Characterization of [ 3H]U69593 binding sites in the rat heart by receptor binding assays

The binding properties of [ 3H]U69593, a selective k-ligand, in rat heart homogenates were characterized by direct and displacement receptor binding assays. It was found that there are substantial specific [ 3H]UU69593 binding sites in the rat heart. They were saturable, reversible and stereospecifi...

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Veröffentlicht in:Journal of molecular and cellular cardiology 1991-11, Vol.23 (11), p.1297-1302
Hauptverfasser: Tai, K.K., Jin, W-Q., Chan, T.K.Y., Wong, T.M.
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container_end_page 1302
container_issue 11
container_start_page 1297
container_title Journal of molecular and cellular cardiology
container_volume 23
creator Tai, K.K.
Jin, W-Q.
Chan, T.K.Y.
Wong, T.M.
description The binding properties of [ 3H]U69593, a selective k-ligand, in rat heart homogenates were characterized by direct and displacement receptor binding assays. It was found that there are substantial specific [ 3H]UU69593 binding sites in the rat heart. They were saturable, reversible and stereospecific. Both association and dissociation rates were monophasic and the Scatchard plot was linear, indicating a homogeneity of binding sites. The Hill coefficient was close ti 1, indicating an absence of cooperativity. The B max and K d were 7.91 fmol/mg and 2.92 n m, respectively. The binding sites were most abundant in the right atrium, followed by right ventricle, left ventricle and left atrium in descending order. The study provides information on the properties and distribution of k-binding sites in the rat heart.
doi_str_mv 10.1016/0022-2828(91)90086-2
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ispartof Journal of molecular and cellular cardiology, 1991-11, Vol.23 (11), p.1297-1302
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source Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE
subjects Analgesics - metabolism
Animals
Benzeneacetamides
Binding Sites
Biological and medical sciences
Cell receptors
Cell structures and functions
Female
Fundamental and applied biological sciences. Psychology
k-binding sites
Kinetics
Molecular and cellular biology
Myocardium - metabolism
Neuropeptide receptors
Pyrrolidines - metabolism
Radioligand Assay
Rat heart
Rats
Rats, Inbred Strains
Receptor binding
U-69593
U50,448H
title Characterization of [ 3H]U69593 binding sites in the rat heart by receptor binding assays
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