Literature DB >> 6130188

Comparison of guinea pig uterine and rat vas deferens preparations for assessment of beta 2-adrenoceptor-mediated activity.

E Krstew, E Malta, C Raper.   

Abstract

In the present study, investigations were performed to determine the subtype(s) of beta-receptor-mediating relaxation in K+-depolarized guinea pig uterine preparations, and inhibition of twitches in field-stimulated rat vas deferens preparations. The relative activities of (-)-isoprenaline, salbutamol, terbutaline, noradrenaline, and RO363, and the affinity constants determined for the beta 1-receptor antagonist atenolol, and the beta 2-receptor antagonist lCl 118551, indicated that all the inhibitory responses in both preparations were mediated solely through beta 2-adrenoceptor stimulation. In the uterine preparations there was a small population of alpha-receptors which were of little consequence when assessing beta 2-receptor-mediated activity. During K+-induced contractures, both neuronal and extraneuronal uptake systems were inactivated. In rat vas deferens preparations, it was necessary to pretreat the tissues with phenoxybenzamine in order to prevent alpha-receptor actions and neuronal and extraneuronal uptake systems interfering with beta-receptor-mediated activity. In both tissues, 6-8 highly reproducible concentration-effect curves to (-)-isoprenaline could be established. However, the uterine preparation responded more robustly to repeated washings, required less sensitive recording apparatus, and showed responses to individual concentrations of drugs that were more readily quantified. However, in general, both preparations appear to be suitable as tissues for assessing the beta 2-adrenoceptor actions of drugs.

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Year:  1982        PMID: 6130188     DOI: 10.1016/0160-5402(82)90045-6

Source DB:  PubMed          Journal:  J Pharmacol Methods        ISSN: 0160-5402


  9 in total

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2.  Is Ro 03-7894 an irreversible antagonist at beta-adrenoceptor sites?

Authors:  E Krstew; G A McPherson; E Malta; P Molenaar; C Raper
Journal:  Br J Pharmacol       Date:  1984-06       Impact factor: 8.739

3.  Different mechanisms of action of agents acting on beta-adrenoceptors in barium-stimulated and electrically-stimulated rat vas deferens.

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Journal:  Br J Pharmacol       Date:  1991-09       Impact factor: 8.739

4.  Binding of agonists and antagonists to beta-adrenoceptors in rat vas deferens: relationship to functional response.

Authors:  J M May; P W Abel; K P Minneman
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-12       Impact factor: 3.000

5.  The influence of molecular structure on the affinity and efficacy of some beta-adrenoceptor agonists.

Authors:  P Molenaar; G A McPherson; E Malta; C Raper
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-11       Impact factor: 3.000

6.  The in vitro pharmacology of xamoterol (ICI 118,587).

Authors:  E Malta; M A Mian; C Raper
Journal:  Br J Pharmacol       Date:  1985-05       Impact factor: 8.739

7.  The affinity and efficacy of the selective beta 1-adrenoceptor stimulant RO363 at beta 1- and beta 2-adrenoceptor sites.

Authors:  G A McPherson; E Malta; P Molenaar; C Raper
Journal:  Br J Pharmacol       Date:  1984-08       Impact factor: 8.739

8.  Influence of thyroid status on responses of rat isolated pulmonary artery, vas deferens and trachea to smooth muscle relaxant drugs.

Authors:  S R O'Donnell; J C Wanstall; M B Mustafa
Journal:  Br J Pharmacol       Date:  1987-09       Impact factor: 8.739

9.  Responses to the beta 2-selective agonist procaterol of vascular and atrial preparations with different functional beta-adrenoceptor populations.

Authors:  S R O'Donnell; J C Wanstall
Journal:  Br J Pharmacol       Date:  1985-01       Impact factor: 8.739

  9 in total

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