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

Detalhes bibliográficos
Autor(a) principal: Pupo, André S.
Data de Publicação: 1999
Outros Autores: Cavenaghi, Daniela LC, Campos, Marcelo, Morais, Paola D., Jurkiewicz, Neide Hyppolito [UNIFESP], Jurkiewicz, Aron [UNIFESP]
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNIFESP
Texto Completo: http://dx.doi.org/10.1038/sj.bjp.0702735
http://repositorio.unifesp.br/handle/11600/26118
Resumo: 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.
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spelling Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockadeindoraminalpha(1)-adrenoceptorsvas deferensaorta1 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.UNESP, Inst Biociencias, Dept Pharmacol, BR-18600000 Botucatu, SP, BrazilUNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, BrazilUNIFESP, Escola Paulista Med, Dept Pharmacol, BR-0403406 São Paulo, BrazilWeb of ScienceStockton PressUniversidade de São Paulo (USP)Universidade Federal de São Paulo (UNIFESP)Pupo, André S.Cavenaghi, Daniela LCCampos, MarceloMorais, Paola D.Jurkiewicz, Neide Hyppolito [UNIFESP]Jurkiewicz, Aron [UNIFESP]2016-01-24T12:30:51Z2016-01-24T12:30:51Z1999-08-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion1832-1836http://dx.doi.org/10.1038/sj.bjp.0702735British Journal of Pharmacology. Basingstoke: Stockton Press, v. 127, n. 8, p. 1832-1836, 1999.10.1038/sj.bjp.07027350007-1188http://repositorio.unifesp.br/handle/11600/26118WOS:000082312500010engBritish Journal of Pharmacologyinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UNIFESPinstname:Universidade Federal de São Paulo (UNIFESP)instacron:UNIFESP2021-09-30T15:48:16Zoai:repositorio.unifesp.br/:11600/26118Repositório InstitucionalPUBhttp://www.repositorio.unifesp.br/oai/requestbiblioteca.csp@unifesp.bropendoar:34652021-09-30T15:48:16Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)false
dc.title.none.fl_str_mv Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
title Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
spellingShingle Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
Pupo, André S.
indoramin
alpha(1)-adrenoceptors
vas deferens
aorta
title_short Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
title_full Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
title_fullStr Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
title_full_unstemmed Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
title_sort Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
author Pupo, André S.
author_facet Pupo, André S.
Cavenaghi, Daniela LC
Campos, Marcelo
Morais, Paola D.
Jurkiewicz, Neide Hyppolito [UNIFESP]
Jurkiewicz, Aron [UNIFESP]
author_role author
author2 Cavenaghi, Daniela LC
Campos, Marcelo
Morais, Paola D.
Jurkiewicz, Neide Hyppolito [UNIFESP]
Jurkiewicz, Aron [UNIFESP]
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade de São Paulo (USP)
Universidade Federal de São Paulo (UNIFESP)
dc.contributor.author.fl_str_mv Pupo, André S.
Cavenaghi, Daniela LC
Campos, Marcelo
Morais, Paola D.
Jurkiewicz, Neide Hyppolito [UNIFESP]
Jurkiewicz, Aron [UNIFESP]
dc.subject.por.fl_str_mv indoramin
alpha(1)-adrenoceptors
vas deferens
aorta
topic indoramin
alpha(1)-adrenoceptors
vas deferens
aorta
description 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.
publishDate 1999
dc.date.none.fl_str_mv 1999-08-01
2016-01-24T12:30:51Z
2016-01-24T12:30:51Z
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.1038/sj.bjp.0702735
British Journal of Pharmacology. Basingstoke: Stockton Press, v. 127, n. 8, p. 1832-1836, 1999.
10.1038/sj.bjp.0702735
0007-1188
http://repositorio.unifesp.br/handle/11600/26118
WOS:000082312500010
url http://dx.doi.org/10.1038/sj.bjp.0702735
http://repositorio.unifesp.br/handle/11600/26118
identifier_str_mv British Journal of Pharmacology. Basingstoke: Stockton Press, v. 127, n. 8, p. 1832-1836, 1999.
10.1038/sj.bjp.0702735
0007-1188
WOS:000082312500010
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv British Journal of Pharmacology
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv 1832-1836
dc.publisher.none.fl_str_mv Stockton Press
publisher.none.fl_str_mv Stockton Press
dc.source.none.fl_str_mv reponame:Repositório Institucional da UNIFESP
instname:Universidade Federal de São Paulo (UNIFESP)
instacron:UNIFESP
instname_str Universidade Federal de São Paulo (UNIFESP)
instacron_str UNIFESP
institution UNIFESP
reponame_str Repositório Institucional da UNIFESP
collection Repositório Institucional da UNIFESP
repository.name.fl_str_mv Repositório Institucional da UNIFESP - Universidade Federal de São Paulo (UNIFESP)
repository.mail.fl_str_mv biblioteca.csp@unifesp.br
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