Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange.

J. M. Nunnari, M. G. Repaske, S. Brandon, E. J. Cragoe, L. E. Limbird

Research output: Contribution to journalArticle

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Abstract

Previous reports from this laboratory have demonstrated that alpha 2-adrenergic receptors accelerate Na+/H+ exchange in NG108-15 neuroblastoma X glioma cells and evoke platelet secretion via a pathway involving Na+/H+ exchange. The present studies were designed to examine whether agents that interact with Na+/H+ antiporters also might influence alpha 2-adrenergic receptor-ligand interactions. We observed that Na+ decreases receptor affinity for the agonists epinephrine, norepinephrine, and UK14304 and slightly increases receptor affinity for the antagonists yohimbine and idazoxan in digitonin-solubilized preparations from porcine brain cortex. Increases in [H+] also decrease receptor affinity for agonists and cause either a slight increase or no change in receptor affinity for antagonists. Amiloride analogs accelerate the rate of [3H] yohimbine dissociation from digitonin-solubilized receptors with a relative effectiveness that parallels their ability to block Na+/H+ exchange in other systems. Interestingly, these modulatory effects of Na+,H+ and 5-amino-substituted analogs of amiloride are retained in homogeneous preparations of the alpha 2-adrenergic receptor, suggesting that the allosteric-binding sites for these agents are on the receptor-binding protein itself.

Original languageEnglish (US)
Pages (from-to)12387-12392
Number of pages6
JournalJournal of Biological Chemistry
Volume262
Issue number25
StatePublished - Sep 5 1987
Externally publishedYes

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Adrenergic alpha-2 Receptors
Digitonin
Brain
Swine
Yohimbine
Amiloride
Idazoxan
Allosteric Site
Sodium-Hydrogen Antiporter
Platelets
Neuroblastoma
Glioma
Epinephrine
Norepinephrine
Carrier Proteins
Blood Platelets
Binding Sites
Ligands

ASJC Scopus subject areas

  • Biochemistry

Cite this

Nunnari, J. M., Repaske, M. G., Brandon, S., Cragoe, E. J., & Limbird, L. E. (1987). Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange. Journal of Biological Chemistry, 262(25), 12387-12392.

Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange. / Nunnari, J. M.; Repaske, M. G.; Brandon, S.; Cragoe, E. J.; Limbird, L. E.

In: Journal of Biological Chemistry, Vol. 262, No. 25, 05.09.1987, p. 12387-12392.

Research output: Contribution to journalArticle

Nunnari, JM, Repaske, MG, Brandon, S, Cragoe, EJ & Limbird, LE 1987, 'Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange.', Journal of Biological Chemistry, vol. 262, no. 25, pp. 12387-12392.
Nunnari JM, Repaske MG, Brandon S, Cragoe EJ, Limbird LE. Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange. Journal of Biological Chemistry. 1987 Sep 5;262(25):12387-12392.
Nunnari, J. M. ; Repaske, M. G. ; Brandon, S. ; Cragoe, E. J. ; Limbird, L. E. / Regulation of porcine brain alpha 2-adrenergic receptors by Na+,H+ and inhibitors of Na+/H+ exchange. In: Journal of Biological Chemistry. 1987 ; Vol. 262, No. 25. pp. 12387-12392.
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