What drug is an adenosine 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 adenosine triphosphate (ATP), and the pharmaceutical drug regadenoson.
Is adenosine an agonist or antagonist?
Adenosine (1), a non-selective AR agonist, and its derivatives as A1AR-selective agonists, including nucleosides (2–16) and non-nucleosides (17–20).
What does adenosine A1 receptor do?
The role of adenosine in the induction of hippocampal synaptic depression in ischemia/hypoxia through adenosine A1 receptor (A1R) activation is thought to be neuroprotective by preventing excitotoxicity both presynaptically by inhibiting glutamate release [75] and postsynaptically by reducing cellular excitability [19] …
What do adenosine agonists do?
Adenosine release has been shown to occur during seizures; adenosine agonists suppress seizures and raise seizure thresholds; and adenosine antagonists are proconvulsant. These actions are not surprising in view of the powerful inhibitory effect that adenosine has on synaptic activity and neurotransmitter release.
What drugs increase adenosine?
In addition, methylxanthines such as caffeine have profound biological effects as antagonists at adenosine receptors. Moreover, drugs such as dipyridamole and methotrexate act by enhancing the activation of adenosine receptors.
Is an adenosine receptor antagonist?
An adenosine receptor antagonist is a drug which acts as an antagonist of one or more of the adenosine receptors. Examples include caffeine, theophylline, and theobromine.
What is adenosine A1 receptor?
Adenosine A 1 receptor. The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as endogenous ligand .
What is the best A1 adenosine agonist?
Caffeine, as well as theophylline, has been found to antagonize both A 1 and A 2A receptors in the brain. 2-Chloro-N (6)-cyclopentyladenosine ( CCPA ). Tecadenoson is an effective A1 adenosine agonist, as is selodenoson.
What is the role of adenosine A1R agonists in heart failure?
Preclinical data have shown that partial adenosine A1R agonists protect and improve cardiac function at doses that do not result in undesirable effects on heart rate, atrioventricular conduction, and blood pressure, suggesting that these compounds may constitute a valuable new therapy for chronic HF.
How do adenosine A1 receptor agonists inhibit cold-evoked shivering?
As with BAT thermogenesis, either icv or local injection into the NTS of an adenosine A1 receptor agonist inhibits cold-evoked shivering (Tupone et al., 2013 ).