CGS-15943 is a
drug which acts as a
potent and reasonably selective
antagonist for the
adenosine receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
s
A1 and
A2A, having a
Ki of 3.3nM at A
2A and 21nM at A
1. It was one of the first
adenosine receptor
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a di ...
antagonists discovered that is not a
xanthine
Xanthine ( or ; archaically xanthic acid; systematic name 3,7-dihydropurine-2,6-dione) is a purine base found in most human body tissues and fluids, as well as in other organisms. Several stimulants are derived from xanthine, including caffeine ...
derivative, instead being a triazoloquinazoline.
Consequently, CGS-15943 has the advantage over most xanthine derivatives that it is not a
phosphodiesterase inhibitor
A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE), thereby preventing the inactivation of the intracellular second messengers, cyclic adenosine monophosphate (cAMP) and cyc ...
, and so has more a specific pharmacological effects profile. It produces similar effects to
caffeine
Caffeine is a central nervous system (CNS) stimulant of the methylxanthine class. It is mainly used recreationally as a cognitive enhancer, increasing alertness and attentional performance. Caffeine acts by blocking binding of adenosine to ...
in animal studies, though with higher potency.
See also
*
ATL-444
ATL-444 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A. It has been used to study the role of the adenosine receptor system in the reinforcing action of cocaine, as well as the devel ...
*
SCH-58261
SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A2A, with more than 50x selectivity for A2A over other adenosine receptors. It has been used to investigate the mechanism of action of caffeine, whic ...
References
Adenosine receptor antagonists
Experimental drugs
2-Furyl compounds
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