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Related Experiment Videos

Selective bronchodilators from 1-(5'-oxohexyl)xanthines.

K I Miyamoto1, R Sakai, Y Yamamoto

  • 1Research Laboratory for Development of Medicine, School of Pharmacy, Hokuriku University, Kanazawa, Japan.

The Journal of Pharmacy and Pharmacology
|November 1, 1992
PubMed
Summary
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Researchers synthesized novel xanthine derivatives to assess their effects on respiratory and cardiac functions. N3 alkylation enhanced tracheal relaxation, offering potential for selective bronchodilators with reduced cardiac side effects compared to existing treatments.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry

Background:

  • Xanthine derivatives are known for their bronchodilator and cardiac effects.
  • Understanding structure-activity relationships is crucial for developing selective therapeutic agents.

Purpose of the Study:

  • To synthesize and evaluate a series of 1-(5'-oxohexyl)xanthines with varying N3 and N7 alkyl substitutions.
  • To compare their relaxant activity on guinea-pig tracheal muscle and positive chronotropic activity on guinea-pig right atrium.
  • To investigate potential mechanisms of action, including phosphodiesterase (PDE) inhibition and adenosine antagonism.

Main Methods:

  • Synthesis of twenty-one 1-(5'-oxohexyl)xanthine derivatives.
  • In vitro assessment of tracheal relaxant activity in isolated guinea-pig tracheal muscle.

Related Experiment Videos

  • In vitro assessment of positive chronotropic activity in isolated guinea-pig right atrium.
  • Measurement of cAMP-phosphodiesterase (PDE) inhibitory activity and [3H]8-cyclopentyl-1,3-dipropylxanthine binding.

    • Main Results:

    • Tracheal relaxant activity increased with N3 alkyl chain length but decreased with N7 alkylation.
    • Positive chronotropic activity was enhanced by N3 n-propyl but reduced by longer N3 or any N7 alkyl chains.
    • No correlation was found between tracheal relaxant activity, PDE inhibition, and adenosine antagonism.
    • 3-n-Pentyl- and 7-methyl-3-n-pentyl-1-(5'-oxohexyl)xanthines demonstrated superior bronchoselectivity over oxpentifylline and theophylline.

    Conclusions:

    • N3 alkylation is key for achieving selectivity towards tracheal muscle relaxation.
    • Longer alkyl chains at N3 and N7 positions reduce cardiac potency.
    • Novel xanthine derivatives show promise as selective bronchodilators with minimized cardiac effects.