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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| Acceso en línea: | http://hdl.handle.net/20.500.12110/paper_00283908_v39_n13_p2515_Verbitsky |
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todo:paper_00283908_v39_n13_p2515_Verbitsky2023-10-03T14:39:03Z Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor Verbitsky, M. Rothlin, C.V. Katz, E. Belén Elgoyhen, A. 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 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. Fil:Verbitsky, M. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Katz, E. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_00283908_v39_n13_p2515_Verbitsky |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
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 |
| spellingShingle |
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 Verbitsky, M. Rothlin, C.V. Katz, E. Belén Elgoyhen, A. Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| topic_facet |
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 |
| description |
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. |
| format |
JOUR |
| author |
Verbitsky, M. Rothlin, C.V. Katz, E. Belén Elgoyhen, A. |
| author_facet |
Verbitsky, M. Rothlin, C.V. Katz, E. Belén Elgoyhen, A. |
| author_sort |
Verbitsky, M. |
| title |
Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| title_short |
Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| title_full |
Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| title_fullStr |
Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| title_full_unstemmed |
Mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| title_sort |
mixed nicotinic-muscarinic properties of the α9 nicotinic cholinergic receptor |
| url |
http://hdl.handle.net/20.500.12110/paper_00283908_v39_n13_p2515_Verbitsky |
| work_keys_str_mv |
AT verbitskym mixednicotinicmuscarinicpropertiesofthea9nicotiniccholinergicreceptor AT rothlincv mixednicotinicmuscarinicpropertiesofthea9nicotiniccholinergicreceptor AT katze mixednicotinicmuscarinicpropertiesofthea9nicotiniccholinergicreceptor AT belenelgoyhena mixednicotinicmuscarinicpropertiesofthea9nicotiniccholinergicreceptor |
| _version_ |
1782026541124812800 |