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List of works by John Atack

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.

scientific article

3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.

scientific article

3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.

scientific article

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.

scientific article published on March 2004

6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.

scientific article

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

scientific article published on 01 November 2005

A Biophysical Approach to the Identification of Novel ApoE Chemical Probes

scientific article published on 29 January 2019

A neural tube defect specific form of acetylcholinesterase in amniotic fluid

scientific article published on 01 December 1983

A new pyridazine series of GABAA alpha5 ligands.

scientific article

Absence of biochemical heterogeneity in McArdle's disease. A high resolution SDS-polyacrylamide gel electrophoresis study

scientific article published on 01 March 1987

African trypanosomiasis: Synthesis & SAR enabling novel drug discovery of ubiquinol mimics for trypanosome alternative oxidase

scientific article

Alpha2-containing GABA(A) receptors are involved in mediating stimulant effects of cocaine.

scientific article

Aluminosilicates and senile plaque formation in Alzheimer's disease.

scientific article published in February 1986

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

scientific article

An inverse agonist selective for alpha5 subunit-containing GABAA receptors improves encoding and recall but not consolidation in the Morris water maze.

scientific article

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

scientific article

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

scientific article (publication date: August 2003)

Bilateral changes in neocortical [3H]pirenzepine and [3H]oxotremorine-M binding following unilateral lesions of the rat nucleus basalis magnocellularis: an autoradiographic study

scientific article published on 01 April 1989

Carbamate analogues of (-)-physostigmine: in vitro inhibition of acetyl- and butyrylcholinesterase

scientific article published on 01 July 1988

Cell surface expression of the human N-methyl-D-aspartate receptor subunit 1a requires the co-expression of the NR2A subunit in transfected cells.

scientific article published on February 1996

Cerebrospinal fluid cholinesterases in aging and in dementia of the Alzheimer type

scientific article published on 01 February 1988

Cerebrospinal fluid inositol monophosphatase: elevated activity in depression and neuroleptic-treated schizophrenia

scientific article published on 01 September 1998

Cerebrospinal fluid neurochemistry in the myoclonic subtype of Alzheimer's disease

scientific article published on 01 November 1988

Cerebrospinal fluid production is normal in Down syndrome ⬇️

scientific article published on July 1, 1998

Changes in [3H]zolpidem and [3H]Ro 15-1788 binding in rat globus pallidus and substantia nigra pars reticulata following a nigrostriatal tract lesion

scientific article published on 01 April 2000

Characterization of [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding to GABAA receptors in postmortem human brain

scientific article

Characterization of inositol monophosphatase in human cerebrospinal fluid.

scientific article published in June 1993

Characterization of the effects of lithium on phosphatidylinositol (PI) cycle activity in human muscarinic m1 receptor-transfected CHO cells.

scientific article

Cholinergic correlates of cognitive impairment in Parkinson's disease: comparisons with Alzheimer's disease.

scientific article published on May 1985

Co-crystallization of human inositol monophosphatase with the lithium mimetic L-690,330

scientific article published on 02 October 2018

Cocaine effects on mouse incentive-learning and human addiction are linked to alpha2 subunit-containing GABAA receptors

scientific article

Combining Sanford Arylations on Benzodiazepines with the Nuisance Effect

scientific article published on 02 August 2017

Comparison of lorazepam [7-chloro-5-(2-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one] occupancy of rat brain gamma-aminobutyric acid(A) receptors measured using in vivo [3H]flumazenil (8-fluoro 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[

scientific article published on 12 December 2006

Contribution of GABAA receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys ⬇️

scientific article published on December 30, 2010

Contribution of specific binding to the central benzodiazepine site to the brain concentrations of two novel benzodiazepine site ligands.

scientific article published in September 2007

Crystallization and structure of ebselen bound to Cys141 of human inositol monophosphatase

scientific article published on 15 September 2020

Decreased CSF inositol monophosphatase activity after lithium treatment.

scientific article published in July 1994

Detection of gender differences in rat lens proteins using 2-D-DIGE.

scientific article published on January 2006

Development of an oligonucleotide-based fluorescence assay for the identification of tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors.

scientific article

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

scientific article

Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands.

scientific article

Differential expression of cytochrome oxidase (COX) genes in different regions of monkey brain

scientific article published on July 1, 1992

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

article

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.

scientific article

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

scientific article

GABA(A) Receptor Subtypes: Novel Targets for Novel Medicines

scientific article published on 18 April 2012

GABAA Receptor Subtype-Selective Modulators. II. α5-Selective Inverse Agonists for Cognition Enhancement ⬇️

scientific article published on January 1, 2011

GABAA Receptor α2/α3 Subtype-Selective Modulators as Potential Nonsedating Anxiolytics ⬇️

scientific article published on January 1, 2010

GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.

scientific article published on January 2011

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

scientific article published on May 22, 2003

Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135)

scientific article published on 27 May 2008

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

scientific article published on 27 December 2005

Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

scientific article published on 4 January 2006

In vitro and in vivo inhibition of inositol monophosphatase by the bisphosphonate L-690,330.

scientific article

In vitro and in vivo inhibition of prolyl endopeptidase ⬇️

scientific article published on November 26, 1991

In vitro and in vivo properties of 3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)-pyrazolo[1,5-d]-[1,2,4]triazine (MRK-016), a GABAA receptor alpha5 subtype-selective inverse agonist.

scientific article published on 24 August 2009

In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.

scientific article published on 27 January 2006

In vivo labelling of alpha5 subunit-containing GABA(A) receptors using the selective radioligand [(3)H]L-655,708.

scientific article published on 26 April 2005

Inositol monophosphatase inhibitors: A novel treatment for bipolar disorder? ⬇️

scientific article published on 01 June 1995

Inositol monophosphatase, the putative therapeutic target for lithium

scientific article published on 01 August 1996

Interaction of 9-amino-1,2,3,4-tetrahydroaminoacridine (THA) with human cortical nicotinic and muscarinic receptor binding in vitro

scientific article published on 01 August 1988

Intralaminar Neurochemical Distributions in Human Midtemporal Cortex: Comparison Between Alzheimer's Disease and the Normal ⬇️

scientific article published on May 1, 1984

JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease

scientific article published on 24 September 2014

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

scientific article

Lipophilic nalmefene prodrugs to achieve a one-month sustained release.

scientific article

Lumbar cerebrospinal fluid choline in healthy aging and in Down's syndrome.

scientific article published in September 1990

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

scientific article published on 10 February 2010

Mechanism of inositol monophosphatase, the putative target of lithium therapy

scientific article

Mode of action of DNA-competitive small molecule inhibitors of tyrosyl DNA phosphodiesterase 2.

scientific article published on 20 April 2016

Molecular blueprint of allosteric binding sites in a homologue of the agonist-binding domain of the α7 nicotinic acetylcholine receptor.

scientific article published on 27 April 2015

Molecular forms of acetylcholinesterase and butyrylcholinesterase in human plasma and cerebrospinal fluid

scientific article published on 01 June 1987

Molecular forms of butyrylcholinesterase in the human neocortex during development and degeneration of the cortical cholinergic system.

scientific article published in June 1987

Neural tube defect-specific acetylcholinesterase: its properties and quantitation in the detection of anencephaly and spina bifida

scientific article published on 01 November 1987

Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.

scientific article published on 20 March 2010

Pharmacokinetics and metabolism studies on (3-tert-butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy) pyrazolo[1,5-d][1,2,4]triazine, a functionally selective GABA(A) alpha5 inverse agonist for cognitive dysfunction.

scientific article

Pharmacological characterisation of MDI-222, a novel AMPA receptor positive allosteric modulator with an improved safety profile

scientific article published on 26 November 2019

Plasma and erythrocyte acetylcholinesterase in senile dementia of Alzheimer type.

scientific article published in January 1982

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.

scientific article

Preclinical and clinical pharmacology of the GABAA receptor alpha5 subtype-selective inverse agonist alpha5IA.

scientific article published on 19 September 2009

Probing the role of metal ions in the mechanism of inositol monophosphatase by site-directed mutagenesis

scientific article published on 01 October 1993

Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro

scientific article published on 2 March 2005

R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization.

scientific article published on 2 July 2007

Rat and human hippocampal alpha5 subunit-containing gamma-aminobutyric AcidA receptors have alpha5 beta3 gamma2 pharmacological characteristics.

scientific article published in November 1998

Rat pharmacokinetics and pharmacodynamics of a sustained release formulation of the GABAA alpha5-selective compound L-655,708.

scientific article published on 2 February 2006

Reducing abuse liability of GABAA/benzodiazepine ligands via selective partial agonist efficacy at alpha1 and alpha2/3 subtypes

scientific article

Regional analysis of rat brain proteins during senescence

scientific article published on 01 January 1987

Regional differences in the inhibition of mouse in vivo [3H]Ro 15-1788 binding reflect selectivity for alpha 1 versus alpha 2 and alpha 3 subunit-containing GABAA receptors.

scientific article published in March 1999

Regional specificity of membrane instability in Alzheimer's disease brain.

scientific article published in July 1993

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

scientific article published in January 2005

Role of GABAA alpha5-containing receptors in ethanol reward: the effects of targeted gene deletion, and a selective inverse agonist

scientific article

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

scientific article

Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents.

scientific article

Selective labelling of diazepam-insensitive GABAA receptors in vivo using [3H]Ro 15-4513

scientific article

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

scientific article

Structure and mechanism of inositol monophosphatase.

scientific article published on March 1995

Structure of inositol monophosphatase, the putative target of lithium therapy ⬇️

scientific article published on November 1, 1992

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

scientific article

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.

scientific article

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.

scientific article

The 5HT(1B) receptor agonist, CP-93129, inhibits [(3)H]-GABA release from rat globus pallidus slices and reverses akinesia following intrapallidal injection in the reserpine-treated rat

scientific article

The X-ray structure of human calbindin-D28K: an improved model

article

The characterisation of molecular forms of acetylcholinesterase in Hirschsprung's disease ⬇️

scientific article published on February 15, 1988

The complexity of the GABAA receptor shapes unique pharmacological profiles.

scientific article published on 02 July 2009

The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor

scientific article published on 18 July 2011

The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone

scientific article

The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.

scientific article published on 10 November 2006

The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates

scientific article published on 30 April 2009

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

scientific article published on 19 May 2006

Tyrosine 121 moves revealing a ligandable pocket that couples catalysis to ATP-binding in serine racemase

scientific article published on 11 April 2022

cDNA cloning of human and rat brain myo-inositol monophosphatase. Expression and characterization of the human recombinant enzyme ⬇️

scientific article published on June 15, 1992

pp60c-src Kinase expression in brain of adult rats in relation to age ⬇️

scientific article published on January 1, 1990

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