Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes
The aim of this study was to characterize [3H]CGP 12177 (CGP) binding to β-adrenergic receptors in isolated hepatocytes of the European eel (Anguilla anguilla), in which the involvement of cAMP in epinephrine-induced glucose release has been previously observed. Specific binding of CGP was saturable...
Published in: | General and Comparative Endocrinology |
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2001
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Online Access: | http://hdl.handle.net/11392/1199604 https://doi.org/10.1006/gcen.2000.7591 |
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ftunivferrarair:oai:sfera.unife.it:11392/1199604 2024-09-09T19:00:41+00:00 Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes E. FABBRI C. SELVA T. W. MOON CAPUZZO, Antonio E., Fabbri C., Selva T. W., Moon Capuzzo, Antonio 2001 STAMPA http://hdl.handle.net/11392/1199604 https://doi.org/10.1006/gcen.2000.7591 eng eng info:eu-repo/semantics/altIdentifier/wos/WOS:000167821000001 volume:121 issue:3 firstpage:223 lastpage:231 journal:GENERAL AND COMPARATIVE ENDOCRINOLOGY http://hdl.handle.net/11392/1199604 doi:10.1006/gcen.2000.7591 info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-0034744947 Adrenergic receptor binding cAMP CGP 12177 Epinephrine European eel Glucose release info:eu-repo/semantics/article 2001 ftunivferrarair https://doi.org/10.1006/gcen.2000.7591 2024-06-19T13:33:12Z The aim of this study was to characterize [3H]CGP 12177 (CGP) binding to β-adrenergic receptors in isolated hepatocytes of the European eel (Anguilla anguilla), in which the involvement of cAMP in epinephrine-induced glucose release has been previously observed. Specific binding of CGP was saturable, reversible, and linear as a function of cell number. Analysis of binding data suggested a single class of binding sites, with a Kd of 1.31 nM and a number of approximately 7000 β-adrenergic receptors per cell. The potency order of specific inhibition of [3H]CGP binding was CGP > propranolol ≥ alprenolol ≫ butoxamine ≥ atenolol, while phentolamine and prazosin failed to significantly displace the tracer at concentrations up to 100 μM. The binding kinetics of CGP were closely related to its biological effect. In fact, the drug dose-dependently counteracted the enhancement of intracellular cAMP levels induced by epinephrine in isolated hepatocytes with a Kd of 1.06 nM. Moreover, it antagonized the hormone-induced stimulation of adenylyl cyclase activity in hepatic membranes as well as of glucose release from cells. These data clearly show that β-adrenergic receptors are coupled to the adenylyl cyclase/cAMP transduction pathway in eel liver. © 2001 Academic Press. Article in Journal/Newspaper Anguilla anguilla Università degli Studi di Ferrara: CINECA IRIS General and Comparative Endocrinology 121 3 223 231 |
institution |
Open Polar |
collection |
Università degli Studi di Ferrara: CINECA IRIS |
op_collection_id |
ftunivferrarair |
language |
English |
topic |
Adrenergic receptor binding cAMP CGP 12177 Epinephrine European eel Glucose release |
spellingShingle |
Adrenergic receptor binding cAMP CGP 12177 Epinephrine European eel Glucose release E. FABBRI C. SELVA T. W. MOON CAPUZZO, Antonio Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
topic_facet |
Adrenergic receptor binding cAMP CGP 12177 Epinephrine European eel Glucose release |
description |
The aim of this study was to characterize [3H]CGP 12177 (CGP) binding to β-adrenergic receptors in isolated hepatocytes of the European eel (Anguilla anguilla), in which the involvement of cAMP in epinephrine-induced glucose release has been previously observed. Specific binding of CGP was saturable, reversible, and linear as a function of cell number. Analysis of binding data suggested a single class of binding sites, with a Kd of 1.31 nM and a number of approximately 7000 β-adrenergic receptors per cell. The potency order of specific inhibition of [3H]CGP binding was CGP > propranolol ≥ alprenolol ≫ butoxamine ≥ atenolol, while phentolamine and prazosin failed to significantly displace the tracer at concentrations up to 100 μM. The binding kinetics of CGP were closely related to its biological effect. In fact, the drug dose-dependently counteracted the enhancement of intracellular cAMP levels induced by epinephrine in isolated hepatocytes with a Kd of 1.06 nM. Moreover, it antagonized the hormone-induced stimulation of adenylyl cyclase activity in hepatic membranes as well as of glucose release from cells. These data clearly show that β-adrenergic receptors are coupled to the adenylyl cyclase/cAMP transduction pathway in eel liver. © 2001 Academic Press. |
author2 |
E., Fabbri C., Selva T. W., Moon Capuzzo, Antonio |
format |
Article in Journal/Newspaper |
author |
E. FABBRI C. SELVA T. W. MOON CAPUZZO, Antonio |
author_facet |
E. FABBRI C. SELVA T. W. MOON CAPUZZO, Antonio |
author_sort |
E. FABBRI |
title |
Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
title_short |
Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
title_full |
Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
title_fullStr |
Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
title_full_unstemmed |
Characterization of [3H]CGP 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
title_sort |
characterization of [3h]cgp 12177 binding to beta-adrenergic receptors in intact eel hepatocytes |
publishDate |
2001 |
url |
http://hdl.handle.net/11392/1199604 https://doi.org/10.1006/gcen.2000.7591 |
genre |
Anguilla anguilla |
genre_facet |
Anguilla anguilla |
op_relation |
info:eu-repo/semantics/altIdentifier/wos/WOS:000167821000001 volume:121 issue:3 firstpage:223 lastpage:231 journal:GENERAL AND COMPARATIVE ENDOCRINOLOGY http://hdl.handle.net/11392/1199604 doi:10.1006/gcen.2000.7591 info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-0034744947 |
op_doi |
https://doi.org/10.1006/gcen.2000.7591 |
container_title |
General and Comparative Endocrinology |
container_volume |
121 |
container_issue |
3 |
container_start_page |
223 |
op_container_end_page |
231 |
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1809941228978962432 |