beta 1-Adrenergic receptors in kidney tubular cell membrane in the rat

We used a beta-adrenergic antagonist, (-) 3H-dihydroalprenolol, to demonstrate binding sites in purified rat kidney preparations that consistsed of plasma membranes of cells from tubules. The tubular origin of these plasma membranes was shown by electron microscopy and Na-K-ATPase enrichment. The bi...

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Veröffentlicht in:Kidney international 1980-06, Vol.17 (6), p.764-770
Hauptverfasser: Gavendo, S, Kapuler, S, Serban, I, Iaina, A, Ben-David, E, Eliahou, H
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container_end_page 770
container_issue 6
container_start_page 764
container_title Kidney international
container_volume 17
creator Gavendo, S
Kapuler, S
Serban, I
Iaina, A
Ben-David, E
Eliahou, H
description We used a beta-adrenergic antagonist, (-) 3H-dihydroalprenolol, to demonstrate binding sites in purified rat kidney preparations that consistsed of plasma membranes of cells from tubules. The tubular origin of these plasma membranes was shown by electron microscopy and Na-K-ATPase enrichment. The binding was rapid (t1/2, 78 sec) and rapidly reversible (t1/2, 48 sec). The binding sites were saturable and bound 69.8 +/- (SD) 29.1 fmoles/mg of membrane protein. The binding was stereospecific with the isomers of beta-adrenergic agonists and beta-adrenergic antagonist propranolol, the (-) isomers being about 40 times more potent than the (+) isomers incompeting for these sites. (-) 3H-dihydroalprenolol had a high affinity for the binding sites, expressed by the mean equilibrium dissociation constant (KD) (KD, 7.1 nM). The beta-adrenergic antagonist (-) propranolol also showed high affinity (KD, 62.8 nM). The order of potency for inhibition of binding by beta-adrenergic agonists was: (-) isoproterenol (KD, 0.66 microM) greater than (-) epinephrine (KD, 4.3 microM) greater than or equal to (-) norepinephrine (KD, 13.5 microM). Conclusion. The (-) 3H-dihydroalprenolol binding sites in the rat kidney tubular cell membrane are beta-adrenergic receptor of the beta1 subgroup.
doi_str_mv 10.1038/ki.1980.89
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The (-) 3H-dihydroalprenolol binding sites in the rat kidney tubular cell membrane are beta-adrenergic receptor of the beta1 subgroup.</abstract><cop>United States</cop><pmid>6251307</pmid><doi>10.1038/ki.1980.89</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record>
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source MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Alma/SFX Local Collection
subjects Alprenolol - analogs & derivatives
Animals
Cell Membrane - metabolism
Depression, Chemical
Dihydroalprenolol - antagonists & inhibitors
Dihydroalprenolol - metabolism
Epinephrine - pharmacology
Isoproterenol - pharmacology
Kidney Tubules - ultrastructure
Kinetics
Norepinephrine - pharmacology
Rats
Receptors, Adrenergic - metabolism
Receptors, Adrenergic, beta - metabolism
title beta 1-Adrenergic receptors in kidney tubular cell membrane in the rat
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