The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors
In the present study, we provide evidence that the α9 nicotinic acetylcholine receptor (nAChR) shares pharmacological properties with members of the Cys-loop family of receptors. Thus, the type A γ-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type...
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todo:paper_0026895X_v55_n2_p248_Rothlin2023-10-03T14:37:11Z The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors Rothlin, C.V. Katz, E. Verbitsky, M. Belén Elgoyhen, A. 4 aminobutyric acid 4 aminobutyric acid A receptor 4 aminobutyric acid A receptor blocking agent acetylcholine bicuculline cysteine ethylene glycol 1,2 bis(2 aminophenyl) ether n,n,n',n' tetraacetic acid glycine glycine receptor glycine receptor antagonist ligand nicotinic receptor receptor blocking agent serotonin 3 antagonist serotonin 3 receptor strychnine tropisetron 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid 4 aminobutyric acid A receptor 4 aminobutyric acid receptor blocking agent amino acid receptor affecting agent barium bicuculline calcium chelating agent complementary DNA drug derivative egtazic acid glycine receptor hybrid protein Indo 1 pentaacetoxymethyl ester Indo-1 pentaacetoxymethyl ester indole derivative nicotinic receptor serotonin serotonin 3 receptor serotonin antagonist serotonin receptor strychnine tropisetron animal cell article competitive inhibition concentration response controlled study hair cell ligand binding nonhuman oocyte priority journal receptor binding Xenopus animal cell membrane potential drug effect female genetics metabolism Xenopus laevis Acetylcholine Animals Barium Bicuculline Calcium Chelating Agents DNA, Complementary Egtazic Acid Female GABA Antagonists Glycine Glycine Agents Indoles Membrane Potentials Oocytes Receptors, GABA-A Receptors, Glycine Receptors, Nicotinic Receptors, Serotonin Receptors, Serotonin, 5-HT3 Recombinant Fusion Proteins Serotonin Serotonin Antagonists Strychnine Xenopus laevis In the present study, we provide evidence that the α9 nicotinic acetylcholine receptor (nAChR) shares pharmacological properties with members of the Cys-loop family of receptors. Thus, the type A γ-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type 3 serotonin receptor antagonist ICS-205,930 block ACh-evoked currents in α9-injected Xenopus laevis oocytes with the following rank order of potency: strychnine > ICS-205,930 > bicuculline. Block by antagonists was reflected in an increase in the acetylcholine (ACh) EC50 value, with no changes in agonist maximal response or Hill coefficient, which suggests a competitive type of block. Moreover, whereas neither γ-aminobutyric acid nor glycine modified ACh-evoked currents, serotonin blocked responses to ACh in a concentration-dependent manner. The present results suggest that the α9 nAChR must conserve in its primary structure some residues responsible for ligand binding common to other Cys-loop receptors. In addition, it adds further evidence that the α9 nAChR and the cholinergic receptor present at the base of cochlear outer hair cells have similar pharmacological properties. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar http://hdl.handle.net/20.500.12110/paper_0026895X_v55_n2_p248_Rothlin |
| institution |
Universidad de Buenos Aires |
| institution_str |
I-28 |
| repository_str |
R-134 |
| collection |
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) |
| topic |
4 aminobutyric acid 4 aminobutyric acid A receptor 4 aminobutyric acid A receptor blocking agent acetylcholine bicuculline cysteine ethylene glycol 1,2 bis(2 aminophenyl) ether n,n,n',n' tetraacetic acid glycine glycine receptor glycine receptor antagonist ligand nicotinic receptor receptor blocking agent serotonin 3 antagonist serotonin 3 receptor strychnine tropisetron 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid 4 aminobutyric acid A receptor 4 aminobutyric acid receptor blocking agent amino acid receptor affecting agent barium bicuculline calcium chelating agent complementary DNA drug derivative egtazic acid glycine receptor hybrid protein Indo 1 pentaacetoxymethyl ester Indo-1 pentaacetoxymethyl ester indole derivative nicotinic receptor serotonin serotonin 3 receptor serotonin antagonist serotonin receptor strychnine tropisetron animal cell article competitive inhibition concentration response controlled study hair cell ligand binding nonhuman oocyte priority journal receptor binding Xenopus animal cell membrane potential drug effect female genetics metabolism Xenopus laevis Acetylcholine Animals Barium Bicuculline Calcium Chelating Agents DNA, Complementary Egtazic Acid Female GABA Antagonists Glycine Glycine Agents Indoles Membrane Potentials Oocytes Receptors, GABA-A Receptors, Glycine Receptors, Nicotinic Receptors, Serotonin Receptors, Serotonin, 5-HT3 Recombinant Fusion Proteins Serotonin Serotonin Antagonists Strychnine Xenopus laevis |
| spellingShingle |
4 aminobutyric acid 4 aminobutyric acid A receptor 4 aminobutyric acid A receptor blocking agent acetylcholine bicuculline cysteine ethylene glycol 1,2 bis(2 aminophenyl) ether n,n,n',n' tetraacetic acid glycine glycine receptor glycine receptor antagonist ligand nicotinic receptor receptor blocking agent serotonin 3 antagonist serotonin 3 receptor strychnine tropisetron 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid 4 aminobutyric acid A receptor 4 aminobutyric acid receptor blocking agent amino acid receptor affecting agent barium bicuculline calcium chelating agent complementary DNA drug derivative egtazic acid glycine receptor hybrid protein Indo 1 pentaacetoxymethyl ester Indo-1 pentaacetoxymethyl ester indole derivative nicotinic receptor serotonin serotonin 3 receptor serotonin antagonist serotonin receptor strychnine tropisetron animal cell article competitive inhibition concentration response controlled study hair cell ligand binding nonhuman oocyte priority journal receptor binding Xenopus animal cell membrane potential drug effect female genetics metabolism Xenopus laevis Acetylcholine Animals Barium Bicuculline Calcium Chelating Agents DNA, Complementary Egtazic Acid Female GABA Antagonists Glycine Glycine Agents Indoles Membrane Potentials Oocytes Receptors, GABA-A Receptors, Glycine Receptors, Nicotinic Receptors, Serotonin Receptors, Serotonin, 5-HT3 Recombinant Fusion Proteins Serotonin Serotonin Antagonists Strychnine Xenopus laevis Rothlin, C.V. Katz, E. Verbitsky, M. Belén Elgoyhen, A. The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| topic_facet |
4 aminobutyric acid 4 aminobutyric acid A receptor 4 aminobutyric acid A receptor blocking agent acetylcholine bicuculline cysteine ethylene glycol 1,2 bis(2 aminophenyl) ether n,n,n',n' tetraacetic acid glycine glycine receptor glycine receptor antagonist ligand nicotinic receptor receptor blocking agent serotonin 3 antagonist serotonin 3 receptor strychnine tropisetron 1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid 4 aminobutyric acid A receptor 4 aminobutyric acid receptor blocking agent amino acid receptor affecting agent barium bicuculline calcium chelating agent complementary DNA drug derivative egtazic acid glycine receptor hybrid protein Indo 1 pentaacetoxymethyl ester Indo-1 pentaacetoxymethyl ester indole derivative nicotinic receptor serotonin serotonin 3 receptor serotonin antagonist serotonin receptor strychnine tropisetron animal cell article competitive inhibition concentration response controlled study hair cell ligand binding nonhuman oocyte priority journal receptor binding Xenopus animal cell membrane potential drug effect female genetics metabolism Xenopus laevis Acetylcholine Animals Barium Bicuculline Calcium Chelating Agents DNA, Complementary Egtazic Acid Female GABA Antagonists Glycine Glycine Agents Indoles Membrane Potentials Oocytes Receptors, GABA-A Receptors, Glycine Receptors, Nicotinic Receptors, Serotonin Receptors, Serotonin, 5-HT3 Recombinant Fusion Proteins Serotonin Serotonin Antagonists Strychnine Xenopus laevis |
| description |
In the present study, we provide evidence that the α9 nicotinic acetylcholine receptor (nAChR) shares pharmacological properties with members of the Cys-loop family of receptors. Thus, the type A γ-aminobutyric acid receptor antagonist bicuculline, the glycinergic antagonist strychnine, and the type 3 serotonin receptor antagonist ICS-205,930 block ACh-evoked currents in α9-injected Xenopus laevis oocytes with the following rank order of potency: strychnine > ICS-205,930 > bicuculline. Block by antagonists was reflected in an increase in the acetylcholine (ACh) EC50 value, with no changes in agonist maximal response or Hill coefficient, which suggests a competitive type of block. Moreover, whereas neither γ-aminobutyric acid nor glycine modified ACh-evoked currents, serotonin blocked responses to ACh in a concentration-dependent manner. The present results suggest that the α9 nAChR must conserve in its primary structure some residues responsible for ligand binding common to other Cys-loop receptors. In addition, it adds further evidence that the α9 nAChR and the cholinergic receptor present at the base of cochlear outer hair cells have similar pharmacological properties. |
| format |
JOUR |
| author |
Rothlin, C.V. Katz, E. Verbitsky, M. Belén Elgoyhen, A. |
| author_facet |
Rothlin, C.V. Katz, E. Verbitsky, M. Belén Elgoyhen, A. |
| author_sort |
Rothlin, C.V. |
| title |
The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| title_short |
The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| title_full |
The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| title_fullStr |
The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| title_full_unstemmed |
The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| title_sort |
α9 nicotinic acetylcholine receptor shares pharmacological properties with type a γ-aminobutyric acid, glycine, and type 3 serotonin receptors |
| url |
http://hdl.handle.net/20.500.12110/paper_0026895X_v55_n2_p248_Rothlin |
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