolipram [4].

References

Moderate hypoxia reduces pentylenetetrazol-induced seizures. Rauca, C., Rüthrich, H.L. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
Characterization of the binding of a novel nonxanthine adenosine antagonist radioligand, [3H]CGS 15943, to multiple affinity states of the adenosine A1 receptor in the rat cortex. Jarvis, M.F., Williams, M., Do, U.H., Sills, M.A. Mol. Pharmacol. (1991) [Pubmed]
Xanthine effects on renal proximal tubular function and cyclic AMP metabolism. Coulson, R., Scheinman, S.J. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes. Ukena, D., Schudt, C., Sybrecht, G.W. Biochem. Pharmacol. (1993) [Pubmed]

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