Literature DB >> 3754007

Comparison of muscarinic receptor properties in hatched chick heart atrium and ventricle.

S Sorota, L P Adam, A J Pappano.   

Abstract

We have reported previously that chick myocardium responds to muscarinic agonists with a decrease in slow inward current in both atrial and ventricular muscle. A second ionic current, the background potassium current, is increased in the atrium but not in the ventricle. A possible explanation for the modulation of potassium current in atrium only is the existence of a unique muscarinic receptor population in atrium responsible for potassium conductance changes. We looked for differences in atrial and ventricular muscarinic receptors by pharmacological and biochemical techniques. The dissociation constants for binding of l-[3H]quinuclidinyl benzilate were 46 pM in both tissues. Estimates for binding of atropine in competitive binding experiments gave dissociation constants of 1.8 nM in atrium and 2.0 nM in ventricle. Pharmacologic evaluation of atropine occupancy of muscarinic receptor by Schild analysis showed no difference in the dissociation constants in atrium (1.7 nM) and ventricle (1.1 nM). Displacement of 0.1 nM [3H]quinuclidinyl benzilate with carbachol showed the atrium to have a higher apparent affinity for agonist than the ventricle (atrium IC50 = 8.2 X 10(-6) M, ventricle IC50 = 2.1 X 10(-5) M). Computerized curve fitting analysis detected three binding states (super high, high and low affinity) for carbachol in the atrium and ventricle in the absence and presence of 5'-guanylylimidodiphosphate (10(-4) M). We did not detect a qualitative difference between atrial and ventricular muscarinic receptors. Muscarinic-induced potassium conductance changes which occur in the atria do not appear to be due to a unique muscarinic receptor in atria.

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Year:  1986        PMID: 3754007

Source DB:  PubMed          Journal:  J Pharmacol Exp Ther        ISSN: 0022-3565            Impact factor:   4.030


  8 in total

Review 1.  Functional M3 muscarinic acetylcholine receptors in mammalian hearts.

Authors:  Zhiguo Wang; Hong Shi; Huizhen Wang
Journal:  Br J Pharmacol       Date:  2004-05-17       Impact factor: 8.739

2.  Radioligand binding characteristics of the chicken cardiac muscarinic receptor.

Authors:  A D Michel; R L Whiting
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1989-09       Impact factor: 3.000

3.  Muscarinic cholinoceptors in the human heart: demonstration, subclassification, and distribution.

Authors:  N M Deighton; S Motomura; D Borquez; H R Zerkowski; N Doetsch; O E Brodde
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990 Jan-Feb       Impact factor: 3.000

4.  Antagonism of novel inotropic agents at A1 adenosine receptors and m-cholinoceptors in human myocardium.

Authors:  M Ungerer; M Böhm; R H Schwinger; E Erdmann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-06       Impact factor: 3.000

5.  Cardiac muscarinic receptors decrease with age. In vitro and in vivo studies.

Authors:  O E Brodde; U Konschak; K Becker; F Rüter; U Poller; J Jakubetz; J Radke; H R Zerkowski
Journal:  J Clin Invest       Date:  1998-01-15       Impact factor: 14.808

6.  The M2 selective antagonist AF-DX 116 shows high affinity for muscarine receptors in bovine tracheal membranes.

Authors:  A F Roffel; W G in't Hout; R A de Zeeuw; J Zaagsma
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-05       Impact factor: 3.000

7.  Two populations of muscarinic binding sites in the chick heart distinguished by affinities for ligands and selective inactivation.

Authors:  J Jakubík; S Tucek
Journal:  Br J Pharmacol       Date:  1994-12       Impact factor: 8.739

8.  Characterization of the acetylcholine-sensitive muscarinic K+ channel in isolated feline atrial and ventricular myocytes.

Authors:  S Koumi; R Sato; H Hayakawa
Journal:  J Membr Biol       Date:  1995-05       Impact factor: 1.843

  8 in total

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