Adenosine antagonists as potential therapeutic agents

  title={Adenosine antagonists as potential therapeutic agents},
  author={Michael J.A. Williams and Michael F. Jarvis},
  journal={Pharmacology Biochemistry and Behavior},
  • M. Williams, M. Jarvis
  • Published 1 February 1988
  • Biology, Chemistry
  • Pharmacology Biochemistry and Behavior
Adenosine: The prototypic neuromodulator
Pharmacology of adenosine receptors of the rat isolated superior cervical ganglion
This study has examined the effect of purines and pyrimidines on the rat superior cervical ganglion in vitro and found adenosine and its analogues produced concentration dependent hyperpolarisations, suggesting that protein kinase C is involved in the interaction ofadenosine with muscarine.
A safety assessment of fixed combinations of acetaminophen and acetylsalicylic acid, coformulated with caffeine.
Different therapeutic benefits of ASA, acetaminophen and caffeine appear to outweigh any known risk, and it is doubtful if preventing the availability of these products will significantly affect the role of analgesic abuse/overuse in end-stage renal disease.
Adenosine in Central Nervous System Function
Brain adenosine receptors, like those in other tissues (Williams, 1989), can be delineated into two major subclasses, termed A1 and A2 (Hamprecht and Van Calker, 1985), and differentiated by
Anxiolytic effect of carbamazepine in the elevated plus-maze: possible role of adenosine
The present results provide preliminary support for a participation of this neurotransmitter in the anxiolytic action of CBZ, and the combination of an anxiogenic dose with a combination of adenosine receptor antagonist and aminophylline resulted in cancellation of each other effects.


Adenosine receptor binding: structure-activity analysis generates extremely potent xanthine antagonists.
1,3-dipropyl-8-(2-amino-4-chlorophenyl) xanthine, a compound of extraordinary receptor affinity, with a Ki for adenosine A1 receptors of 22 pM, is proposed, which is 4,000,000 times more potent than xanthines itself and 70,000 years more powerful than theophylline.
Adenosine receptors and behavioral actions of methylxanthines.
The data strongly suggest that the behavioral stimulant effects of methylxanthines involve a blockade of central adenosine receptors.
Characterization of adenosine receptors in isolated cerebral arteries of cat
The results are compatible with the opinion thatadenosine relaxes cerebral vessels by an action on adenosine A2‐receptors and may be linked to adenylate cyclase and can be antagonized by 8‐phenyl‐theophylline.
Purine receptors in mammalian tissues: pharmacology and functional significance.
  • M. Williams
  • Biology, Chemistry
    Annual review of pharmacology and toxicology
  • 1987
There is no evidence that specific anabolic processes form adenosine, distinct from those involved in its general metabolic functions, and the physiological factors regulating the extracellular availability of the nucleoside and its distribution make the development of a "purinergic"hesis of neuromodulation difficult.
Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.
During a search for benzodiazepine receptor modulators, a highly potent adenosine antagonist (CGS 15943) was discovered and the synthesis of 2 and some of its analogues and the structure-activity relationships in four biological test systems are described.
Interactions in the behavioral effects of methylxanthines and adenosine derivatives.
The behavioral effects of L-PIA appeared to be mediated in the brain and were not secondary to the cardiovascular effects, indicating a difference in the behavioral profile of these two agents.
Xanthine derivatives as adenosine receptor antagonists.