PMID: 8958583Dec 3, 1996Paper

Characterization of the binding properties and physiological action of divalinal-angiotensin IV, a putative AT4 receptor antagonist

Regulatory Peptides
L T KrebsJ W Harding

Abstract

Divalinal-Ang IV [V psi (CH2-NH2)YV psi (CH2-NH2)HPF] is being employed increasingly as a specific AT4 antagonist. This use, which necessitates a comprehensive physiological and pharmacological evaluation of Divalinal-Ang IV's functional and receptor binding characteristics in order to ensure its efficacy and specificity, was the stimulus for this study using bovine adrenal membranes. [125I]Ang IV and [125I]Divalinal-Ang IV were shown to bind with high affinity to a similar number of binding sites, suggesting that both bound the same receptor. This notion was verified by competition curves using [125I]Ang IV and [125I]Divalinal-Ang IV that indicated identical rank order affinities for several angiotensin-related peptides and 100% cross-displacement by Ang IV and Divalinal-Ang IV. Furthermore, an autoradiographic comparison of [125I]Ang IV and [125I]Divalinal-Ang IV in 20 microns sections of bovine adrenals revealed near identical binding distributions characterized by heavy binding in the glomerulosa layer and the medulla. Physiological studies in which test compounds were injected into the internal carotid of the rat and cerebral blood flor (CBF) was measured by laser Doppler flowmetry indicated that pretreatment with Divalina...Continue Reading

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Citations

Nov 26, 1999·Journal of Cellular Biochemistry·S I BriandG Guillemette
Nov 25, 1997·Brain Research. Brain Research Reviews·J W Wright, J W Harding
Aug 26, 1998·Regulatory Peptides·E A KramárJ W Wright
Jan 14, 1999·Brain Research Bulletin·O von Bohlen und Halbach, D Albrecht
Feb 20, 2003·Trends in Endocrinology and Metabolism : TEM·Anthony L AlbistonSiew Yeen Chai
Oct 12, 2012·The Journal of Pharmacology and Experimental Therapeutics·Alene T McCoyJoseph W Harding
Jun 5, 2008·Biochemistry and Cell Biology = Biochimie Et Biologie Cellulaire·Siying YeAnthony L Albiston
Oct 27, 2010·Hypertension·Elena Y SenchenkovaD Neil Granger
May 16, 2000·Life Sciences·L M Tan, M K Sim
Jul 23, 2011·Progress in Neurobiology·John W Wright, Joseph W Harding
Mar 5, 2011·European Journal of Pharmacology·Qiang Wen, Meng-Kwoon Sim
Aug 1, 2009·Molecular and Cellular Endocrinology·Heidi DemaegdtGeorges Vauquelin
Dec 17, 2008·Molecular and Cellular Endocrinology·Patrick M L Vanderheyden
Jul 23, 2003·Journal of Neurochemistry·Rebecca A LewAnthony L Albiston
Dec 2, 2008·CNS Neuroscience & Therapeutics·Dimitri De BundelYvette Michotte
Apr 12, 2011·Fundamental & Clinical Pharmacology·Heidi DemaegdtGeorges Vauquelin
Feb 19, 2013·Neuropharmacology·Jason J ParisJay P McLaughlin
Jan 11, 2013·International Journal of Hypertension·Hanna Andersson, Mathias Hallberg
Dec 3, 2014·Progress in Neurobiology·John W WrightJoseph W Harding
Mar 14, 2007·Regulatory Peptides·Patrícia Maria FerreiraMaria José Campagnole-Santos
Sep 24, 2004·The Anatomical Record. Part A, Discoveries in Molecular, Cellular, and Evolutionary Biology·Gilbert A BurnsJoseph W Harding
Sep 13, 2006·Journal of Peptide Science : an Official Publication of the European Peptide Society·Andreas AxénMathias Hallberg
Jun 15, 2007·Journal of Peptide Science : an Official Publication of the European Peptide Society·Andreas AxénMathias Hallberg
Jun 1, 2007·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Daniela GrigoreBarbara T Alexander
Jun 16, 1999·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·G P VinsonO Djahanbakhch
Jan 16, 2015·American Journal of Physiology. Regulatory, Integrative and Comparative Physiology·Regina NostramoEsther L Sabban
Mar 5, 1998·The American Journal of Physiology·R K HandaS E Handa
Nov 22, 2000·American Journal of Physiology. Heart and Circulatory Physiology·S Ito, A F Sved

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