PSB-10 is a drug which acts as a selective antagonist for the adenosine A₃

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 ...

(k_i value at human A₃ receptor is 0.44 nM), with high selectivity over the other three

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 ...

subtypes (k_i values at human A₁, A_2A and A_2B receptors are 4.1, 3.3 and 30 μM). Further pharmacological experiments in a sup>35STPγS binding assay using hA₃-CHO-cells indicated that PSB-10 acts as an inverse agonist (IC₅₀ = 4 nM). It has been shown to produce

antiinflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs remedy pain by reducing inflammation as ...

effects in animal studies. Simple

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 ...

derivatives such as

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 ...

and

DPCPX 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX, PD-116,948) is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor. It has high selectivity for A1 over other adenosine receptor subtypes, but as with other xanthine ...

have generally low affinity for the A₃ subtype and must be extended by expanding the ring system and adding an aromatic group to give high A₃ affinity and selectivity. The affinity towards adenosine A₃ subtype was measured against the radioligand PSB-11.

References

Chlorobenzenes Purines Lactams Adenosine receptor antagonists {{nervous-system-drug-stub