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Am J Physiol Endocrinol Metab 250: E583-E590, 1986;
0193-1849/86 $5.00
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AJP - Endocrinology and Metabolism, Vol 250, Issue 5 583-E590, Copyright © 1986 by American Physiological Society

ARTICLES

Desensitization and redistribution of beta-adrenergic receptors on human mononuclear leukocytes

H. J. Motulsky, E. M. Cunningham, A. DeBlasi and P. A. Insel

We have used intact human mononuclear leukocytes (MNL) to examine desensitization of beta-adrenergic receptors in normal mammalian cells. MNL were prepared and radioligand binding experiments were performed at 4 degrees C. At this temperature the ligand [125I]iodocyanopindolol ([125I]ICYP) identified the same number of receptors as at 37 degrees C, and the agonist isoproterenol competed for this binding with high affinity (dissociation constant, Ki = 20 nM). At 37 degrees C, results were similar when the binding incubation was terminated after 1 min, but the apparent affinity of the receptors for isoproterenol was several 100-fold lower when the incubation was allowed to reach steady state. In desensitized MNL (prepared by incubating whole blood with 10 microM isoproterenol at 37 degrees C for 10 min, and then isolating and washing the MNL at 4 degrees C), isoproterenol-stimulated cAMP accumulation was reduced 63 +/- 4%. After desensitization, the total number of beta-receptors was unchanged, but isoproterenol and the hydrophilic antagonist CGP-12177 were able to compete with [125I]ICYP for binding to only 18 +/- 6% of these sites. Direct binding with [3H]CGP-12177 yielded similar results. These results demonstrate that isoproterenol promotes a rapid desensitization of beta-adrenergic receptors on MNL and a concomitant redistribution of receptors into a cellular compartment to which some ligands (including catecholamines) have restricted access. The findings demonstrate that redistribution of beta-receptors may be a mechanism mediating desensitization to catecholamines in normal mammalian cells.


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N. Fujii, S. Homma, F. Yamazaki, R. Sone, T. Shibata, H. Ikegami, K. Murakami, and H. Miyazaki
beta -Adrenergic receptor number in human lymphocytes is inversely correlated with aerobic capacity
Am J Physiol Endocrinol Metab, June 1, 1998; 274(6): E1106 - E1112.
[Abstract] [Full Text] [PDF]


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