Effects of indoramin in rat vas deferens and aorta: concomitant alpha1-adrenoceptor and neuronal uptake blockade

British Journal of Pharmacology
André S PupoA Jurkiewicz

Abstract

1. The actions of the alpha1-adrenoceptor antagonist indoramin have been examined against the contractions induced by noradrenaline in the rat vas deferens and aorta taking into account a putative neuronal uptake blocking activity of this antagonist which could result in self-cancelling actions. 2. Indoramin behaved as a simple competitive antagonist of the contractions induced by noradrenaline in the vas deferens and aorta yielding pA2 values of 7.38+/-0.05 (slope=0.98+/-0.03) and 6.78+/-0.14 (slope=1.08+/-0.06), respectively. 3. When the experiments were repeated in the presence of cocaine (6 microM) the potency (pA2) of indoramin in antagonizing the contractions of the vas deferens to noradrenaline was increased to 8.72+/-0.07 (slope=1.10+/-0.05) while its potency remained unchanged in the aorta (pA2=6.69+/-0.12; slope=1.04+/-0.05). 4. In denervated vas deferens, indoramin antagonized the contractions to noradrenaline with a potency similar to that found in the presence of cocaine (8.79+/-0.07; slope=1.09+/-0.06). 5. It is suggested that indoramin blocks alpha1-adrenoceptors and neuronal uptake in rat vas deferens resulting in Schild plots with slopes not different from unity even in the absence of selective inhibition of ne...Continue Reading

References

Feb 1, 1976·British Journal of Pharmacology·A Jurkiewicz, N H Jurkiewicz
Nov 1, 1969·European Journal of Pharmacology·Y KasuyaM Watanabe
Jan 1, 1984·Clinical and Experimental Pharmacology & Physiology·J L Black, E J Mylecharane
Aug 1, 1998·European Journal of Pharmacology·A S Pupo
Dec 16, 1998·European Journal of Pharmacology·J R Docherty
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD

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Citations

Jun 24, 2003·European Journal of Pharmacology·Marcelo CamposAndré S Pupo
Oct 25, 2003·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·M CamposA S Pupo
Jan 29, 2005·British Journal of Pharmacology·Isaltino M ConceiçãoLúcia Garcez-do-Carmo

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