Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade

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dc.contributor.author Pupo, André S.
dc.contributor.author Cavenaghi, Daniela LC
dc.contributor.author Campos, Marcelo
dc.contributor.author Morais, Paola D.
dc.contributor.author Jurkiewicz, Neide Hyppolito [UNIFESP]
dc.contributor.author Jurkiewicz, Aron [UNIFESP]
dc.date.accessioned 2016-01-24T12:30:51Z
dc.date.available 2016-01-24T12:30:51Z
dc.date.issued 1999-08-01
dc.identifier http://dx.doi.org/10.1038/sj.bjp.0702735
dc.identifier.citation British Journal of Pharmacology. Basingstoke: Stockton Press, v. 127, n. 8, p. 1832-1836, 1999.
dc.identifier.issn 0007-1188
dc.identifier.uri http://repositorio.unifesp.br/handle/11600/26118
dc.description.abstract 1 the actions of the alpha(1)-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 pA(2) 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 mu M) the potency (pA(2)) 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 (pA(2) = 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 alpha(1)-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 neuronal uptake. As a major consequence of this double mechanism of action, the pA(2) values for this antagonist are underestimated when calculated in situations where the neuronal uptake is active, yielding spurious pK(B) values. en
dc.format.extent 1832-1836
dc.language.iso eng
dc.publisher Stockton Press
dc.relation.ispartof British Journal of Pharmacology
dc.rights Acesso aberto
dc.subject indoramin en
dc.subject alpha(1)-adrenoceptors en
dc.subject vas deferens en
dc.subject aorta en
dc.title Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade en
dc.type Artigo
dc.contributor.institution Universidade de São Paulo (USP)
dc.contributor.institution Universidade Federal de São Paulo (UNIFESP)
dc.description.affiliation UNESP, Inst Biociencias, Dept Pharmacol, BR-18600000 Botucatu, SP, Brazil
dc.description.affiliation UNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, Brazil
dc.description.affiliationUnifesp UNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, Brazil
dc.identifier.doi 10.1038/sj.bjp.0702735
dc.description.source Web of Science
dc.identifier.wos WOS:000082312500010



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