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Effects of CGS-15943A on the relaxations produced by adenosine analogs in human blood vessels

M H Sabouni1, G L Brown, A N Kotake

  • 1Department of Pharmacology, School of Medicine, East Carolina University, Greenville, NC 27858-4354.

European Journal of Pharmacology
|October 23, 1990
PubMed

Insights

CGS-15943A antagonized adenosine-induced relaxations in human coronary arteries but not in mammary arteries or saphenous veins. This suggests differential adenosine receptor activity in various blood vessels, impacting vasodilation responses.

Area of Science:

  • Pharmacology
  • Cardiovascular Physiology
  • Vascular Biology

Background:

  • Adenosine plays a crucial role in regulating vascular tone.
  • Adenosine receptors are implicated in vasodilation.
  • Understanding differential responses in various blood vessels is key for therapeutic development.

Purpose of the Study:

  • To investigate the in vitro antagonistic effects of CGS-15943A on adenosine-induced relaxations in human blood vessels.
  • To compare the responsiveness of coronary arteries, internal mammary arteries, and saphenous veins to adenosine analogs.
  • To determine the influence of contracting agents on adenosine-mediated vasodilation.

Main Methods:

  • Human coronary arteries, internal mammary arteries, and saphenous veins were isolated.
  • Vessel rings were contracted using KCl or prostaglandin F2 alpha.
  • Concentration-response curves for adenosine and its analogs (NECA, CAD) were generated in the presence and absence of CGS-15943A or 8-phenyltheophylline (8PT).

Main Results:

  • Adenosine and its analogs produced concentration-dependent relaxations in coronary arteries, which were significantly antagonized by CGS-15943A and 8PT.
  • Similar relaxations were observed in mammary arteries and saphenous veins, but they were of smaller magnitude and not antagonized by CGS-15943A.
  • Relaxing responses were influenced by the pre-contracting agent, with papaverine causing complete relaxation in peripheral vessels.

Conclusions:

  • Coronary arteries exhibit greater sensitivity to adenosine analog-induced relaxation compared to mammary arteries and saphenous veins.
  • CGS-15943A specifically antagonizes adenosine responses in coronary arteries, indicating differential receptor pharmacology.
  • The findings highlight the heterogeneity of adenosine receptor-mediated vasodilation across different human vascular beds.

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