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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Publicado: 1999
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Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v55_n2_p248_Rothlin
http://hdl.handle.net/20.500.12110/paper_0026895X_v55_n2_p248_Rothlin
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spelling paper:paper_0026895X_v55_n2_p248_Rothlin2023-06-08T14:53:56Z The α9 nicotinic acetylcholine receptor shares pharmacological properties with type A γ-aminobutyric acid, glycine, and type 3 serotonin receptors 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. 1999 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v55_n2_p248_Rothlin 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
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.
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
publishDate 1999
url https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v55_n2_p248_Rothlin
http://hdl.handle.net/20.500.12110/paper_0026895X_v55_n2_p248_Rothlin
_version_ 1768541834807607296