Corpus ID: 347428

Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.

  title={Pharmacological characterization of CGS 15943A: a novel nonxanthine adenosine antagonist.},
  author={Geetha Ghai and Joseph Francis and M. Williams and Ronald Dotson and Maria Hopkins and D T Cot{\'e} and F. R. Goodman and Mark B. Zimmerman},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={242 3},
CGS 15943A is a potent adenosine receptor antagonist with a novel nonxanthine heterocyclic ring structure. In vitro, CGS 15943A competitively inhibited the 2-chloroadenosine-induced A2 receptor-mediated relaxation of dog coronary artery strips contracted with KCl (25 mM). Similarly, CGS 15943A blocked 2-chloroadenosine- and N-ethylcarboxamideadenosine-induced A2 receptor-mediated relaxation of histamine-contracted guinea pig tracheal strips. Schild analysis of these results yielded pA2 values… Expand
Comparative effects of a selective adenosine A2 receptor agonist, CGS 21680, and nitroprusside in vascular smooth muscle.
The adenosine A2 receptor agonists, NECA and CGS 21680, are potent vasorelaxants that display regional vascular and species variations that differ from those of nitroprusside. Expand
Effects of CGS-15943A on the relaxations produced by adenosine analogs in human blood vessels.
Cor coronary arteries are more responsive than mammary arteries or saphenous veins to the relaxing effects of adenosine analogs and that these relaxing responses are dependent on the contracting agent. Expand
CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and caffeine-tolerant rats.
The results suggest that caffeine and CGS 15943 increase locomotor activity by a common mechanism of action possibly involving adenosine receptors or a cellular element conformationally similar to adenosines receptors. Expand
In vivo characterisation of ZM 241385, a selective adenosine A2A receptor antagonist.
The results indicate that ZM 241385 can be used to evaluate the role of adenosine A2A receptors in the action ofAdenosine in vivo and that it was 140-fold more potent in attenuating vasodilator responses to exogenous adenosines in the constant flow perfused hind limb than the bradycardic effects. Expand
Adenosine A2 receptor function in rat ventricular myocytes.
The results suggest the presence of adenosine A2a receptors in the rat ventricular myocyte that appear to be responsible for an increase in inotropy via cAMP-dependent and -independent mechanisms. Expand
Comparison of the behavioural effects of an adenosine A1/A2-receptor antagonist, CGS 15943A, and an A1-selective antagonist, DPCPX
The present data show that CGS 15943A increased in a dose-dependent manner locomotor activity of mice confronted with a free exploratory test without markedly modifying rears or, at low or medium doses, novelty seeking responses. Expand
Influence of CGS 15943 A (a nonxanthine adenosine antagonist) on the protection offered by a variety of antiepileptic drugs against maximal electroshock-induced seizures in mice
The protection provided by common antiepileptic drugs against electroconvulsions seems independent of adenosine-mediated inhibition, and the involvement of purinergic transmission in the final anticonvulsant effect may be suggested. Expand
Adenosine antagonists as potential therapeutic agents
The availability of such novel entities may permit the development of a new class of therapeutic agents able to affect neuromodulator, as opposed to neurotransmitter, function. Expand
Stimulation of the A2A adenosine receptor increases expression of the tyrosine hydroxylase gene.
  • H. Chae, K. Kim
  • Biology, Medicine
  • Brain research. Molecular brain research
  • 1997
The results suggest that stimulation of the A2A adenosine receptor leads to an elevated expression of the TH gene by changing the binding pattern of DNA binding proteins that interact with CRE through activation of protein kinase A. Expand
The effects of selective A1 and A2a adenosine receptor antagonists on cerebral ischemic injury in the gerbil
The results suggest that adenosine A2a receptor antagonists may be useful for the prevention of cerebral injuries resulting from stroke or cardiac arrest. Expand