Key result
Prolonged A1 adenosine receptor stimulation with R-PIA reduced renal A1 receptor Bmax by approximately 40% and Gi alpha proteins by 30%, whereas chronic antagonist treatment caused no up-regulation.
Authors
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May inform A1 agonist tachyphylaxis mechanisms in kidney; hypothesis-generating in animals and leaves open human translation.
Lee et al. (2002) studied Renal A1 adenosine receptor regulation. R-phenylisopropyladenosine (R-PIA) vs. Theophylline was evaluated on Renal cortex membrane A1 AR binding (Bmax) and Gi alpha-protein levels. Prolonged A1 adenosine receptor stimulation with R-PIA reduced renal A1 receptor Bmax by approximately 40% and Gi alpha proteins by 30%, whereas chronic antagonist treatment caused no up-regulation.
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