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.
Wittendorp
Maria C
MC
Department of Medical Physiology, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
von Frijtag Drabbe Künzel
Jacobien
J
Ijzerman
Adriaan P
AP
Boddeke
Hendrikus W G M
HW
Biber
Knut
K
D000595:Amino Acid Sequence; D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D016466:CHO Cells; D003001:Cloning, Molecular; D005576:Colforsin / Q000494:pharmacology; D006224:Cricetinae; D000242:Cyclic AMP / Q000096:biosynthesis; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D008969:Molecular Sequence Data; D009457:Neuroglia / Q000378:metabolism; D011869:Radioligand Assay; D043682:Receptor, Adenosine A1 / Q000096:biosynthesis* / Q000187:drug effects*; D020133:Reverse Transcriptase Polymerase Chain Reaction; D013045:Species Specificity
D007202:Indicators and Reagents; D043682:Receptor, Adenosine A1; D005576:Colforsin; D000242:Cyclic AMP