Literature DB >> 8298805

Blockade of human atrial 5-HT4 receptors by GR 113808.

A J Kaumann1.   

Abstract

1. The mode of antagonism of 5-hydroxytryptamine (5-HT)-induced positive inotropic effects by the highly selective 5-HT4 receptor antagonist GR 113808 ([1-[2-methylsulphonylamino ethyl]-4-piperidinyl]methyl 1-methyl-1H-indole-3-carboxylate) was investigated on isolated preparations of human right atrium. 2. GR 113808 caused concentration-dependent (2-100 nM) surmountable antagonism of the effects of 5-HT with a pKB (M) of 8.8. 3. The affinity of GR 113808 for human atrial 5-HT4 receptors, together with its high selectivity for 5-HT4 receptors comprise useful properties for investigating the question of 5-HT4 receptor subtypes.

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Year:  1993        PMID： 8298805      PMCID： PMC2175795          DOI： 10.1111/j.1476-5381.1993.tb13937.x

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


  7 in total

Review 1.  The 5-HT4 receptor: a place in the sun.

Authors:  J Bockaert; J R Fozard; A Dumuis; D E Clarke
Journal:  Trends Pharmacol Sci       Date:  1992-04       Impact factor: 14.819

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.  Some quantitative uses of drug antagonists.

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

4.  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

5.  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

6.  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

7.  Chloride anion concentration as a determinant of renal vascular responsiveness to vasoconstrictor agents.

Authors:  C P Quilley; Y S Lin; J C McGiff
Journal:  Br J Pharmacol       Date:  1993-01       Impact factor: 8.739
  7 in total
  23 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.  Involvement of 5-HT1B receptors in collar-induced hypersensitivity to 5-hydroxytryptamine of the rabbit carotid artery.

Authors:  I S Geerts; K E Matthys; A G Herman; H Bult
Journal:  Br J Pharmacol       Date:  1999-07       Impact factor: 8.739

3.  A comparative study of functional 5-HT4 receptors in human colon, rat oesophagus and rat ileum.

Authors:  P G McLean; I M Coupar; P Molenaar
Journal:  Br J Pharmacol       Date:  1995-05       Impact factor: 8.739

4.  5-HT3 and 5-HT4 receptor-mediated facilitation of the emptying phase of the peristaltic reflex in the marmoset isolated ileum.

Authors:  B R Tuladhar; B Costall; R J Naylor
Journal:  Br J Pharmacol       Date:  1996-04       Impact factor: 8.739

5.  Stimulation of cyclic AMP formation in the circular smooth muscle of human colon by activation of 5-HT4-like receptors.

Authors:  P G McLean; I M Coupar
Journal:  Br J Pharmacol       Date:  1996-01       Impact factor: 8.739

6.  Prucalopride is a partial agonist through human and porcine atrial 5-HT4 receptors: comparison with recombinant human 5-HT4 splice variants.

Authors:  Kurt A Krobert; Trond Brattelid; Finn Olav Levy; Alberto J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2005-07-13       Impact factor: 3.000

7.  Pharmacological characterization of the 5-hydroxytryptamine receptor mediating relaxation in the rat isolated ileum.

Authors:  B R Tuladhar; B Costall; R J Naylor
Journal:  Br J Pharmacol       Date:  1996-09       Impact factor: 8.739

8.  Differences in response to 5-HT4 receptor agonists and antagonists of the 5-HT4-like receptor in human colon circular smooth muscle.

Authors:  F S Tam; K Hillier; K T Bunce; C Grossman
Journal:  Br J Pharmacol       Date:  1995-05       Impact factor: 8.739

9.  Functional 5-HT receptors in human occipital artery.

Authors:  Raphaela Verheggen; Andreas Meier; Inga Werner; Andreas Wienekamp; Thomas Kruschat; Trond Brattelid; Finn Olav Levy; Alberto Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2004-03-06       Impact factor: 3.000

Review 10.  Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications.

Authors:  Carlos M Villalón; David Centurión
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2007-08-17       Impact factor: 3.000
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