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Title: Amiloride interacts with renal. cap alpha. - and. beta. -adrenergic receptors

Abstract

The authors have used radioligand binding techniques to assess whether amiloride and certain analogues of amiloride (ethylisopropyl amiloride and benzamil) can bind to adrenergic receptors in the kidney. They found that amiloride could compete for (/sup 3/H)rauwolscine (..cap alpha../sub 2/-adrenergic receptors), (/sup 3/H)prazosin (..cap alpha../sub 1/-adrenergic receptors), and (/sup 125/I)iodocyanopindolol (..beta..-adrenergic receptors) binding in rat renal cortical membranes with inhibitor constants of 13.6 /plus minus/ 5.7, 24.4 /plus minus/ 7.4, and 8.36 /plus minus/ 13.5 ..mu..M, respectively. Ethylisopropyl amiloride and benzamil were from 2- to 25-fold more potent than amiloride in competing for radioligand binding sites in studies with these membranes. In addition, amiloride and the two analogues competed for (/sup 3/H)prazosin sites on intact Madin-Darby canine kidney cells and amiloride blocked epinephrine-stimulated prostaglandin E/sub 2/ production in these cells. They conclude that amiloride competes for binding to several classes of renal adrenergic receptors with a rank order of potency of ..cap alpha../sub 2/ > ..cap alpha../sub 1/ > ..beta... Binding to, and antagonism of, adrenergic receptors occurs at concentrations of amiloride that are lower than previously observed nonspecific interactions of this agent.

Authors:
; ;
Publication Date:
Research Org.:
Univ. of California, La Jolla (USA)
OSTI Identifier:
6145790
Resource Type:
Journal Article
Journal Name:
Am. J. Physiol.; (United States)
Additional Journal Information:
Journal Volume: 253:1
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; DIURETICS; RADIORECEPTOR ASSAY; KIDNEYS; MEMBRANE TRANSPORT; SYMPATHOMIMETICS; RECEPTORS; DOSE-RESPONSE RELATIONSHIPS; LIGANDS; MEMBRANES; PROSTAGLANDINS; RATS; SOMATIC CELLS; TRITIUM COMPOUNDS; ANIMAL CELLS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BODY; DRUGS; ISOTOPE APPLICATIONS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; ORGANIC COMPOUNDS; ORGANS; PROTEINS; RODENTS; TRACER TECHNIQUES; VERTEBRATES; 551001* - Physiological Systems- Tracer Techniques

Citation Formats

Howard, M J, Mullen, M D, and Insel, P A. Amiloride interacts with renal. cap alpha. - and. beta. -adrenergic receptors. United States: N. p., 1987. Web.
Howard, M J, Mullen, M D, & Insel, P A. Amiloride interacts with renal. cap alpha. - and. beta. -adrenergic receptors. United States.
Howard, M J, Mullen, M D, and Insel, P A. 1987. "Amiloride interacts with renal. cap alpha. - and. beta. -adrenergic receptors". United States.
@article{osti_6145790,
title = {Amiloride interacts with renal. cap alpha. - and. beta. -adrenergic receptors},
author = {Howard, M J and Mullen, M D and Insel, P A},
abstractNote = {The authors have used radioligand binding techniques to assess whether amiloride and certain analogues of amiloride (ethylisopropyl amiloride and benzamil) can bind to adrenergic receptors in the kidney. They found that amiloride could compete for (/sup 3/H)rauwolscine (..cap alpha../sub 2/-adrenergic receptors), (/sup 3/H)prazosin (..cap alpha../sub 1/-adrenergic receptors), and (/sup 125/I)iodocyanopindolol (..beta..-adrenergic receptors) binding in rat renal cortical membranes with inhibitor constants of 13.6 /plus minus/ 5.7, 24.4 /plus minus/ 7.4, and 8.36 /plus minus/ 13.5 ..mu..M, respectively. Ethylisopropyl amiloride and benzamil were from 2- to 25-fold more potent than amiloride in competing for radioligand binding sites in studies with these membranes. In addition, amiloride and the two analogues competed for (/sup 3/H)prazosin sites on intact Madin-Darby canine kidney cells and amiloride blocked epinephrine-stimulated prostaglandin E/sub 2/ production in these cells. They conclude that amiloride competes for binding to several classes of renal adrenergic receptors with a rank order of potency of ..cap alpha../sub 2/ > ..cap alpha../sub 1/ > ..beta... Binding to, and antagonism of, adrenergic receptors occurs at concentrations of amiloride that are lower than previously observed nonspecific interactions of this agent.},
doi = {},
url = {https://www.osti.gov/biblio/6145790}, journal = {Am. J. Physiol.; (United States)},
number = ,
volume = 253:1,
place = {United States},
year = {Wed Jul 01 00:00:00 EDT 1987},
month = {Wed Jul 01 00:00:00 EDT 1987}
}