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Abstract:

The rat α9 nicotinic acetylcholine receptor (nAChR) was expressed in Xenopus laevis oocytes and tested for its sensitivity to a wide variety of cholinergic compounds. Acetylcholine (ACh), carbachol, choline and methylcarbachol elicited agonist-evoked currents, giving maximal or near maximal responses. Both the nicotinic agonist suberyldicholine as well as the muscarinic agonists McN-A-343 and methylfurtrethonium behaved as weak partial agonists of the receptor. Most classical cholinergic compounds tested, being either nicotinic (nicotine, epibatidine, cytisine, methyllycaconitine, mecamylamine, dihydro-β-erythroidine), or muscarinic (muscarine, atropine, gallamine, pilocarpine, bethanechol) agonists and antagonists, blocked the recombinant α9 receptor. Block by nicotine, epibatidine, cytisine, methyllycaconitine and atropine was overcome at high ACh concentrations, suggesting a competitive type of block. The present results indicate that α9 displays mixed nicotinic-muscarinic features that resemble the ones described for the cholinergic receptor of cochlear outer hair cells (OHCs). We suggest that α9 contains the structural determinants responsible for the pharmacological properties of the native receptor. Copyright (C) 2000 Elsevier Science Ltd.

Registro:

Documento: Artículo
Título:Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor
Autor:Verbitsky, M.; Rothlin, C.V.; Katz, E.; Belén Elgoyhen, A.
Filiación:Instituto de Investigaciones en Ingeniería Genética y Biología Molecular, Consejo Nacional de Investigaciones Científicas y Técnicas, Universidad de Buenos Aires, Vuelta de Obligado 2490, Buenos Aires 1428, Argentina
Departamento de Biología, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires 1428, Argentina
Palabras clave:Cochlea; Hair cells; Ion channels; Muscarinic receptors; Neurotransmitter receptors; Nicotinic receptors; acetylcholine; atropine; bethanechol; carbachol; choline; cholinergic receptor stimulating agent; cytisine; dicholine suberate; dihydro beta erythroidine; epibatidine; gallamine; ion channel; mecamylamine; methylcarbachol; methyllycaconitine; muscarine; muscarinic agent; muscarinic receptor; muscarinic receptor blocking agent; neurotransmitter receptor; nicotine; nicotinic agent; nicotinic receptor; nicotinic receptor blocking agent; phenyltrimethylammonium; pilocarpine; pirenzepine; tetramethylammonium; [4 [(3 chlorophenyl)carbamoyloxy] 2 butynyl]trimethylammonium; animal cell; binding site; cochlea; controlled study; drug receptor binding; electrophysiology; hair cell; nonhuman; oocyte; priority journal; review; Xenopus laevis
Año:2000
Volumen:39
Número:13
Página de inicio:2515
Página de fin:2524
DOI: http://dx.doi.org/10.1016/S0028-3908(00)00124-6
Título revista:Neuropharmacology
Título revista abreviado:Neuropharmacology
ISSN:00283908
CODEN:NEPHB
CAS:acetylcholine, 51-84-3, 60-31-1, 66-23-9; atropine, 51-55-8, 55-48-1; bethanechol, 590-63-6, 674-38-4, 91609-06-2; carbachol, 462-58-8, 51-83-2; choline, 123-41-1, 13232-47-8, 1927-06-6, 4858-96-2, 62-49-7, 67-48-1; cytisine, 485-35-8; dicholine suberate, 3810-71-7, 7262-79-5; dihydro beta erythroidine, 23255-54-1; epibatidine, 140111-52-0, 148152-66-3, 152378-30-8; gallamine, 153-76-4; mecamylamine, 60-40-2, 826-39-1; methylcarbachol, 14721-69-8; methyllycaconitine, 21019-30-7, 72629-98-2; muscarine, 300-54-9; nicotine, 54-11-5; phenyltrimethylammonium, 138-24-9, 3426-74-2; pilocarpine, 148-72-1, 54-71-7, 92-13-7; pirenzepine, 28797-61-7, 29868-97-1; tetramethylammonium, 51-92-3; [4 [(3 chlorophenyl)carbamoyloxy] 2 butynyl]trimethylammonium, 55-45-8
Registro:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_00283908_v39_n13_p2515_Verbitsky

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Citas:

---------- APA ----------
Verbitsky, M., Rothlin, C.V., Katz, E. & Belén Elgoyhen, A. (2000) . Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor. Neuropharmacology, 39(13), 2515-2524.
http://dx.doi.org/10.1016/S0028-3908(00)00124-6
---------- CHICAGO ----------
Verbitsky, M., Rothlin, C.V., Katz, E., Belén Elgoyhen, A. "Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor" . Neuropharmacology 39, no. 13 (2000) : 2515-2524.
http://dx.doi.org/10.1016/S0028-3908(00)00124-6
---------- MLA ----------
Verbitsky, M., Rothlin, C.V., Katz, E., Belén Elgoyhen, A. "Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor" . Neuropharmacology, vol. 39, no. 13, 2000, pp. 2515-2524.
http://dx.doi.org/10.1016/S0028-3908(00)00124-6
---------- VANCOUVER ----------
Verbitsky, M., Rothlin, C.V., Katz, E., Belén Elgoyhen, A. Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor. Neuropharmacology. 2000;39(13):2515-2524.
http://dx.doi.org/10.1016/S0028-3908(00)00124-6