Literature DB >> 6119400

[Antinoradrenergic activity of raubasine on isolated thoracic aorta and vas deferens of rat (author's transl)].

J Roquebert, P Gomond, P Demichel.   

Abstract

1. The type and intensity of antagonism exerted by yohimbine and raubasine on the noradrenaline action have been studied in vitro. 2. Cumulative dose-response curves with noradrenaline as the agonist, were made using isolated thoracic aorta and vas deferens of rat kept in a Krebs solution. When an antagonist shift the curve to the right the competitive nature of the interaction was verified by assessing the regression straight line of log (x-I) on log (antagonist concentration) and calculation of pA2. 3. In rat isolated vas deferens, the isotonic contractile response to low doses of noradrenaline were antagonized and those to high does potentiated by raubasine. The alpha-adrenoceptor blocker thus caused a shift to the right and an increase of the maximum height of log dose-response curves of alpha-adrenoceptor stimulant. Yohimbine shift the dose-response curves to the right without change of maximal contraction. The curves were analysed with the Schhild plot, and the slopes obtained 0.82 (Yohimbine), 0.96 (Raubasine) were not significantly different from I. The pA2 value is of 6.10 for yohimbine and of 6.50 for raubasine. In the presence of cocaine, which blocks the neuronal uptake, the dose-response curves were shifted to the right in parallel without alteration of maximal contraction. The pA2 value is of 6.57 for yohimbine and of 6.75 for raubasine. Yohimbine and raubasine carry on a competitive type antagonism on the noradrenaline effect. 4. On the thoracic aorta, yohimbine (pA2 = 6.83) and raubasine (pA2 = 7.21) act as competitive antagonists.

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Year:  1981        PMID: 6119400

Source DB:  PubMed          Journal:  J Pharmacol        ISSN: 0021-793X


  7 in total

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Authors:  G Benzi; A Gorini; B Ghigini; R Arnaboldi; R F Villa
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3.  Study of the mechanism of the relaxant action of (+)-glaucine in rat vas deferens.

Authors:  F Orallo; A Fernández Alzueta; M I Loza; N Vivas; A Badía; M Campos; M A Honrubia; M I Cadavid
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4.  Characterization of two distinct alpha-adrenoceptor binding sites in smooth muscle cell membranes from rat and bovine aorta.

Authors:  J J Descombes; J C Stoclet
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-05       Impact factor: 3.000

5.  alpha-Adrenoceptor blocking properties of raubasine in pithed rats.

Authors:  P Demichel; P Gomond; J Roquebert
Journal:  Br J Pharmacol       Date:  1982-11       Impact factor: 8.739

6.  Effects of four non-cholinergic cognitive enhancers in comparison with tacrine and galanthamine on scopolamine-induced amnesia in rats.

Authors:  P Chopin; M Briley
Journal:  Psychopharmacology (Berl)       Date:  1992       Impact factor: 4.530

7.  Modifications by hypoxia and drug treatment of cerebral ATPase plasticity.

Authors:  G Benzi; A Gorini; B Ghigini; R Arnaboldi; R F Villa
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  7 in total

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