Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor

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 response...

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Autor principal: Verbitsky, M.
Otros Autores: Rothlin, C.V, Katz, E., Belén Elgoyhen, A.
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: Elsevier Ltd 2000
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024 7 |2 scopus  |a 2-s2.0-0033814975 
024 7 |2 cas  |a 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 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
030 |a NEPHB 
100 1 |a Verbitsky, M. 
245 1 0 |a Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor 
260 |b Elsevier Ltd  |c 2000 
270 1 0 |m Belen Elgoyhen, A.; Istituto de Investigaciones, Consejo Nac. Invest. Cientificas, Universidad de Buenos Aires, Vuelta de Obligado 2490, Buenos Aires 1428, Argentina; email: elgoyhen@dna.uba.ar 
506 |2 openaire  |e Política editorial 
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520 3 |a 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.  |l eng 
536 |a Detalles de la financiación: Agencia Nacional de Promoción Científica y Tecnológica 
536 |a Detalles de la financiación: Howard Hughes Medical Institute 
536 |a Detalles de la financiación: Fundación Antorchas 
536 |a Detalles de la financiación: National Organization for Hearing Research Foundation 
536 |a Detalles de la financiación: This work was supported by an International Research Scholar grant from the Howard Hughes Medical Institute, the National Organization for Hearing Research (USA), Fundación Antorchas and Agencia Nacional de Promoción Cientı́fica y Tecnológica (Argentina). 
593 |a 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 
593 |a Departamento de Biología, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Buenos Aires 1428, Argentina 
690 1 0 |a COCHLEA 
690 1 0 |a HAIR CELLS 
690 1 0 |a ION CHANNELS 
690 1 0 |a MUSCARINIC RECEPTORS 
690 1 0 |a NEUROTRANSMITTER RECEPTORS 
690 1 0 |a NICOTINIC RECEPTORS 
690 1 0 |a ACETYLCHOLINE 
690 1 0 |a ATROPINE 
690 1 0 |a BETHANECHOL 
690 1 0 |a CARBACHOL 
690 1 0 |a CHOLINE 
690 1 0 |a CHOLINERGIC RECEPTOR STIMULATING AGENT 
690 1 0 |a CYTISINE 
690 1 0 |a DICHOLINE SUBERATE 
690 1 0 |a DIHYDRO BETA ERYTHROIDINE 
690 1 0 |a EPIBATIDINE 
690 1 0 |a GALLAMINE 
690 1 0 |a ION CHANNEL 
690 1 0 |a MECAMYLAMINE 
690 1 0 |a METHYLCARBACHOL 
690 1 0 |a METHYLLYCACONITINE 
690 1 0 |a MUSCARINE 
690 1 0 |a MUSCARINIC AGENT 
690 1 0 |a MUSCARINIC RECEPTOR 
690 1 0 |a MUSCARINIC RECEPTOR BLOCKING AGENT 
690 1 0 |a NEUROTRANSMITTER RECEPTOR 
690 1 0 |a NICOTINE 
690 1 0 |a NICOTINIC AGENT 
690 1 0 |a NICOTINIC RECEPTOR 
690 1 0 |a NICOTINIC RECEPTOR BLOCKING AGENT 
690 1 0 |a PHENYLTRIMETHYLAMMONIUM 
690 1 0 |a PILOCARPINE 
690 1 0 |a PIRENZEPINE 
690 1 0 |a TETRAMETHYLAMMONIUM 
690 1 0 |a [4 [(3 CHLOROPHENYL)CARBAMOYLOXY] 2 BUTYNYL]TRIMETHYLAMMONIUM 
690 1 0 |a ANIMAL CELL 
690 1 0 |a BINDING SITE 
690 1 0 |a COCHLEA 
690 1 0 |a CONTROLLED STUDY 
690 1 0 |a DRUG RECEPTOR BINDING 
690 1 0 |a ELECTROPHYSIOLOGY 
690 1 0 |a HAIR CELL 
690 1 0 |a NONHUMAN 
690 1 0 |a OOCYTE 
690 1 0 |a PRIORITY JOURNAL 
690 1 0 |a REVIEW 
690 1 0 |a XENOPUS LAEVIS 
653 0 0 |a mcn-a-343, RBI, United States 
700 1 |a Rothlin, C.V. 
700 1 |a Katz, E. 
700 1 |a Belén Elgoyhen, A. 
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