Pharmacological characterization of a new purinergic receptor site in rabbit aorta

Gen Pharmacol. 1992 Nov;23(6):1067-71. doi: 10.1016/0306-3623(92)90288-u.

Abstract

1. The pharmacological properties of a vasodilating purine-activated receptor that is not a P1 or P2-purinoceptor were investigated. 2. In rabbit isolated thoracic aorta precontracted with noradrenaline, ATP induced a 50% relaxation at 0.25 mM (EC 50%); in the absence of endothelium, EC 50% was 2.5 mM. 3. Adenosine induced a relaxation that was not different in both the presence and absence of endothelium, being EC 50% 0.48 and 0.37 mM, respectively. 4. The potent and selective P2y-purinoceptor agonist 2-methylthio-ATP (0.03-10 microM) induced a relaxation only in the presence of endothelium. 5. In de-endothelialized aorta, 8-phenyltheophilline (8-PT: P1 antagonist) and 3,7-dimethyl-1-propargylxanthine (DMPX: A2 antagonist) did not antagonize ATP- and adenosine-induced relaxation. 6. The present data support the presence of a new site of action for purines in rabbit isolated thoracic aorta. 7. A P3 subtype of purinoceptor, that may be identified in the hypothesized "nucleotide" receptor, is proposed.

MeSH terms

  • Adenosine / pharmacology
  • Adenosine Triphosphate / analogs & derivatives
  • Adenosine Triphosphate / pharmacology
  • Animals
  • Aorta, Thoracic / drug effects
  • In Vitro Techniques
  • Male
  • Muscle Relaxation / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Rabbits
  • Receptors, Purinergic / drug effects*
  • Theophylline / analogs & derivatives
  • Theophylline / pharmacology
  • Thionucleotides / pharmacology
  • Vasodilation / drug effects

Substances

  • Receptors, Purinergic
  • Thionucleotides
  • Adenosine Triphosphate
  • Theophylline
  • 8-phenyltheophylline
  • Adenosine
  • 2-methylthio-ATP