Related Experiment Video
Updated: Jun 10, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Progress towards novel adenosine receptor therapeutics gleaned from the recent patent literature
1Novartis Institutes for BioMedical Research, Horsham, West Sussex, UK. neil.press@novartis.com
Importance Of The Field:
The principle of treating disease with selective adenosine receptor ligands has been demonstrated with drugs on the market, while the lesser understood receptor subtypes are still being probed with new and drug-like pharmaceutical tools. The field of adenosine receptor research is, therefore, highly important as an emerging and proven point of intervention in disease.
Areas Covered In This Review:
From 2008 to 2009, > 120 primary patent applications have claimed adenosine receptor ligands, which we analyze by applicant and target. Particularly significant disclosures are described in detail, paying particular attention to the biological data marshalled to support the case.
What The Reader Will Gain:
The first published disclosure of new compounds, compound uses or drug targets is often in the patent literature, which can be difficult to trawl, interpret and verify as it is not subject to peer review. We have critically reviewed this area and share our conclusions regarding progress, trends and identification of early tool compounds or compounds of potential clinical significance ahead of peer-reviewed publication.
Take Home Message:
Adenosine receptor research is a thriving field with continuing claims of exciting new compounds with high specificity and intriguing examples of new uses for such ligands.
Related Concept Videos
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Adrenergic Receptors: ɑ Subtype
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase C—inositol-1,4,5-trisphosphate...
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline moieties. Phenoxybenzamine, with a haloalkylamine...
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Adrenergic Agonists: Direct-Acting Agents
These agents can be classified...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:

