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John Atack

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Devin M Swanson; Victoria D Wong; John R Atack; Pascal Bonaventure; Curt A Dvorak; Lisa K Dvorak; JIll Jablonowski; Timothy W Lovenberg; Kirsten Morton; Diane Nepomuceno; Dale A Rudolph; Mark Seierstad; Chandra Shah; Nicholas I Carruthers
The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.
John R Atack; D J Hallett; S Tye; Keith A Wafford; C Ryan; S M Sanabria-Bohórquez; Wai-Si Eng; R E Gibson; H Donald Burns; Gerard R Dawson; R W Carling; Leslie J Street; Andrew Pike; I De Lepeleire; K Van Laere; G Bormans; J N de Hoon; A Van Hecken; Ruth M McKernan; M G Murphy; Richard Hargreaves
Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.
John R Atack; Keith A Wafford; Leslie J Street; Gerard R Dawson; S Tye; K Van Laere; G Bormans; S M Sanabria-Bohórquez; I De Lepeleire; J N de Hoon; A Van Hecken; H D Burns; Ruth M McKernan; M G Murphy; Richard Hargreaves
MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

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All Publications

2011: Devin M Swanson; Victoria D Wong; John R Atack; Pascal Bonaventure; Curt A Dvorak; Lisa K Dvorak; JIll Jablonowski; Timothy W Lovenberg; Kirsten Morton; Diane Nepomuceno; Dale A Rudolph; Mark Seierstad; Chandra Shah; Nicholas I Carruthers
The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor.
Bioorganic & medicinal chemistry letters 2011;21(18):5552-6.
2011: John R Atack; D J Hallett; S Tye; Keith A Wafford; C Ryan; S M Sanabria-Bohórquez; Wai-Si Eng; R E Gibson; H Donald Burns; Gerard R Dawson; R W Carling; Leslie J Street; Andrew Pike; I De Lepeleire; K Van Laere; G Bormans; J N de Hoon; A Van Hecken; Ruth M McKernan; M G Murphy; Richard Hargreaves
Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.
Journal of psychopharmacology (Oxford, England) 2011;25(3):329-44.
2011: John R Atack; Keith A Wafford; Leslie J Street; Gerard R Dawson; S Tye; K Van Laere; G Bormans; S M Sanabria-Bohórquez; I De Lepeleire; J N de Hoon; A Van Hecken; H D Burns; Ruth M McKernan; M G Murphy; Richard Hargreaves
MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.
Journal of psychopharmacology (Oxford, England) 2011;25(3):314-28.
2010: Michael A Letavic; Leah Aluisio; John R Atack; Pascal Bonaventure; Nicholas I Carruthers; Christine Dugovic; Anita Everson; Mark A Feinstein; Ian C Fraser; Kenway Hoey; Xiaohui Jiang; John M Keith; Tatiana Koudriakova; Perry Leung; Brian Lord; Timothy W Lovenberg; Kiev S Ly; Kirsten L Morton; S Timothy Motley; Diane Nepomuceno; Michele Rizzolio; Raymond Rynberg; Kia Sepassi; Jonathan Shelton
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Bioorganic & medicinal chemistry letters 2010;20(14):4210-4.
2010: Emily M Stocking; Leah Aluisio; John R Atack; Pascal Bonaventure; Nicholas I Carruthers; Christine Dugovic; Anita Everson; Ian Fraser; Xiaohui Jiang; Perry Leung; Brian Lord; Kiev S Ly; Kirsten L Morton; Diane Nepomuceno; Chandravadan R Shah; Jonathan Shelton; Akinola Soyode-Johnson; Michael A Letavic
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
Bioorganic & medicinal chemistry letters 2010;20(9):2755-60.
2010: Claire I Dixon; Hannah V Morris; Gerome Breen; Sylvane Desrivieres; Sarah Jugurnauth; Rebecca C Steiner; Homero Vallada; Camila Guindalini; ronaldo laranjeira; Guilherme Messas; Thomas W Rosahl; John R Atack; Dianne R Peden; Delia Belelli; Jeremy J Lambert; Sarah L King; Gunter Schumann; Dai stephens
Cocaine effects on mouse incentive-learning and human addiction are linked to alpha2 subunit-containing GABAA receptors.
Proceedings of the National Academy of Sciences of the United States of America 2010;107(5):2289-94.
2010: James R Shoblock; Natalie Welty; Diane Nepomuceno; Brian Lord; Leah Aluisio; Ian Fraser; S Timothy Motley; Steve W Sutton; Kirsten Morton; Ruggero Galici; John R Atack; Lisa Dvorak; Devin M Swanson; Nicholas I Carruthers; Curt Dvorak; Timothy W Lovenberg; Pascal Bonaventure
In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor.
Psychopharmacology 2010;208(2):265-77.
2010: John R Atack; Dean F Wong; Tim D Fryer; Christine Ryan; Sandra Sanabria; Yun Zhou; Robert F Dannals; Wai-si Eng; Raymond E Gibson; H Donald Burns; Jose M Vega; Laura Vessy; Paul Scott-Stevens; John S Beech; Jean-Claude Baron; Bindi Sohal; Michael L Schrag; Franklin I Aigbirhio; Ruth M McKernan; Richard Hargreaves
Benzodiazepine binding site occupancy by the novel GABAA receptor subtype-selective drug 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 (TPA023) in rats, primates, and humans.
The Journal of pharmacology and experimental therapeutics 2010;332(1):17-25.
2009: John R Atack; Wai-Si Eng; Ray E Gibson; Christine Ryan; Barbara Francis; Bindi Sohal; Gerard R Dawson; Richard Hargreaves; H Donald Burns
The plasma-occupancy relationship of the novel GABAA receptor benzodiazepine site ligand, alpha5IA, is similar in rats and primates.
British journal of pharmacology 2009;157(5):796-803.
2008: Jessica Zhu; Chester Kuei; Steven Sutton; Fredrik Kamme; Jingxue Yu; Pascal Bonaventure; John R Atack; Timothy W Lovenberg; Changlu Liu
Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135).
European journal of pharmacology 2008;590(1-3):43-52.
2008: Koen Van Laere; Guy Bormans; Sandra Sanabria; Tjibbe de Groot; Patrick Dupont; Inge De Lepeleire; Jan de Hoon; Luc Mortelmans; Richard Hargreaves; John R Atack; H Donald Burns
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.
Biological psychiatry 2008;64(2):153-61.
2008: H V Morris; Gerard R Dawson; David S Reynolds; John R Atack; T W Rosahl; Dai stephens
Alpha2-containing GABA(A) receptors are involved in mediating stimulant effects of cocaine.
Pharmacology, biochemistry, and behavior 2008;90(1):9-18.
2008: Ruggero Galici; Jamin D Boggs; Kirsten L Miller; Pascal Bonaventure; John R Atack
Effects of SB-269970, a 5-HT7 receptor antagonist, in mouse models predictive of antipsychotic-like activity.
Behavioural pharmacology 2008;19(2):153-9.
2008: John R Atack
GABA(A) receptor subtype-selective efficacy: TPA023, an alpha2/alpha3 selective non-sedating anxiolytic and alpha5IA, an alpha5 selective cognition enhancer.
CNS neuroscience & therapeutics 2008;14(1):25-35.
2007: Andrew Pike; Susan M Cook; Alan P Watt; Paul Scott-Stevens; Thomas W Rosahl; Ruth M McKernan; Luanda Pym; Alec Guiblin; Christopher Moyes; Bindi Sohal; John R Atack
Contribution of specific binding to the central benzodiazepine site to the brain concentrations of two novel benzodiazepine site ligands.
Biopharmaceutics & drug disposition 2007;28(6):275-82.
2007: Rosa L Fradley; Martin R Guscott; Sharlene Bull; David J Hallett; Simon C Goodacre; Keith A Wafford; Elizabeth M Garrett; Richard J Newman; Gillian F O'Meara; Paul J Whiting; Thomas W Rosahl; Gerard R Dawson; David S Reynolds; John R Atack
Differential contribution of GABA(A) receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands.
Journal of psychopharmacology (Oxford, England) 2007;21(4):384-91.
2007: John R Atack; Y Ohashi; Ruth M McKernan
Characterization of [35S]t-butylbicyclophosphorothionate ([35S]TBPS) binding to GABAA receptors in postmortem human brain.
British journal of pharmacology 2007;150(8):1066-74.
2007: John R Atack; Paul Scott-Stevens; John S Beech; Tim D Fryer; Jessica L Hughes; Marcel C Cleij; Jean-Claude Baron; John C Clark; Richard Hargreaves; Franklin I Aigbirhio
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[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester) binding and [11C]flumazenil micro-positron emission tomography.
The Journal of pharmacology and experimental therapeutics 2007;320(3):1030-7.
2007: Jonathan D Best; David W Smith; Michael A Reilly; Ruth O'Donnell; Huw D Lewis; Semantha Ellis; Neil Wilkie; Thomas W Rosahl; Philippe Laroque; Christine Boussiquet-Leroux; Ian Churcher; John R Atack; Timothy Harrison; Mark S Shearman
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.
The Journal of pharmacology and experimental therapeutics 2007;320(2):552-8.
2006: John R Atack; Peter J Bayley; Guy R Seabrook; Keith A Wafford; Ruth M McKernan; Gerard R Dawson
L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for alpha5-containing GABAA receptors.
Neuropharmacology 2006;51(6):1023-9.
2006: Neil Collinson; John R Atack; P Laughton; Gerard R Dawson; Dai stephens
An inverse agonist selective for alpha5 subunit-containing GABAA receptors improves encoding and recall but not consolidation in the Morris water maze.
Psychopharmacology 2006;188(4):619-28.
2006: Julian L Goggi; Huw D Lewis; Joanie Mok; Timothy Harrison; Mark S Shearman; John R Atack; Jonathan D Best
A comparative assessment of gamma-secretase activity in transgenic and non-transgenic rodent brain.
Journal of neuroscience methods 2006;157(2):246-52.
2006: John R Atack; Peter J Bayley; Stephen R Fletcher; Ruth M McKernan; Keith A Wafford; Gerard R Dawson
The proconvulsant effects of the GABAA alpha5 subtype-selective compound RY-080 may not be alpha5-mediated.
European journal of pharmacology 2006;548(1-3):77-82.
2006: Jennifer Li; Rebecca L Fish; Susan M Cook; F David Tattersall; John R Atack
Comparison of in vivo and ex vivo [3H]flumazenil binding assays to determine occupancy at the benzodiazepine binding site of rat brain GABAA receptors.
Neuropharmacology 2006;51(1):168-72.
2006: Robert W Carling; Michael G N Russell; Kevin W Moore; Andrew Mitchinson; Alec Guiblin; Alison Smith; Keith A Wafford; George Marshall; John R Atack; Leslie J Street
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Bioorganic & medicinal chemistry letters 2006;16(13):3550-4.
2006: H V Morris; Gerard R Dawson; David S Reynolds; John R Atack; Dai stephens
Both alpha2 and alpha3 GABAA receptor subtypes mediate the anxiolytic properties of benzodiazepine site ligands in the conditioned emotional response paradigm.
The European journal of neuroscience 2006;23(9):2495-504.
2006: John R Atack; Andrew Pike; Ashley Clarke; Susan M Cook; Bindi Sohal; Ruth M McKernan; Gerard R Dawson
Rat pharmacokinetics and pharmacodynamics of a sustained release formulation of the GABAA alpha5-selective compound L-655,708.
Drug metabolism and disposition: the biological fate of chemicals 2006;34(5):887-93.
2006: Jonathan D Best; Mark T Jay; Otu Franklin; Ian Churcher; Michael Reilly; Pablo Morentin-Gutierrez; Christine Pattison; Timothy Harrison; Mark S Shearman; John R Atack
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.
The Journal of pharmacology and experimental therapeutics 2006;317(2):786-90.
2006: John R Atack; Andrew Pike; George Marshall; Joanna Stanley; Rachael Lincoln; Susan M Cook; Richard T Lewis; Wesley P Blackaby; Simon C Goodacre; Ruth M McKernan; Gerard R Dawson; Keith A Wafford; David S Reynolds
The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone.
Neuropharmacology 2006;50(6):677-89.
2006: Richard T Lewis; Wesley P Blackaby; Timothy Blackburn; Andrew S R Jennings; Andrew Pike; Rowan A Wilson; David J Hallett; Susan M Cook; Pushpinder Ferris; George R Marshall; David S Reynolds; Wayne F A Sheppard; Alison J Smith; Bindi Sohal; Joanna Stanley; Spencer J Tye; Keith A Wafford; John R Atack
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Journal of medicinal chemistry 2006;49(8):2600-10.
2006: Andrew S R Jennings; Richard T Lewis; Michael G N Russell; David J Hallett; Leslie J Street; José L Castro; John R Atack; Susan M Cook; Rachael Lincoln; Joanna Stanley; Alison J Smith; David S Reynolds; Bindi Sohal; Andrew Pike; George R Marshall; Keith A Wafford; Wayne F A Sheppard; Spencer J Tye
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Bioorganic & medicinal chemistry letters 2006;16(6):1477-80.
2006: Simon C Goodacre; David J Hallett; Robert W Carling; José L Castro; David S Reynolds; Andrew Pike; Keith A Wafford; Robert Newman; John R Atack; Leslie J Street
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.
Bioorganic & medicinal chemistry letters 2006;16(6):1582-5.
2006: Wesley P Blackaby; John R Atack; Frances A Bromidge; José L Castro; Simon C Goodacre; David J Hallett; Richard T Lewis; George R Marshall; Andrew Pike; Alison J Smith; Leslie J Street; David F D Tattersall; Keith A Wafford
Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Bioorganic & medicinal chemistry letters 2006;16(5):1175-9.
2006: Gerard R Dawson; Karen A Maubach; Neil Collinson; M Cobain; Barry J Everitt; Angus M MacLeod; Hedaythul I Choudhury; Louise McDonald; Gopalan V Pillai; Wayne Rycroft; Alison J Smith; Francine Sternfeld; F David Tattersall; Keith A Wafford; David S Reynolds; Guy R Seabrook; John R Atack
An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.
The Journal of pharmacology and experimental therapeutics 2006;316(3):1335-45.
2006: Michael G N Russell; Robert W Carling; Leslie J Street; David J Hallett; Simon C Goodacre; Elena Mezzogori; Michael Reader; Susan M Cook; Frances A Bromidge; Robert Newman; Alison J Smith; Keith A Wafford; George R Marshall; David S Reynolds; Rebecca Dias; Pushpinder Ferris; Joanna Stanley; Rachael Lincoln; Spencer J Tye; Wayne F A Sheppard; Bindi Sohal; Andrew Pike; Maria Dominguez; John R Atack; José L Castro
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.
Journal of medicinal chemistry 2006;49(4):1235-8.
2006: Philip Jones; John R Atack; Matthew P Braun; Brian P Cato; Mark S Chambers; desmond oconnor; Susan M Cook; Sarah C Hobbs; Robert Maxey; Helen J Szekeres; Nicola Szeto; Keith A Wafford; Angus M MacLeod
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.
Bioorganic & medicinal chemistry letters 2006;16(4):872-5.
2006: Simon C Goodacre; Leslie J Street; David J Hallett; James Crawforth; Sarah Kelly; Andrew P Owens; Wesley P Blackaby; Richard T Lewis; Joanna Stanley; Alison J Smith; Pushpinder Ferris; Bindi Sohal; Susan M Cook; Andrew Pike; Nicola Brown; Keith A Wafford; George Marshall; José L Castro; John R Atack
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
Journal of medicinal chemistry 2006;49(1):35-8.
2006: Paul C Guest; Heather A Skynner; Kamran Salim; F David Tattersall; Michael R Knowles; John R Atack
Detection of gender differences in rat lens proteins using 2-D-DIGE.
Proteomics 2006;6(2):667-76.
2006: John R Atack; Keith A Wafford; Spencer J Tye; Susan M Cook; Bindi Sohal; Andrew Pike; Cyrille Sur; David Melillo; Linda J Bristow; Frances A Bromidge; Ian Ragan; Julie Kerby; Leslie J Street; Robert W Carling; José L Castro; Paul Whiting; Gerard R Dawson; Ruth M McKernan
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.
The Journal of pharmacology and experimental therapeutics 2006;316(1):410-22.
2005: Dai stephens; Jana Pistovcakova; Lynn Worthing; John R Atack; Gerard R Dawson
Role of GABAA alpha5-containing receptors in ethanol reward: the effects of targeted gene deletion, and a selective inverse agonist.
European journal of pharmacology 2005;526(1-3):240-50.
2005: Robert W Carling; Andrew Madin; Alec Guiblin; Michael G N Russell; Kevin W Moore; Andrew Mitchinson; Bindi Sohal; Andrew Pike; Susan M Cook; Ian C Ragan; Ruth M McKernan; Kathleen Quirk; Pushpinder Ferris; George Marshall; Sally-Anne Thompson; Keith A Wafford; Gerard R Dawson; John R Atack; Timothy Harrison; José L Castro; Leslie J Street
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 activity but is not sedating in animal models.
Journal of medicinal chemistry 2005;48(23):7089-92.
2005: Rebecca Dias; Wayne F A Sheppard; Rosa L Fradley; Elizabeth M Garrett; Joanna L Stanley; Spencer J Tye; Simon C Goodacre; Rachael Lincoln; Susan M Cook; Rachel Conley; David J Hallett; Alexander C Humphries; Sally-Anne Thompson; Keith A Wafford; Leslie J Street; José L Castro; Paul J Whiting; Thomas W Rosahl; John R Atack; Ruth M McKernan; Gerard R Dawson; David S Reynolds
Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2005;25(46):10682-8.
2005: Wesley P Blackaby; John R Atack; Frances A Bromidge; Richard Lewis; Michael G N Russell; Alison Smith; Keith A Wafford; Ruth M McKernan; Leslie J Street; José L Castro
Pyrazolopyridinones as functionally selective GABAA ligands.
Bioorganic & medicinal chemistry letters 2005;15(22):4998-5002.
2005: Luanda Pym; Susan M Cook; Thomas W Rosahl; Ruth M McKernan; John R Atack
Selective labelling of diazepam-insensitive GABAA receptors in vivo using [3H]Ro 15-4513.
British journal of pharmacology 2005;146(6):817-25.
2005: Monique B van Niel; Kevin Wilson; Charles H Adkins; John R Atack; José L Castro; Dawn E Clarke; Stephen Fletcher; Ute Gerhard; Mark M Mackey; Sallie Malpas; Karen A Maubach; Robert Newman; desmond oconnor; Gopalan V Pillai; Peter B Simpson; Steven R Thomas; Angus M MacLeod
A new pyridazine series of GABAA alpha5 ligands.
Journal of medicinal chemistry 2005;48(19):6004-11.
2005: John R Atack; Luanda Alder; Susan M Cook; Alison J Smith; Ruth M McKernan
In vivo labelling of alpha5 subunit-containing GABA(A) receptors using the selective radioligand [(3)H]L-655,708.
Neuropharmacology 2005;49(2):220-9.
2005: John R Atack
The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics.
Expert opinion on investigational drugs 2005;14(5):601-18.
2005: Jonathan D Best; Mark T Jay; Otu Franklin; Jerome Ma; Alan Nadin; Semantha Ellis; Huw D Lewis; Christine Pattison; Michael Reilly; Timothy Harrison; Mark S Shearman; Toni L Williamson; John R Atack
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-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
The Journal of pharmacology and experimental therapeutics 2005;313(2):902-8.
2005: Michael G N Russell; Robert W Carling; John R Atack; Frances A Bromidge; Susan M Cook; Peter Hunt; Catherine Isted; Matt Lucas; Ruth M McKernan; Andrew Mitchinson; Kevin W Moore; Robert Narquizian; Alison Macaulay; David Thomas; Sally-Anne Thompson; Keith A Wafford; José L Castro
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.
Journal of medicinal chemistry 2005;48(5):1367-83.
2005: John R Atack; Peter H Hutson; Neil Collinson; George Marshall; Graham Bentley; Christopher Moyes; Susan M Cook; Ian Collins; Keith A Wafford; Ruth M McKernan; Gerard R Dawson
Anxiogenic properties of an inverse agonist selective for alpha3 subunit-containing GABA A receptors.
British journal of pharmacology 2005;144(3):357-66.
2005: Gerard R Dawson; Neil Collinson; John R Atack
Development of subtype selective GABAA modulators.
CNS spectrums 2005;10(1):21-7.
2005: Paul Scott-Stevens; John R Atack; Bindi Sohal; P Worboys
Rodent pharmacokinetics and receptor occupancy of the GABAA receptor subtype selective benzodiazepine site ligand L-838417.
Biopharmaceutics & drug disposition 2005;26(1):13-20.
2004: Mark S Chambers; John R Atack; Robert W Carling; Neil Collinson; Susan M Cook; Gerard R Dawson; Pushpinder Ferris; Sarah C Hobbs; desmond oconnor; George Marshall; Wayne Rycroft; Angus M MacLeod
An orally bioavailable, functionally selective inverse agonist at the benzodiazepine site of GABAA alpha5 receptors with cognition enhancing properties.
Journal of medicinal chemistry 2004;47(24):5829-32.
2004: Andrew Mitchinson; John R Atack; Peter Blurton; Robert W Carling; José L Castro; Karen S Curley; Michael G N Russell; George Marshall; Ruth M McKernan; Kevin W Moore; Robert Narquizian; Alison Smith; Leslie J Street; Sally-Anne Thompson; Keith A Wafford
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.
Bioorganic & medicinal chemistry letters 2004;14(13):3441-4.
2004: Leslie J Street; Francine Sternfeld; Richard A Jelley; Austin J Reeve; Robert W Carling; Kevin W Moore; Ruth M McKernan; Bindi Sohal; Susan Cook; Andrew Pike; Gerard R Dawson; Frances A Bromidge; Keith A Wafford; Guy R Seabrook; Sally-Anne Thompson; George Marshall; Gopalan V Pillai; José L Castro; John R Atack; Angus M MacLeod
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.
Journal of medicinal chemistry 2004;47(14):3642-57.
2004: Helen J Szekeres; John R Atack; Mark S Chambers; Susan M Cook; Alison Macaulay; Gopalan V Pillai; Angus M MacLeod
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Bioorganic & medicinal chemistry letters 2004;14(11):2871-5.
2004: Francine Sternfeld; Robert W Carling; Richard A Jelley; Tammy Ladduwahetty; Kevin J Merchant; Kevin W Moore; Austin J Reeve; Leslie J Street; desmond oconnor; Bindi Sohal; John R Atack; Susan Cook; Guy R Seabrook; Keith A Wafford; F David Tattersall; Neil Collinson; Gerard R Dawson; José L Castro; Angus M MacLeod
Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.
Journal of medicinal chemistry 2004;47(9):2176-9.
2004: James Crawforth; John R Atack; Susan M Cook; Karl R Gibson; Alan Nadin; Andrew P Owens; Andrew Pike; Michael Rowley; Alison J Smith; Bindi Sohal; Francine Sternfeld; Keith A Wafford; Leslie J Street
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
Bioorganic & medicinal chemistry letters 2004;14(7):1679-82.
2004: Robert W Carling; Kevin W Moore; Leslie J Street; Deborah Wild; Catherine Isted; Paul D Leeson; Steven Thomas; desmond oconnor; Ruth M McKernan; Kathleen Quirk; Susan M Cook; John R Atack; Keith A Wafford; Sally-Anne Thompson; Gerard R Dawson; Pushpinder Ferris; José L Castro
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.
Journal of medicinal chemistry 2004;47(7):1807-22.
2004: Ciara McCabe; David Shaw; John R Atack; Leslie J Street; Keith A Wafford; Gerard R Dawson; David S Reynolds; Julian C Leslie
Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour.
Neuropharmacology 2004;46(2):171-8.
2003: David S Reynolds; Thomas W Rosahl; Jennifer Cirone; Gillian F O'Meara; Alison Haythornthwaite; Richard J Newman; Janice Myers; Cyrille Sur; Owain Howell; A Richard Rutter; John R Atack; Alison Macaulay; Karen L Hadingham; Peter H Hutson; Delia Belelli; Jeremy J Lambert; Gerard R Dawson; Ruth M McKernan; Paul J Whiting; Keith A Wafford
Sedation and anesthesia mediated by distinct GABA(A) receptor isoforms.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2003;23(24):8608-17.
2003: John R Atack
Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site.
Current drug targets. CNS and neurological disorders 2003;2(4):213-32.
2003: Mark S Chambers; John R Atack; Howard B Broughton; Neil Collinson; Susan Cook; Gerard R Dawson; Sarah C Hobbs; George Marshall; Karen A Maubach; Gopalan V Pillai; Austin J Reeve; Angus M MacLeod
Identification of a novel, selective GABA(A) alpha5 receptor inverse agonist which enhances cognition.
Journal of medicinal chemistry 2003;46(11):2227-40.
2003: David S Reynolds; Gillian F O'Meara; Richard J Newman; Frances A Bromidge; John R Atack; Paul J Whiting; Thomas W Rosahl; Gerard R Dawson
GABA(A) alpha 1 subunit knock-out mice do not show a hyperlocomotor response following amphetamine or cocaine treatment.
Neuropharmacology 2003;44(2):190-8.
2002: Neil Collinson; Frederick M Kuenzi; Wolfgang Jarolimek; Karen A Maubach; Rosa Cothliff; Cyrille Sur; Alison Smith; Otu Franklin; Owain Howell; John R Atack; Ruth M McKernan; Guy R Seabrook; Gerard R Dawson; Paul J Whiting; Thomas W Rosahl
Enhanced learning and memory and altered GABAergic synaptic transmission in mice lacking the alpha 5 subunit of the GABAA receptor.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2002;22(13):5572-80.
2002: John R Atack; Mark B Schapiro
Inositol monophosphatase activity in normal, Down syndrome and dementia of the Alzheimer type CSF.
Neurobiology of aging 2002;23(3):389-96.
2002: Ian Collins; Christopher Moyes; William B Davey; Michael Rowley; Frances A Bromidge; Kathleen Quirk; John R Atack; Ruth M McKernan; Sally-Anne Thompson; Keith A Wafford; Gerard R Dawson; Andrew Pike; Bindi Sohal; Nancy N Tsou; Richard G Ball; José L Castro
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Journal of medicinal chemistry 2002;45(9):1887-900.
2002: Mark S Chambers; John R Atack; Frances A Bromidge; Howard B Broughton; Susan Cook; Gerard R Dawson; Sarah C Hobbs; Karen A Maubach; Austin J Reeve; Guy R Seabrook; Keith A Wafford; Angus M MacLeod
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
Journal of medicinal chemistry 2002;45(6):1176-9.
2002: M D Kelly; A Smith; G Banks; Peter B Wingrove; P W Whiting; John R Atack; Guy R Seabrook; Karen A Maubach
Role of the histidine residue at position 105 in the human alpha 5 containing GABA(A) receptor on the affinity and efficacy of benzodiazepine site ligands.
British journal of pharmacology 2002;135(1):248-56.
2001: Cyrille Sur; Keith A Wafford; David S Reynolds; Karen L Hadingham; Frances A Bromidge; Alison Macaulay; Neil Collinson; Gillian F O'Meara; Owain Howell; Robert Newman; Janice Myers; John R Atack; Gerard R Dawson; Ruth M McKernan; Paul J Whiting; Thomas W Rosahl
Loss of the major GABA(A) receptor subtype in the brain is not lethal in mice.
The Journal of neuroscience : the official journal of the Society for Neuroscience 2001;21(10):3409-18.
2001: Alison J Smith; L Alder; Jonathan Silk; Charles H Adkins; A E Fletcher; T Scales; Julie Kerby; George Marshall; Keith A Wafford; Ruth M McKernan; John R Atack
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.
Molecular pharmacology 2001;59(5):1108-18.
2000: A Chadha; Cyrille Sur; John R Atack; Susan M Duty
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.
British journal of pharmacology 2000;130(8):1927-32.
2000: Ruth M McKernan; Thomas W Rosahl; David S Reynolds; Cyrille Sur; Keith A Wafford; John R Atack; SJ Farrar; Janice Myers; G Cook; Pushpinder Ferris; L Garrett; Linda J Bristow; George Marshall; Alison Macaulay; Nicola Brown; Owain Howell; Kevin W Moore; Robert W Carling; Leslie J Street; José L Castro; C I Ragan; Gerard R Dawson; Paul J Whiting
Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.
Nature neuroscience 2000;3(6):587-92.
2000: A Chadha; Owain Howell; John R Atack; Cyrille Sur; Susan M Duty
Changes in [3H]zolpidem and [3H]Ro 15-1788 binding in rat globus pallidus and substantia nigra pars reticulata following a nigrostriatal tract lesion.
Brain research 2000;862(1-2):280-3.
2000: John R Atack; Susan M Cook; Peter H Hutson; S E File
Kindling induced by pentylenetetrazole in rats is not directly associated with changes in the expression of NMDA or benzodiazepine receptors.
Pharmacology, biochemistry, and behavior 2000;65(4):743-50.
2000: Owain Howell; John R Atack; D Dewar; Ruth M McKernan; Cyrille Sur
Density and pharmacology of alpha5 subunit-containing GABA(A) receptors are preserved in hippocampus of Alzheimer's disease patients.
Neuroscience 2000;98(4):669-75.
1999: Cyrille Sur; SJ Farrar; Julie Kerby; Paul J Whiting; John R Atack; Ruth M McKernan
Preferential coassembly of alpha4 and delta subunits of the gamma-aminobutyric acidA receptor in rat thalamus.
Molecular pharmacology 1999;56(1):110-5.
1999: Cyrille Sur; L Fresu; Owain Howell; Ruth M McKernan; John R Atack
Autoradiographic localization of alpha5 subunit-containing GABAA receptors in rat brain.
Brain research 1999;822(1-2):265-70.
1999: John R Atack; A J Smith; F Emms; Ruth M McKernan
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.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 1999;20(3):255-62.
1998: Cyrille Sur; Kathleen Quirk; D Dewar; John R Atack; Ruth M McKernan
Rat and human hippocampal alpha5 subunit-containing gamma-aminobutyric AcidA receptors have alpha5 beta3 gamma2 pharmacological characteristics.
Molecular pharmacology 1998;54(5):928-33.
1998: A J Smith; R M McKernan; John R Atack
Benzodiazepine modulation of recombinant alpha1beta3gamma2 GABA(A) receptor function efficacy determination using the Cytosensor microphysiometer.
European journal of pharmacology 1998;359(2-3):261-9.
1998: John R Atack; J Levine; R H Belmaker
Cerebrospinal fluid inositol monophosphatase: elevated activity in depression and neuroleptic-treated schizophrenia.
Biological psychiatry 1998;44(6):433-7.
1998: John R Atack; Stanley I Rapoport; Mark B Schapiro
Cerebrospinal fluid production is normal in Down syndrome.
Neurobiology of aging 1998;19(4):307-9.
1997: John R Atack
Inositol monophosphatase inhibitors--lithium mimetics?
Medicinal research reviews 1997;17(2):215-24.
1996: John R Atack
Inositol monophosphatase, the putative therapeutic target for lithium.
Brain research. Brain research reviews 1996;22(2):183-90.
1996: Sarah Grimwood; B Le Bourdellès; John R Atack; C Barton; W Cockett; S M Cook; E Gilbert; Peter H Hutson; Ruth M McKernan; J Myers; C Ian Ragan; Peter B Wingrove; Paul J Whiting
Generation and characterisation of stable cell lines expressing recombinant human N-methyl-D-aspartate receptor subtypes.
Journal of neurochemistry 1996;66(6):2239-47.
1995: John R Atack; Howard B Broughton; S J Pollack
Inositol monophosphatase--a putative target for Li+ in the treatment of bipolar disorder.
Trends in neurosciences 1995;18(8):343-9.
1995: John R Atack; Howard B Broughton; S J Pollack
Structure and mechanism of inositol monophosphatase.
FEBS letters 1995;361(1):1-7.
1994: R Bone; L Frank; J P Springer; John R Atack
Structural studies of metal binding by inositol monophosphatase: evidence for two-metal ion catalysis.
Biochemistry 1994;33(32):9468-76.
1994: R Bone; L Frank; J P Springer; S J Pollack; S A Osborne; John R Atack; M R Knowles; George McAllister; C Ian Ragan; Howard B Broughton
Structural analysis of inositol monophosphatase complexes with substrates.
Biochemistry 1994;33(32):9460-7.
1994: John R Atack; A M Prior; S R Fletcher; Kathleen Quirk; Ruth M McKernan; C Ian Ragan
Effects of L-690,488, a prodrug of the bisphosphonate inositol monophosphatase inhibitor L-690,330, on phosphatidylinositol cycle markers.
The Journal of pharmacology and experimental therapeutics 1994;270(1):70-6.
1994: S J Pollack; John R Atack; M R Knowles; George McAllister; C Ian Ragan; R Baker; S R Fletcher; L L Iversen; Howard B Broughton
Mechanism of inositol monophosphatase, the putative target of lithium therapy.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(13):5766-70.
1993: John R Atack; A M Prior; D Griffith; C Ian Ragan
Characterization of the effects of lithium on phosphatidylinositol (PI) cycle activity in human muscarinic m1 receptor-transfected CHO cells.
British journal of pharmacology 1993;110(2):809-15.
1993: S J Pollack; M R Knowles; John R Atack; Howard B Broughton; C Ian Ragan; S Osborne; George McAllister
Probing the role of metal ions in the mechanism of inositol monophosphatase by site-directed mutagenesis.
European journal of biochemistry / FEBS 1993;217(1):281-7.
1993: John R Atack; Stanley I Rapoport; C L Varley
Characterization of inositol monophosphatase in human cerebrospinal fluid.
Brain research 1993;613(2):305-8.
1993: John R Atack; S M Cook; Alan P Watt; S R Fletcher; C Ian Ragan
In vitro and in vivo inhibition of inositol monophosphatase by the bisphosphonate L-690,330.
Journal of neurochemistry 1993;60(2):652-8.
1992: R Bone; J P Springer; John R Atack
Structure of inositol monophosphatase, the putative target of lithium therapy.
Proceedings of the National Academy of Sciences of the United States of America 1992;89(21):10031-5.
1992: John R Atack; S M Cook; Alan P Watt; C Ian Ragan
Measurement of lithium-induced changes in mouse inositol(1)phosphate levels in vivo.
Journal of neurochemistry 1992;59(5):1946-54.
1992: George McAllister; P Whiting; E A Hammond; M R Knowles; John R Atack; F J Bailey; R Maigetter; C Ian Ragan
cDNA cloning of human and rat brain myo-inositol monophosphatase. Expression and characterization of the human recombinant enzyme.
The Biochemical journal 1992;284 ( Pt 3)():749-54.