Literature DB >> 7582523

Labelling with [125I]-SB 207710 of a small 5-HT4 receptor population in piglet right atrium: functional relevance.

A J Kaumann1, J A Lynham, A M Brown.   

Abstract

1. We investigated the affinity of SB 207710 for sinoatrial 5-HT4 receptors and the density of right atrial 5-HT4 receptors with [125I]-SB 207710 in right atria of new-born piglets. 2. SB 207710 (1-100 nM) antagonized the 5-HT-evoked tachycardia surmountably with a pKB of 9.8. 3. [125I]-SB 207710 (5-1500 pM) labelled a small population of saturable binding sites with a pKD of 10.1 and with 5-HT4 receptor characteristics. The density of atrial binding sites with 5-HT4 receptor characteristics was 174 and 22 times lower respectively than those of atrial beta 1- and beta 2-adrenoceptors, labelled with (-)-[125I]-cyanopindolol. 4. We suggest that the small 5-HT4 receptor population may in part explain why the maximal tachycardia caused by 5-HT is smaller than that caused by catecholamines.

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Year:  1995        PMID： 7582523      PMCID： PMC1909015          DOI： 10.1111/j.1476-5381.1995.tb15900.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  12 in total

1.  Piglet sinoatrial 5-HT receptors resemble human atrial 5-HT4-like receptors.

Authors:  A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-11       Impact factor: 3.000

2.  Further characterization, by use of tryptamine and benzamide derivatives, of the putative 5-HT4 receptor mediating tachycardia in the pig.

Authors:  C M Villalón; M O den Boer; J P Heiligers; P R Saxena
Journal:  Br J Pharmacol       Date:  1991-01       Impact factor: 8.739

3.  The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons.

Authors:  A Dumuis; M Sebben; J Bockaert
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-10       Impact factor: 3.000

4.  Some quantitative uses of drug antagonists.

Authors:  O ARUNLAKSHANA; H O SCHILD
Journal:  Br J Pharmacol Chemother       Date:  1959-03

5.  Identification and characterization of serotonin 5-HT4 receptor binding sites in human brain: comparison with other mammalian species.

Authors:  T Doménech; J Beleta; A G Fernández; R W Gristwood; F Cruz Sánchez; E Tolosa; J M Palacios
Journal:  Brain Res Mol Brain Res       Date:  1994-01

6.  A 5-HT4-like receptor in human right atrium.

Authors:  A J Kaumann; L Sanders; A M Brown; K J Murray; M J Brown
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1991-08       Impact factor: 3.000

7.  Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.

Authors:  C J Grossman; G J Kilpatrick; K T Bunce
Journal:  Br J Pharmacol       Date:  1993-07       Impact factor: 8.739

8.  Beta 2-adrenoceptor-mediated positive inotropic effect of adrenaline in human ventricular myocardium. Quantitative discrepancies with binding and adenylate cyclase stimulation.

Authors:  A J Kaumann; H Lemoine
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-04       Impact factor: 3.000

9.  Blockade of human atrial 5-HT4 receptors by SB 207710, a selective and high affinity 5-HT4 receptor antagonist.

Authors:  A J Kaumann; L M Gaster; F D King; A M Brown
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-05       Impact factor: 3.000

Review 10.  Do human atrial 5-HT4 receptors mediate arrhythmias?

Authors:  A J Kaumann
Journal:  Trends Pharmacol Sci       Date:  1994-12       Impact factor: 14.819
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  12 in total

1.  Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.

Authors:  J Mialet; I Berque-Bestel; P Eftekhari; M Gastineau; M Giner; Y Dahmoune; P Donzeau-Gouge; J Hoebeke; M Langlois; S Sicsic; R Fischmeister; F Lezoualc'h
Journal:  Br J Pharmacol       Date:  2000-02       Impact factor: 8.739

2.  Fading of 5-HT4 receptor-mediated inotropic responses to 5-hydroxytryptamine is caused by phosphodiesterase activity in porcine atrium.

Authors:  Alberto J Kaumann; Finn Olav Levy
Journal:  Br J Pharmacol       Date:  2006-01       Impact factor: 8.739

3.  Selective desensitization of the 5-HT4 receptor-mediated response in pig atrium but not in stomach.

Authors:  J H De Maeyer; J A J Schuurkes; R A Lefebvre
Journal:  Br J Pharmacol       Date:  2009-01-13       Impact factor: 8.739

4.  Comparison of the densities of 5-HT4 receptors, beta 1- and beta 2-adrenoceptors in human atrium: functional implications.

Authors:  A J Kaumann; J A Lynham; A M Brown
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1996-04       Impact factor: 3.000

5.  Porcine left atrial and sinoatrial 5-HT(4) receptor-induced responses: fading of the response and influence of development.

Authors:  Joris H De Maeyer; Roel Straetemans; Jan A J Schuurkes; Romain A Lefebvre
Journal:  Br J Pharmacol       Date:  2006-01       Impact factor: 8.739

6.  Blockade of human and porcine myocardial 5-HT4 receptors by SB 203186.

Authors:  S G Parker; E M Taylor; S A Hamburger; M Vimal; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1995-12       Impact factor: 3.000

7.  Autoradiographic distribution of serotonin transporters and receptor subtypes in human brain.

Authors:  Katarina Varnäs; Christer Halldin; Håkan Hall
Journal:  Hum Brain Mapp       Date:  2004-07       Impact factor: 5.038

8.  Surprises from a cardiac 5-HT₄TG mouse: spontaneous atrial arrhythmias by endogenous 5-HT of atrial origin? Different mechanism of arrhythmias through 5-HT₄ receptors and β-adrenoceptors?

Authors:  Alberto J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2013-05       Impact factor: 3.000

9.  Functional serotonin 5-HT4 receptors in porcine and human ventricular myocardium with increased 5-HT4 mRNA in heart failure.

Authors:  Trond Brattelid; Eirik Qvigstad; James A Lynham; Peter Molenaar; Halfdan Aass; Odd Geiran; Tor Skomedal; Jan-Bjørn Osnes; Finn Olav Levy; Alberto J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2004-09-07       Impact factor: 3.000

10.  Ontogenic changes of the control by phosphodiesterase-3 and -4 of 5-HT responses in porcine heart and relevance to human atrial 5-HT(4) receptors.

Authors:  Alejandro Galindo-Tovar; Maria Luisa Vargas; Elisa Escudero; Alberto J Kaumann
Journal:  Br J Pharmacol       Date:  2009-01-19       Impact factor: 8.739
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