The mouse brain adenosine A1 receptor: functional expression and pharmacology.

The adenosinergic system is involved in many important physiological functions. Adenosine exerts its extracellular effects through four types of G-protein-coupled receptors: A(1), A(2A), A(2B) and A(3). Adenosine acts as an important regulator of metabolic processes. In the brain adenosine mediates prominent neuroprotective functions via the adenosine A(1) receptor. Whereas the pharmacological characteristics of the rat and human adenosine A(1) receptor have been intensively studied, the mouse adenosine A(1) receptor has not yet been characterised. Accordingly, we have cloned the mouse brain adenosine A(1) receptor and present here a pharmacological characterisation of the mouse adenosine A(1) receptor using functional studies and radioligand binding assays. The results show that the binding affinities of several ligands for the mouse adenosine A(1) receptor are similar to the affinities for the rat and human adenosine A(1) receptor with some exceptions.