We cescribe the functional properties of a nicotinic α9/serotonin subtype 3A (5HT3A) chimeric receptor expressed in Xenopus laevis oocytes. The chimera preserved ligand-binding properties of α9 and channel properties of 5HT3A.Thus, it responded to acetylcholine in a concentration-dependent manner with an EC50 of 70 μM but not to serotonin. It was blocked by methyllycaconitine, strychnine, atropine and nicotine, with the same rank order of potency as α9 receptors. The current-voltage relationship of currents through the α9/5HT3A chimera was similar to that of the 5HT3A receptors. These results are an evidence of functional coupling between the ligand-binding and the channel domains of the chimeric receptor. © 2003 Lippincott Williams & Wilkins.
Documento: | Artículo |
Título: | Functional expression and properties of a nicotinic α9/5-HT3 A chimeric receptor |
Autor: | Verbitsky, M.; Plazas, P.V.; Elgoyhen, A.B. |
Filiación: | Inst. Invest. Ing. Genet. Biol. M., Consejo Nac. de Invest. Cie. y Tec., Vuelta de Obligado 2490, Buenos Aires 1428, Argentina Columbia Genome Center, Columbia University, New York, NY 10032, United States |
Palabras clave: | Hair cells; Ion channels; Nicotinic receptors; Serotonin receptors; acetylcholine; atropine; chimeric protein; cholinergic receptor blocking agent; glycine receptor antagonist; methyllycaconitine; muscarinic receptor blocking agent; nicotine; nicotinic receptor; nicotinic receptor alpha5; nicotinic receptor alpha9; nicotinic receptor blocking agent; receptor subtype; receptor subunit; serotonin; serotonin 3 receptor; serotonin 3a receptor; strychnine; unclassified drug; aconitine; Chrna9 protein, rat; complementary DNA; drug derivative; hybrid protein; methyllycaconitine; nicotinic agent; serotonin antagonist; animal cell; article; concentration response; drug potency; drug receptor binding; electric current; electric potential; female; ligand binding; nonhuman; oocyte; priority journal; Xenopus laevis; animal; biosynthesis; cell membrane potential; drug effect; genetics; metabolism; patch clamp; physiology; rat; Aconitine; Animals; Atropine; DNA, Complementary; Membrane Potentials; Muscarinic Antagonists; Nicotine; Nicotinic Agonists; Nicotinic Antagonists; Oocytes; Patch-Clamp Techniques; Rats; Receptors, Nicotinic; Receptors, Serotonin, 5-HT3; Recombinant Fusion Proteins; Serotonin Antagonists; Strychnine; Xenopus laevis |
Año: | 2003 |
Volumen: | 14 |
Número: | 15 |
Página de inicio: | 1931 |
Página de fin: | 1934 |
DOI: | http://dx.doi.org/10.1097/00001756-200310270-00010 |
Título revista: | NeuroReport |
Título revista abreviado: | NeuroReport |
ISSN: | 09594965 |
CODEN: | NERPE |
CAS: | acetylcholine, 51-84-3, 60-31-1, 66-23-9; atropine, 51-55-8, 55-48-1; methyllycaconitine, 21019-30-7, 72629-98-2; nicotine, 54-11-5; serotonin, 50-67-9; strychnine, 1421-86-9, 57-24-9; aconitine, 127-29-7, 302-27-2, 4491-19-4, 6078-26-8, 6846-46-4; Aconitine, 302-27-2; Atropine, 51-55-8; Chrna9 protein, rat; DNA, Complementary; methyllycaconitine, 21019-30-7; Muscarinic Antagonists; Nicotine, 54-11-5; Nicotinic Agonists; Nicotinic Antagonists; Receptors, Nicotinic; Receptors, Serotonin, 5-HT3; Recombinant Fusion Proteins; Serotonin Antagonists; Strychnine, 57-24-9 |
Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_09594965_v14_n15_p1931_Verbitsky |