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J Appl Physiol 53: 731-736, 1982;
8750-7587/82 $5.00
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Journal of Applied Physiology, Vol 53, Issue 3 731-736, Copyright © 1982 by American Physiological Society

ARTICLES

Rat lung cholinergic receptor: characterization and regulation by corticosteroids

D. L. Marquardt, H. J. Motulsky and S. I. Wasserman

Muscarinic cholinergic receptors have been implicated in the regulation of bronchomotor tone, bronchial mucus secretion, and lung mast-cell mediator release. Rat lung membranes prepared by homogenization, sonication, and sedimentation of 37,000 g in sucrose have been demonstrated to possess muscarinic cholinergic receptors as assessed by radioligand binding employing l-quinuclidinyl[phenyl-4-3H]benzilate ([3H]QNB). QNB binding was saturable, stereoselective, and reversible in the presence of 1 microM atropine. The rat lung muscarinic receptor demonstrated a Kd of 0.268 +/- 0.126 (+/- SD) nM and a density of 35.4 +/- 4.6 fmol/mg protein by Scatchard analysis. The Hill coefficient was 1.015 +/- 0.085, indicating noncooperative binding. Muscarinic cholinergic receptors in the rat lung were equal in number to alpha 1-adrenergic receptors, but beta-adrenergic receptors are 14 times more prevalent as defined by [3H]prazosin and l-[propyl-2, 3-3H]dihydroalprenolol ([3H]DNA) binding. Dexamethasone (140 micrograms) administration in vivo caused an increase in all three receptor types by 24-48 h, suggesting steroids regulate not only the number of beta-receptors but also that of alpha- and cholinergic receptors. These data suggest new avenues by which steroids may regulate lung function.


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