Effects of indoramin in rat vas deferens and aorta: concomitant alpha(1)-adrenoceptor and neuronal uptake blockade
Autor(a) principal: | |
---|---|
Data de Publicação: | 1999 |
Outros Autores: | , , , , |
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. |
id |
UFSP_3cb247b54ba3ddb886ef0979688304c8 |
---|---|
oai_identifier_str |
oai:repositorio.unifesp.br/:11600/26118 |
network_acronym_str |
UFSP |
network_name_str |
Repositório Institucional da UNIFESP |
repository_id_str |
3465 |
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 |
_version_ |
1814268363871879168 |