GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer (Q34778798)

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English	GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer	scientific article

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scholarly article

1 reference

Europe PubMed Central

4 August 2017

1 reference

Europe PubMed Central

GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer (English)

1 reference

Europe PubMed Central

4 August 2017

author name string

John R Atack

1

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Europe PubMed Central

4 August 2017

publication date

1 January 2008

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Europe PubMed Central

4 August 2017

CNS Neuroscience & Therapeutics

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Europe PubMed Central

4 August 2017

14

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Europe PubMed Central

4 August 2017

1

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Europe PubMed Central

4 August 2017

25-35

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Europe PubMed Central

4 August 2017

Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

The benzodiazepine binding site of GABA A receptors as a target for the development of novel anxiolytics

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Anxiogenic properties of an inverse agonist selective for alpha3 subunit-containing GABA A receptors

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

The proconvulsant effects of the GABAA alpha5 subtype-selective compound RY-080 may not be alpha5-mediated.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Pharmacology of recombinant gamma-aminobutyric acidA receptors rendered diazepam-insensitive by point-mutated alpha-subunits.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Identification of a Novel, Selective GABAAα5 Receptor Inverse Agonist Which Enhances Cognition

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Alpha5GABAA receptors mediate the amnestic but not sedative-hypnotic effects of the general anesthetic etomidate.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Trace fear conditioning involves hippocampal alpha5 GABA(A) receptors

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Pharmacodynamic and pharmacokinetic effects of TPA023, a GABA(A) alpha(2,3) subtype-selective agonist, compared to lorazepam and placebo in healthy volunteers.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Severe anxiety induced by FG 7142, a beta-carboline ligand for benzodiazepine receptors.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

GABAA-receptor heterogeneity in the adult rat brain: differential regional and cellular distribution of seven major subunits

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Novel anxiolytics that act as partial agonists at benzodiazepine receptors

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABAA receptors.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Molecular and neuronal substrate for the selective attenuation of anxiety.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Cytochrome P450 3A-dependent metabolism of a potent and selective gamma-aminobutyric acid Aalpha2/3 receptor agonist in vitro: involvement of cytochrome P450 3A5 displaying biphasic kinetics

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

GABA(A) receptor subtype selective cognition enhancers

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Which GABAA-receptor subtypes really occur in the brain?

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Techniques: Use of concatenated subunits for the study of ligand-gated ion channels.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Blockade of alcohol's amnestic activity in humans by an alpha5 subtype benzodiazepine receptor inverse agonist

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

GABA(A) receptors: immunocytochemical distribution of 13 subunits in the adult rat brain.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the alpha 5 subunit

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Different GABAA receptor subtypes mediate the anxiolytic, abuse-related, and motor effects of benzodiazepine-like drugs in primates

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Analysis of GABAA receptor function and dissection of the pharmacology of benzodiazepines and general anesthetics through mouse genetics

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Benzodiazepine actions mediated by specific gamma-aminobutyric acid(A) receptor subtypes.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Modulation of long-term potentiation in CA1 region of mouse hippocampal brain slices by GABAA receptor benzodiazepine site ligands.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Analysis of the set of GABA(A) receptor genes in the human genome.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

GABA(A) receptor subunits in the rat hippocampus I: immunocytochemical distribution of 13 subunits.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Delay-dependent impairment of a matching-to-place task with chronic and intrahippocampal infusion of the NMDA-antagonist D-AP5.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Autoradiographic localization of alpha5 subunit-containing GABAA receptors in rat brain

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

From the behavioral pharmacology of beta-carbolines to seizures, anxiety, and memory.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Benzodiazepine impairs and beta-carboline enhances performance in learning and memory tasks

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Genetic manipulations of GABAA receptor in mice make inhibition exciting.

1 reference

https://api.crossref.org/works/10.1111%2FJ.1755-5949.2007.00034.X

21 January 2018

Enhanced learning and memory and altered GABAergic synaptic transmission in mice lacking the alpha 5 subunit of the GABAA receptor.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A single histidine in GABAA receptors is essential for benzodiazepine agonist binding

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Issues in the clinical use of benzodiazepines: potency, withdrawal, and rebound.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

High-potency benzodiazepines: recent clinical results.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Contributions of GABAA receptor subtype selectivity to abuse liability and dependence potential of pharmacological treatments for anxiety and sleep disorders.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Characterization of the solubility of a poorly soluble hydroxylated metabolite in human urine and its implications for potential renal toxicity

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Metabolism and disposition of a potent and selective GABA-Aalpha2/3 receptor agonist in healthy male volunteers

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure, pharmacology, and function of GABAA receptor subtypes.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Benzodiazepines and human memory: a review.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes.

1 reference

https://pubmed.ncbi.nlm.nih.gov/18482097

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1111/J.1755-5949.2007.00034.X

1 reference

Europe PubMed Central

4 August 2017

1 reference

Europe PubMed Central

4 August 2017

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