(Q37709562)

22 August 2017

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title

Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023. (English)

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22 August 2017

John R Atack

1

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22 August 2017

publication date

27 November 2009

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22 August 2017

published in

Advances in Pharmacology

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22 August 2017

volume

57

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22 August 2017

page(s)

137-185

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Central benzodiazepine receptor occupancy by zolpidem in the human brain as assessed by positron emission tomography

22 August 2017

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7 January 2021

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.

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RO4938581, a novel cognitive enhancer acting at GABAA alpha5 subunit-containing receptors

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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

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7 January 2021

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

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7 January 2021

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

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7 January 2021

Trace fear conditioning involves hippocampal alpha5 GABA(A) receptors

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7 January 2021

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

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7 January 2021

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

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7 January 2021

Pharmacodynamic and pharmacokinetic effects of MK-0343, a GABA(A) alpha2,3 subtype selective agonist, compared to lorazepam and placebo in healthy male volunteers

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7 January 2021

Antipsychotic effects of bretazenil, a partial benzodiazepine agonist in acute schizophrenia--a study group report.

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7 January 2021

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

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7 January 2021

The sedative effects of CL 218,872, like those of chlordiazepoxide, are reversed by benzodiazepine antagonists

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7 January 2021

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

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7 January 2021

Changes of benzodiazepine receptors during chronic benzodiazepine administration in humans

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7 January 2021

Comparative single-dose kinetics and dynamics of lorazepam, alprazolam, prazepam, and placebo

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7 January 2021

Benzodiazepine self-administration in humans and laboratory animals--implications for problems of long-term use and abuse.

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7 January 2021

Tolerance to the anticonvulsant effect of benzodiazepines

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7 January 2021

Selective influence on contextual memory: physiochemical properties associated with selectivity of benzodiazepine ligands at GABAA receptors containing the alpha5 subunit.

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7 January 2021

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7 January 2021

Reversal of pathological pain through specific spinal GABAA receptor subtypes.

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7 January 2021

Genuine antihyperalgesia by systemic diazepam revealed by experiments in GABAA receptor point-mutated mice

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7 January 2021

Novel discriminative stimulus effects of TPA023B, subtype-selective gamma-aminobutyric-acid(A)/benzodiazepine modulator: comparisons with zolpidem, lorazepam, and TPA023

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7 January 2021

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7 January 2021

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7 January 2021

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7 January 2021

A proof-of-concept study using [11C]flumazenil PET to demonstrate that pagoclone is a partial agonist

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7 January 2021

Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator.

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7 January 2021

A synthetic non-benzodiazepine ligand for benzodiazepine receptors: A probe for investigating neuronal substrates of anxiety

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7 January 2021

Benzodiazepine receptors: Cellular and behavioral characteristics

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7 January 2021

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7 January 2021

Molecular and neuronal substrate for the selective attenuation of anxiety.

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7 January 2021

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

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7 January 2021

Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour.

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7 January 2021

A comparison between chlordiazepoxide and CL 218,872--a synthetic nonbenzodiazepine ligand for benzodiazepine receptors on spontaneous locomotor activity in rats

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7 January 2021

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

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7 January 2021

NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABAA receptor positive allosteric modulator: in vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy

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7 January 2021

Molecular regulation of cognitive functions and developmental plasticity: impact of GABAA receptors

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7 January 2021

Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflamm

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7 January 2021

The benzodiazepine receptor ligand CL218,872 has both anxiolytic and sedative properties in rodents

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7 January 2021

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7 January 2021

GABA A receptors: subtypes provide diversity of function and pharmacology

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7 January 2021

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

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7 January 2021

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

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7 January 2021

The anxioselective agent 7-(2-chloropyridin-4-yl)pyrazolo-[1,5-a]-pyrimidin-3-yl](pyridin-2-yl)methanone (DOV 51892) is more efficacious than diazepam at enhancing GABA-gated currents at alpha1 subunit-containing GABAA receptors

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7 January 2021

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

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7 January 2021

Diverse mechanisms of antiepileptic drugs in the development pipeline

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7 January 2021

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

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7 January 2021

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

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7 January 2021

GABA-based therapeutic approaches: GABAA receptor subtype functions

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7 January 2021

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

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7 January 2021

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.

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7 January 2021

Discovery of Imidazo[1,2-b][1,2,4]triazines as GABAAα2/3 Subtype Selective Agonists for the Treatment of Anxiety

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7 January 2021

Assembly of GABA(A) receptors (Review).

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7 January 2021

Are GABAA receptors containing alpha5 subunits contributing to the sedative properties of benzodiazepine site agonists?

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7 January 2021

Rodent pharmacokinetics and receptor occupancy of the GABAA receptor subtype selective benzodiazepine site ligand L-838417.

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7 January 2021

Detection of benzodiazepine receptor occupancy in the human brain by positron emission tomography

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7 January 2021

Structure, pharmacology, and function of GABAA receptor subtypes.

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7 January 2021

Subunit composition, distribution and function of GABA(A) receptor subtypes

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7 January 2021

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

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7 January 2021

Effect of alpha subunit on allosteric modulation of ion channel function in stably expressed human recombinant gamma-aminobutyric acid(A) receptors determined using (36)Cl ion flux.

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7 January 2021

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

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7 January 2021

The benzodiazepine story

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7 January 2021

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

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7 January 2021

In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-a partial agonist

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7 January 2021

Evaluation of the discriminative stimulus effects of the novel sedative-hypnotic CL 284,846

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7 January 2021

Pharmacokinetic and pharmacodynamic interactions of bretazenil and diazepam with alcohol

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7 January 2021

Genetic manipulations of GABAA receptor in mice make inhibition exciting.

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7 January 2021

Benzodiazepine receptor equilibrium constants for flumazenil and midazolam determined in humans with the single photon emission computer tomography tracer [123I]iomazenil.

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7 January 2021

Reciprocal alterations in pre- and postsynaptic inhibitory markers at chandelier cell inputs to pyramidal neurons in schizophrenia

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7 January 2021

Flumazenil: a new benzodiazepine antagonist

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7 January 2021

A risk-benefit assessment of flumazenil in the management of benzodiazepine overdose

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7 January 2021

The distribution of 13 GABAA receptor subunit mRNAs in the rat brain. I. Telencephalon, diencephalon, mesencephalon

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7 January 2021

High affinity ligands for ‘diazepam-insensitive’ benzodiazepine receptors

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7 January 2021

A schizophrenia-related sensorimotor deficit links alpha 3-containing GABAA receptors to a dopamine hyperfunction

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7 January 2021

10.1016/S1054-3589(08)57004-9

Identifiers

DOI

1 reference

22 August 2017

1 reference