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http://acervodigital.unesp.br/handle/11449/36532
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DC Field | Value | Language |
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dc.contributor.author | Lima, V | - |
dc.contributor.author | Mueller, A. | - |
dc.contributor.author | Kamikihara, S. Y. | - |
dc.contributor.author | Raymundi, V | - |
dc.contributor.author | Alewood, D. | - |
dc.contributor.author | Lewis, R. J. | - |
dc.contributor.author | Chen, Z. J. | - |
dc.contributor.author | Minneman, K. P. | - |
dc.contributor.author | Pupo, A. S. | - |
dc.date.accessioned | 2014-05-20T15:26:21Z | - |
dc.date.accessioned | 2016-10-25T18:00:57Z | - |
dc.date.available | 2014-05-20T15:26:21Z | - |
dc.date.available | 2016-10-25T18:00:57Z | - |
dc.date.issued | 2005-01-31 | - |
dc.identifier | http://dx.doi.org/10.1016/j.ejphar.2004.12.011 | - |
dc.identifier.citation | European Journal of Pharmacology. Amsterdam: Elsevier B.V., v. 508, n. 1-3, p. 183-192, 2005. | - |
dc.identifier.issn | 0014-2999 | - |
dc.identifier.uri | http://hdl.handle.net/11449/36532 | - |
dc.identifier.uri | http://acervodigital.unesp.br/handle/11449/36532 | - |
dc.description.abstract | The ability of the conotoxin p-TIA, a 19-amino acid peptide isolated from the marine snail Conus tulipa, to antagonize contractions induced by noradrenaline through activation of alpha(1A)-adrenoceptors in rat vas deferens, alpha(1B)-adrenoceptors in rat spleen and alpha(ID)-adrenoceptors in rat aorta, and to inhibit the binding of [I-125]HEAT (2-[[beta-(4-hydroxyphenyl)ethyl]aminomethyl]-1-tetralone) to membranes of human embryonic kidney (HEK) 293 cells expressing each of the recombinant rat alpha(1)-adrenoceptors was investigated. p-TIA (100 nM to 1 muM) antagonized the contractions of vas deferens and aorta in response to noradrenaline without affecting maximal effects and with similar potencies (pA(2)similar to7.2, n=4). This suggests that p-TIA is a competitive antagonist of alpha(1A)- and alpha(1D)-adrenoceptors with no selectivity between these subtypes. Incubation of p-TIA (30 to 300 nM) with rat spleen caused a significant reduction of the maximal response to noradrenaline, suggesting that p-TIA is a non-competitive antagonist at alpha(1B)-adrenoceptors. After receptor inactivation with phenoxybenzamine, the potency of p-TIA in inhibiting contractions was examined with similar occupancies (similar to25%) at each subtype. Its potency (pIC(50)) was 12 times higher in spleen (8.3 +/- 0.1, n=4) than in vas deferens (7.2 +/- 0.1, n=4) or aorta (7.2 0.1, n=4). In radioligand binding assays, p-TIA decreased the number of binding sites (B,,,,,,) in membranes from HEK293 cells expressing the rat alpha(1B)-adrenoceptors without affecting affinity (K-D), In contrast, in HEK293 cells expressing rat alpha(1A)- or alpha(1D)-adrenoceptors, p-TTA decreased the KD without affecting the B-max. It is concluded that p-TIA will be useful for distinguishing the role of particular alpha(1)-adrenoceptor subtypes in native tissues. (C) 2004 Elsevier B.V. All rights reserved. | en |
dc.format.extent | 183-192 | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier B.V. | - |
dc.source | Web of Science | - |
dc.subject | alpha(1)-adrenoceptor | pt |
dc.subject | conotoxin p-TIA | pt |
dc.subject | vas deferens | pt |
dc.subject | spleen | pt |
dc.subject | aorta | pt |
dc.title | Differential antagonism by conotoxin p-TIA of contractions mediated by distinct alpha(1)-adrenoceptor subtypes in rat vas deferens, spleen and aorta | en |
dc.type | outro | - |
dc.contributor.institution | Universidade Estadual Paulista (UNESP) | - |
dc.contributor.institution | Xenome Ltd | - |
dc.contributor.institution | Emory Univ | - |
dc.description.affiliation | Univ Estadual Paulista Julio Mesquita Filho, Dept Pharmacol, Inst Biociencias, BR-18618000 Botucatu, SP, Brazil | - |
dc.description.affiliation | Xenome Ltd, Indooroopilly, Qld 4068, Australia | - |
dc.description.affiliation | Emory Univ, Sch Med, Dept Pharmacol, Atlanta, GA 30322 USA | - |
dc.description.affiliationUnesp | Univ Estadual Paulista Julio Mesquita Filho, Dept Pharmacol, Inst Biociencias, BR-18618000 Botucatu, SP, Brazil | - |
dc.identifier.doi | 10.1016/j.ejphar.2004.12.011 | - |
dc.identifier.wos | WOS:000226894000023 | - |
dc.rights.accessRights | Acesso restrito | - |
dc.relation.ispartof | European Journal of Pharmacology | - |
Appears in Collections: | Artigos, TCCs, Teses e Dissertações da Unesp |
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