Artículo

Rothlin, C.V.; Lioudyno, M.I.; Silbering, A.F.; Plazas, P.V.; Gomez Casati, M.E.; Katz, E.; Guth, P.S.; Elgoyhen, A.B. "Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors" (2003) Molecular Pharmacology. 63(5):1067-1074
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Abstract:

In the present work, we characterized the effects of serotonin type 3 receptor ligands on recombinant and native α9α10-containing nicotinic acetylcholine receptors (nAChRs). Our results indicate that the recombinant α9α10 nAChR shares striking pharmacological properties with 5-HT3 ligand-gated ion channels. Thus, 5-HT3 receptor antagonists block ACh-evoked currents in α9α10-injected Xenopus laevis oocytes with a rank order of potency of tropisetron (IC50, 70.1 ± 0.9 nM) > ondansetron (IC50, 0.6 ± 0.1 μM) = MDL 72222 (IC50, 0.7 ± 0.1 μM). Although serotonin does not elicit responses in α9α10-injected oocytes, it blocks recombinant α9α10 receptors in a noncompetitive and voltage-dependent manner (IC50, 5.4 ± 0.6 μM). On the other hand, we demonstrate an in vivo correlate of these properties of the recombinant receptor, with those of the α9α10-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.

Registro:

Documento: Artículo
Título:Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors
Autor:Rothlin, C.V.; Lioudyno, M.I.; Silbering, A.F.; Plazas, P.V.; Gomez Casati, M.E.; Katz, E.; Guth, P.S.; Elgoyhen, A.B.
Filiación:Inst. Invest. Ing. Genet./Biol. M., Consejo Nac. de Invest. Cie. y Tec., Universidad de Buenos Aires, Buenos Aires, Argentina
Departamento de Biologia, Fac. de Cie. Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires, Argentina
Department of Pharmacology, Tulane University, New Orleans, LA, United States
Inst. Invest. Ing. Genet./Biol. M., CONICET-UBA, Vuelta de Obligado 2490, 1428 Buenos Aires, Argentina
Palabras clave:biogenic amine; ion channel; nicotinic receptor; ondansetron; recombinant receptor; serotonin; serotonin 3 antagonist; tropisetron; animal cell; article; cholinergic transmission; controlled study; Corti organ; drug potency; drug receptor binding; neuromodulation; nonhuman; priority journal; vestibular system; Xenopus laevis; Animals; Electrophysiology; Hair Cells; Indoles; Oocytes; Receptors, Nicotinic; Receptors, Serotonin; Receptors, Serotonin, 5-HT3; Recombinant Proteins; Serotonin; Xenopus laevis
Año:2003
Volumen:63
Número:5
Página de inicio:1067
Página de fin:1074
DOI: http://dx.doi.org/10.1124/mol.63.5.1067
Título revista:Molecular Pharmacology
Título revista abreviado:Mol. Pharmacol.
ISSN:0026895X
CODEN:MOPMA
CAS:ondansetron, 103639-04-9, 116002-70-1, 99614-01-4; serotonin, 50-67-9; tropisetron, 89565-68-4; Indoles; nAChR alpha9; nicotinic receptor alpha4beta2; Receptors, Nicotinic; Receptors, Serotonin; Receptors, Serotonin, 5-HT3; Recombinant Proteins; Serotonin, 50-67-9; tropisetron, 89565-68-4
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v63_n5_p1067_Rothlin

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Citas:

---------- APA ----------
Rothlin, C.V., Lioudyno, M.I., Silbering, A.F., Plazas, P.V., Gomez Casati, M.E., Katz, E., Guth, P.S.,..., Elgoyhen, A.B. (2003) . Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors. Molecular Pharmacology, 63(5), 1067-1074.
http://dx.doi.org/10.1124/mol.63.5.1067
---------- CHICAGO ----------
Rothlin, C.V., Lioudyno, M.I., Silbering, A.F., Plazas, P.V., Gomez Casati, M.E., Katz, E., et al. "Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors" . Molecular Pharmacology 63, no. 5 (2003) : 1067-1074.
http://dx.doi.org/10.1124/mol.63.5.1067
---------- MLA ----------
Rothlin, C.V., Lioudyno, M.I., Silbering, A.F., Plazas, P.V., Gomez Casati, M.E., Katz, E., et al. "Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors" . Molecular Pharmacology, vol. 63, no. 5, 2003, pp. 1067-1074.
http://dx.doi.org/10.1124/mol.63.5.1067
---------- VANCOUVER ----------
Rothlin, C.V., Lioudyno, M.I., Silbering, A.F., Plazas, P.V., Gomez Casati, M.E., Katz, E., et al. Direct interaction of serotonin type 3 receptor ligands with recombinant and native α9α10-containing nicotinic cholinergic receptors. Mol. Pharmacol. 2003;63(5):1067-1074.
http://dx.doi.org/10.1124/mol.63.5.1067