PMID: 8751073Nov 1, 1995Paper

Regional differences in the density and subtype specificity of endothelin receptors in rabbit urinary tract

Naunyn-Schmiedeberg's Archives of Pharmacology
J LatifpourR M Weiss

Abstract

We investigated the binding characteristics of endothelin (ET) receptors in rabbit ureter, bladder dome, bladder base, and urethra and compared the observed receptor properties with those of cloned human ETA and ETB receptors expressed in Chinese hamster ovary K-1 (CHO) cells. Receptor binding experiments with [125I]ET-1 revealed the presence of a single class of specific, saturable, high affinity [125I]ET-1 binding sites in all of the regions of the studied urinary tract. The rank order of the densities (Bmax values) of [125I]ET-1 binding sites was: ureter "bladder dome > bladder base = urethra. ET-1 and ET-2 inhibited [125I]ET-1 binding to the membrane particulates from the various regions of the urinary tract with single high affinity constants. A selective ETA receptor antagonist, BQ 123, and selective ETB agonists, ET-3 and sarafotoxin S6c (STXc), inhibited [125I]ET-1 binding to bladder dome, bladder base, and urethra with high and low affinity constants indicating the presence of both ETA and ETB receptor subtypes in these tissues. The subtype specificity of ET receptors in the rabbit tissues is confirmed with inhibition data obtained from similar binding studies in cloned human ETA and ETB receptors. The proportions of h...Continue Reading

Citations

Jun 1, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Masashi UkaiMasao Sasamata
Aug 29, 1996·European Journal of Pharmacology·M SaitoJ Latifpour
Aug 24, 1999·British Journal of Pharmacology·W A LauF J Mitchelson
Mar 27, 2001·Annual Review of Pharmacology and Toxicology·W C de Groat, N Yoshimura
Dec 22, 1999·Neurourology and Urodynamics·M SaitoR M Weiss
Jul 23, 2004·Physiological Reviews·Karl-Erik Andersson, Anders Arner
Jul 25, 2000·BJU International·M E SullivanR J Morgan
Dec 22, 1999·Endothelium : Journal of Endothelial Cell Research·F H MumtazM R Dashwood
Oct 10, 2008·Reproduction, Fertility, and Development·Yoshihiro WadaTakahisa Imamura
Oct 15, 2011·Physiological Research·S M JankovicS Stefanovic

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