Literature DB >> 21238

Evidence from agonist and antagonist studies to suggest that the beta1-adrenoceptors subserving the positive inotropic and chronotropic responses of the heart do not belong to two separate subgroups.

P Lumley, K J Broadley.   

Abstract

The positive inotropic and chronotropic responses of guinea-pig isolated left and right atria to 17 sympathomimetic amines were examined under conditions selected to control the pharmacological environment. Each agonist was compared with (--)-isoprenaline as the reference by constructing dose-response curves. Equiactive molar concentration ratios relative to (--)-isoprenaline were calculated at the EC50 for rate and tension responses. Statistical analysis revealed that (--)-noradrenaline and (+/-)-alpha-methylnoradrenaline were tension selective whereas (+/-)-alpha-ethylisoprenaline and N-methyldopamine were rate selective relative to (--)-isoprenaline. However, no structural trends emerged. The rank order of potency varied slightly between rate and tension, but an analysis of the regression and correlation coefficients indicated respectively that the equiactive molar concentration ratios and the rank orders could be considered identical on rate and tension. Antagonism of the (--)-isoprenaline-induced rate and tension responses by acebutolol, atenolol, practolol and propranolol was assessed from the pA2 values which were almost identical for both parameters with each antagnosti. It is concluded that the beta1-adrenoceptors mediating the positive inotropic and chronotropic responses do not warrant subdivision into two separate groups.

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Year:  1977        PMID: 21238     DOI: 10.1111/j.2042-7158.1977.tb11413.x

Source DB:  PubMed          Journal:  J Pharm Pharmacol        ISSN: 0022-3573            Impact factor:   3.765


  9 in total

1.  Affinities of full agonists for cardiac beta-adrenoceptors calculated by use of in vitro desensitization.

Authors:  M L Herepath; K J Broadley
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-06       Impact factor: 3.000

2.  Relaxant effect of dopamine on the isolated rat uterus.

Authors:  L Estañ; I Martinez-Mir; E Rubio; F J Morales-Olivas
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1988-11       Impact factor: 3.000

3.  On equilibrium dissociation constants for complexes of drug-receptor subtypes. Selective and non-selective interactions of partial agonists with two plausible beta-adrenoceptor subtypes mediating positive chronotropic effects of (-)-isoprenaline in kitten atria.

Authors:  A J Kaumann; M Marano
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1982-02       Impact factor: 3.000

4.  Comparative assessment of beta-adrenoceptor blocking agents as simple competitive antagonists in isolated heart muscle: similarity of inotropic and chronotropic blocking potencies against isoproterenol.

Authors:  A J Kaumann; T K McInerny; D P Gilmour; J R Blinks
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1980-04       Impact factor: 3.000

5.  Estimation of dissociation constants and relative efficacies of isoprenaline, orciprenaline and terbutaline in guinea-pig isolated atria by use of functional antagonism [proceedings].

Authors:  K J Broadley; C D Nicholson
Journal:  Br J Pharmacol       Date:  1978-11       Impact factor: 8.739

6.  Dissociation constants of isoprenaline and orciprenaline and their relative efficacies on guinea-pig isolated atria determined by use of an irreversible beta-adrenoceptor antagonist.

Authors:  K J Broadley; C D Nicholson
Journal:  Br J Pharmacol       Date:  1981-04       Impact factor: 8.739

7.  Temperature-induced changes in dissociation constants (KA) of agonists at cardiac beta-adrenoceptors determined by use of the irreversible antagonist Ro 03-7894.

Authors:  K J Broadley; R G Williams
Journal:  Br J Pharmacol       Date:  1983-06       Impact factor: 8.739

8.  Functional antagonism as a means of determining dissociation constants and relative efficacies of sympathomimetic amines in guinea-pig isolated atria.

Authors:  K J Broadley; C D Nicholson
Journal:  Br J Pharmacol       Date:  1979-07       Impact factor: 8.739

9.  The affinity of (-)-propranolol for beta 1- and beta 2-adrenoceptors of human heart. Differential antagonism of the positive inotropic effects and adenylate cyclase stimulation by (-)-noradrenaline and (-)-adrenaline.

Authors:  E Gille; H Lemoine; B Ehle; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-10       Impact factor: 3.000

  9 in total

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