Characterization of the adenosine A1 receptor in summer and winter Arctic ground squirrels

Abstract

Hibernation is an adaptation that allows the Arctic ground squirrel (Urocitellus parryii) to survive the harsh arctic winter. Recently the activation of the Adenosine A1 receptor (A₁AR) has been shown to be necessary for entrance into hibernation during the winter but not summer season. In the current study we characterize the A₁AR in the forebrain, hippocampus and hypothalamus of summer and winter AGS. We also tested the hypothesis that increased A₁AR agonist efficacy is responsible for increased sensitization of the A₁AR during the winter season. The resulting ³⁵S-GTPγS binding data indicated an increase in agonist potency during the winter season in all three brain regions. A plausible explanation of our results is that increased potency in the forebrain during the winter season is due to an increase in efficacy as indicated by a greater number of receptors in the high affinity state. In addition ³⁵S-GTPγS binding, [³H] DPCPX saturation and competition assays establish for the first time pharmacological characteristics such as EC⁵⁰, Kd, Kilo and Kihi in AGS brain.