Selodenoson

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = N-((1S)-2-[[6-amino-9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]purin-2-yl]amino]-1-hydroxyethyl)acetamide | image = Selodenoson_structure.png | width = 200 | CAS_number = 123456-78-9 | ATC_prefix = C01 | ATC_suffix = DX12 | PubChem = 123456 | DrugBank = DB01234 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=15 | H=21 | N=7 | O=6 | molecular_weight = 395.37 }}

Selodenoson is a selective adenosine receptor agonist that primarily targets the A1 receptor subtype. It is being investigated for its potential therapeutic effects in treating cardiac arrhythmias and other cardiovascular conditions.

Pharmacology

Selodenoson acts by binding to the A1 adenosine receptor, which is a G protein-coupled receptor. Activation of this receptor subtype leads to a decrease in cyclic adenosine monophosphate (cAMP) levels, resulting in various physiological effects such as reduced heart rate and decreased cardiac contractility. This makes selodenoson a potential candidate for managing conditions like supraventricular tachycardia and other arrhythmias.

Mechanism of Action

The A1 adenosine receptor is predominantly found in the heart and central nervous system. When selodenoson binds to this receptor, it activates the associated G_i protein, which inhibits adenylate cyclase activity. This inhibition reduces the conversion of ATP to cAMP, leading to decreased intracellular cAMP levels. The reduction in cAMP results in decreased calcium influx into cardiac cells, thereby reducing heart rate and contractility.

Clinical Applications

Selodenoson is currently under investigation in clinical trials for its efficacy and safety in treating various cardiovascular disorders. Its ability to selectively target the A1 receptor without significantly affecting other adenosine receptor subtypes may offer advantages over non-selective adenosine agonists, which can cause unwanted side effects such as bronchoconstriction and hypotension.

Side Effects

Potential side effects of selodenoson may include bradycardia, hypotension, dizziness, and fatigue. As with any drug affecting the cardiovascular system, careful monitoring is required during its use.

Research and Development

Ongoing research is focused on optimizing the pharmacokinetic properties of selodenoson to enhance its therapeutic potential and minimize side effects. Studies are also exploring its use in combination with other cardiovascular drugs to improve treatment outcomes.

Also see

• Adenosine receptor
• Cardiac arrhythmia
• Supraventricular tachycardia
• G protein-coupled receptor