An adenosine receptor antagonist is a
drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
which acts as an
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
of one or more of the
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 ...
s. The best known are xanthines and their derivatives (natural:
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 t ...
,
theophylline
Theophylline, also known as 1,3-dimethylxanthine, is a phosphodiesterase inhibiting drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the ...
, and
theobromine
Theobromine, also known as xantheose, is the principal alkaloid of ''Theobroma cacao'' (cacao plant). Theobromine is slightly water-soluble (330 mg/L) with a bitter taste. In industry, theobromine is used as an additive and precursor to s ...
; and synthetic:
PSB-1901), but there are also non-xanthine representatives (e.g.
ISAM-140
ISAM-140 is a selective non- xanthinic adenosine A2B receptor atagonist. Discovered in 2016, has a K''i'' of 3.49 nM in A2B receptor and >1000-fold selectivity with respect to the other three adenosine receptor subtypes. It has been shown to ...
, ISAM-R316
Etrumadenant and AZD-4635
)
See also
*
Adenosine receptor agonist
An adenosine receptor agonist is a drug which acts as an agonist of one or more of the adenosine receptors. Examples include the neurotransmitter adenosine, its phosphates, adenosine monophosphate (AMP), adenosine diphosphate (ADP), and adenos ...
*
Adenosine reuptake inhibitor
An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). This i ...
References
Drugs acting on the nervous system
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