Literature DB >> 7915008

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

A J Kaumann1, L M Gaster, F D King, A M Brown.   

Abstract

The mode of antagonism of 5-hydroxytryptamine-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist SB 207710 (1-butyl-4-piperidinyl) methyl 8-amino-7-iodo-1,4-benzodioxan-5-carboxylate) was investigated on isolated preparations of human right atrial appendage. SB 207710 caused concentration-dependent (0.1-10 nmol/l) surmountable antagonism of the effects of 5-hydroxytryptamine with a pKB (mol/l) of 10.1. Due to its high selectivity and affinity, SB 207710 could be a powerful tool for the comparison of human atrial 5-HT4 receptors with 5-HT4 receptors of other organs of man and other species.

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Year:  1994        PMID： 7915008     DOI： 10.1007/bf00169146

Source DB:  PubMed          Journal:  Naunyn Schmiedebergs Arch Pharmacol        ISSN： 0028-1298            Impact factor:   3.000


  10 in total

1.  CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors.

Authors:  D J Dooley; H Bittiger; N C Reymann
Journal:  Eur J Pharmacol       Date:  1986-10-14       Impact factor: 4.432

2.  A 5-hydroxytryptamine receptor in human atrium.

Authors:  A J Kaumann; L Sanders; A M Brown; K J Murray; M J Brown
Journal:  Br J Pharmacol       Date:  1990-08       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.  Blockade of human atrial 5-HT4 receptors by GR 113808.

Authors:  A J Kaumann
Journal:  Br J Pharmacol       Date:  1993-11       Impact factor: 8.739

5.  Some quantitative uses of drug antagonists.

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

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.  Comparison of the positive inotropic effects of serotonin, histamine, angiotensin II, endothelin and isoprenaline in the isolated human right atrium.

Authors:  H R Zerkowski; A Broede; K Kunde; S Hillemann; E Schäfer; M Vogelsang; M C Michel; O E Brodde
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-04       Impact factor: 3.000

10.  The beta 1-adrenoceptor antagonist CGP 20712 A unmasks beta 2-adrenoceptors activated by (-)-adrenaline in rat sinoatrial node.

Authors:  A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-04       Impact factor: 3.000
  10 in total
  13 in total

1.  An improved in vitro bioassay for the study of 5-HT(4) receptors in the human isolated large intestinal circular muscle.

Authors:  N H Prins; N P Shankley; N J Welsh; M R Briejer; R A Lefebvre; L M Akkermans; J A Schuurkes
Journal:  Br J Pharmacol       Date:  2000-04       Impact factor: 8.739

2.  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

3.  Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.

Authors:  Rong Xu; Jinsoo Hong; Cheryl L Morse; Victor W Pike
Journal:  J Med Chem       Date:  2010-10-14       Impact factor: 7.446

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

Authors:  A J Kaumann; J A Lynham; A M Brown
Journal:  Br J Pharmacol       Date:  1995-07       Impact factor: 8.739

5.  5-HT4 receptor antagonist affinities of SB207710, SB205008, and SB203186 in the human colon, rat oesophagus, and guinea-pig ileum peristaltic reflex.

Authors:  P G McLean; I M Coupar
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1995-08       Impact factor: 3.000

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.  Evaluation in monkey of two candidate PET radioligands, [11 C]RX-1 and [18 F]RX-2, for imaging brain 5-HT4 receptors.

Authors:  Talakad G Lohith; Rong Xu; Tetsuya Tsujikawa; Cheryl L Morse; Kacey B Anderson; Robert L Gladding; Sami S Zoghbi; Masahiro Fujita; Robert B Innis; Victor W Pike
Journal:  Synapse       Date:  2014-08-11       Impact factor: 2.562

8.  Radioiodinated SB 207710 as a radioligand in vivo: imaging of brain 5-HT4 receptors with SPET.

Authors:  Victor W Pike; Christer Halldin; Kenji Nobuhara; Julka Hiltunen; Rachel S Mulligan; Carl-Gunnar Swahn; Per Karlsson; Hans Olsson; Susan P Hume; Ella Hirani; Jaqueline Whalley; Lyn S Pilowsky; Stig Larsson; Per-Olof Schnell; Peter J Ell; Lars Farde
Journal:  Eur J Nucl Med Mol Imaging       Date:  2003-09-23       Impact factor: 9.236

9.  Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers.

Authors:  Emmanuelle Dubost; Noé Dumas; Christine Fossey; Rosa Magnelli; Sabrina Butt-Gueulle; Céline Ballandonne; Daniel H Caignard; Fabienne Dulin; Jana Sopkova de-Oliveira Santos; Philippe Millet; Yves Charnay; Sylvain Rault; Thomas Cailly; Frederic Fabis
Journal:  J Med Chem       Date:  2012-11-09       Impact factor: 7.446

10.  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
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