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Direct interaction of serotonin type 3 receptor ligands with recombinant and native alpha 9 alpha 10-containing nicotinic cholinergic receptors.
Rothlin, Carla V; Lioudyno, Maria I; Silbering, Ana F; Plazas, Paola V; Casati, María E Gomez; Katz, Eleonora; Guth, Paul S; Elgoyhen, A Belén.
Afiliação
  • Rothlin CV; Instituto de Investigaciones en Ingeniería Genética y Biología Molecular, Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad de Buenos Aires, Argentina.
Mol Pharmacol ; 63(5): 1067-74, 2003 May.
Article em En | MEDLINE | ID: mdl-12695535
In the present work, we characterized the effects of serotonin type 3 receptor ligands on recombinant and native alpha 9 alpha 10-containing nicotinic acetylcholine receptors (nAChRs). Our results indicate that the recombinant alpha 9 alpha 10 nAChR shares striking pharmacological properties with 5-HT(3) ligand-gated ion channels. Thus, 5-HT(3) receptor antagonists block ACh-evoked currents in alpha 9 alpha 10-injected Xenopus laevis oocytes with a rank order of potency of tropisetron (IC(50), 70.1 +/- 0.9 nM) > ondansetron (IC(50), 0.6 +/- 0.1 microM) = MDL 72222 (IC(50), 0.7 +/- 0.1 microM). Although serotonin does not elicit responses in alpha 9 alpha 10-injected oocytes, it blocks recombinant alpha 9 alpha 10 receptors in a noncompetitive and voltage-dependent manner (IC(50), 5.4 +/- 0.6 microM). On the other hand, we demonstrate an in vivo correlate of these properties of the recombinant receptor, with those of the alpha 9 alpha 10-containing nAChR of frog saccular hair cells. The possibility that the biogenic amine serotonin might act as a neuromodulator of the cholinergic efferent transmission in the vestibular apparatus and in the organ of Corti is discussed.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Serotonina / Receptores Nicotínicos Limite: Animals Idioma: En Revista: Mol Pharmacol Ano de publicação: 2003 Tipo de documento: Article País de afiliação: Argentina País de publicação: Estados Unidos
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Serotonina / Receptores Nicotínicos Limite: Animals Idioma: En Revista: Mol Pharmacol Ano de publicação: 2003 Tipo de documento: Article País de afiliação: Argentina País de publicação: Estados Unidos