Structure‐Related Inhibitory Effect of Quinolones on Alky1‐Xanthine Elimination in Rats

Takaaki Hasegawa, Takafumi Kuzuya, Ruttikorn Apichartpichean, Masayuki Nadai, Atsumi Nitta, Kenzo Takagi, Toshitaka Nabeshima

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9 Citations (Scopus)


Abstract: To investigate the relationship between the chemical structures of quinolones, enoxacin (ENX) and its analogues, and their metabolic inhibitory effects on theophylline, a xanthine derivative closely related to theophylline, 1‐methyl‐3‐propylxanthine (MPX), was used as a model of theophylline in rats. The disappearance of MPX from plasma was significantly delayed by treatment with ENX and analogue A (derivatives without substituent group at both 3′‐ and 5′‐carbon atom in the piperazinyl ring): total body clearance of MPX was significantly decreased by approximately 50%. However, analogue A was converted into ENX in the rat body (about 14% of dose). Analogues B and C (derivatives with substituent group at 3′‐ or 5′‐carbon atom in the piperazinyl ring) had little or no effect on MPX disposition. No significant change in the volume of distribution of MPX was observed after coadministration with these quinolones. The results of this study indicate that the substitutions on 3′ and 5′‐carbon atoms of piperazinyl ring at 7‐position of the quinolone molecule may play important role in the inhibition of theophylline metabolism. 1991 Nordic Pharmacological Society

Original languageEnglish
Pages (from-to)5-8
Number of pages4
JournalPharmacology & Toxicology
Issue number1
Publication statusPublished - 07-1991
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Toxicology
  • Pharmacology
  • Health, Toxicology and Mutagenesis


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