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This study was undertaken to clarify whether beta-adrenergic receptor (beta-AR) translocation from intracellular sites to the cell surface contributes to an increase in the number of beta-AR in lymphocytes from trained and untrained men after exercise. Nine trained and 9 untrained subjects performed exercise on a bicycle ergometer until exhaustion. The number of beta-AR in the cell surface (beta-AR(surface)) and intracellular sites (beta-AR(intra)) was determined at rest and after maximal exercise by measuring the binding of the radioligand 125I-iodocyanopindolol in the presence or absence of hydrophilic (CGP-12177A) or lipophilic (propranolol) unlabeled ligands. The number of beta-AR(surface) increased after exercise from 1,524.4 +/- 321.4 to 3,432.6 +/- 503.3 sites/cell (p &lt; 0.01), whereas that of beta-AR(intra) decreased from 356.2 +/- 85.7 to 190.3 +/- 60.2 sites/cell (p &lt; 0.05). The isoproterenol-stimulated cAMP production per 1 x 10(6) lymphocytes after exercise was significantly higher than that at rest. However, the cAMP production per single beta-AR(surface) tended to be lower after exercise. No differences between the trained and untrained subjects were found in beta-AR numbers or intracellular cAMP levels. These findings demonstrate that maximal exercise induces the translocation of beta-AR from intracellular sites to the cell surface in human lymphocytes. However, this translocation accounts for only 10% of the increase in total cellular beta-AR, suggesting that other mechanisms are predominant and contribute substantially to the increase in beta-AR(surface).

Exercise-lnduced Change in .BETA.-Adrenergic Receptor Number in Lymphocytes from Trained and Untrained Men.