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Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia.

Cao L, McDonnell A, Nitzsche A, Alexandrou A, Saintot PP, Loucif AJ, Brown AR, Young G, Mis M, Randall A, Waxman SG, Stanley P, Kirby S, Tarabar S, Gutteridge A, Butt R, McKernan RM, Whiting P, Ali Z, Bilsland J, Stevens EB.

Sci Transl Med. 2016 Apr 20;8(335):335ra56. doi: 10.1126/scitranslmed.aad7653.


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

Atack JR, Hallett DJ, Tye S, Wafford KA, Ryan C, Sanabria-Bohórquez SM, Eng WS, Gibson RE, Burns HD, Dawson GR, Carling RW, Street LJ, Pike A, De Lepeleire I, Van Laere K, Bormans G, de Hoon JN, Van Hecken A, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15.


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

Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10.


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.

Atack JR, Wong DF, Fryer TD, Ryan C, Sanabria S, Zhou Y, Dannals RF, Eng WS, Gibson RE, Burns HD, Vega JM, Vessy L, Scott-Stevens P, Beech JS, Baron JC, Sohal B, Schrag ML, Aigbirhio FI, McKernan RM, Hargreaves RJ.

J Pharmacol Exp Ther. 2010 Jan;332(1):17-25. doi: 10.1124/jpet.109.157909. Epub 2009 Sep 24.


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.

Atack JR, Maubach KA, Wafford KA, O'Connor D, Rodrigues AD, Evans DC, Tattersall FD, Chambers MS, MacLeod AM, Eng WS, Ryan C, Hostetler E, Sanabria SM, Gibson RE, Krause S, Burns HD, Hargreaves RJ, Agrawal NG, McKernan RM, Murphy MG, Gingrich K, Dawson GR, Musson DG, Petty KJ.

J Pharmacol Exp Ther. 2009 Nov;331(2):470-84. doi: 10.1124/jpet.109.157636. Epub 2009 Aug 24.


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

Pike A, Cook SM, Watt AP, Scott-Stevens P, Rosahl TW, McKernan RM, Pym LJ, Guiblin A, Moyes C, Sohal B, Atack JR.

Biopharm Drug Dispos. 2007 Sep;28(6):275-82.


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

Atack JR, Ohashi Y, McKernan RM.

Br J Pharmacol. 2007 Apr;150(8):1066-74. Epub 2007 Mar 5.


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

Atack JR, Bayley PJ, Seabrook GR, Wafford KA, McKernan RM, Dawson GR.

Neuropharmacology. 2006 Nov;51(6):1023-9. Epub 2006 Oct 12.


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

Atack JR, Bayley PJ, Fletcher SR, McKernan RM, Wafford KA, Dawson GR.

Eur J Pharmacol. 2006 Oct 24;548(1-3):77-82. Epub 2006 May 19.


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

Atack JR, Pike A, Clarke A, Cook SM, Sohal B, McKernan RM, Dawson GR.

Drug Metab Dispos. 2006 May;34(5):887-93. Epub 2006 Feb 2.


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

Atack JR, Pike A, Marshall G, Stanley J, Lincoln R, Cook SM, Lewis RT, Blackaby WP, Goodacre SC, McKernan RM, Dawson GR, Wafford KA, Reynolds DS.

Neuropharmacology. 2006 May;50(6):677-89. Epub 2006 Jan 20.


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

Dias R, Sheppard WF, Fradley RL, Garrett EM, Stanley JL, Tye SJ, Goodacre S, Lincoln RJ, Cook SM, Conley R, Hallett D, Humphries AC, Thompson SA, Wafford KA, Street LJ, Castro JL, Whiting PJ, Rosahl TW, Atack JR, McKernan RM, Dawson GR, Reynolds DS.

J Neurosci. 2005 Nov 16;25(46):10682-8.


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.

Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ.

J Med Chem. 2005 Nov 17;48(23):7089-92.


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

Pym LJ, Cook SM, Rosahl T, McKernan RM, Atack JR.

Br J Pharmacol. 2005 Nov;146(6):817-25.


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.

Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM.

J Pharmacol Exp Ther. 2006 Jan;316(1):410-22. Epub 2005 Sep 23.


Pyrazolopyridinones as functionally selective GABAA ligands.

Blackaby WP, Atack JR, Bromidge F, Lewis R, Russell MG, Smith A, Wafford K, McKernan RM, Street LJ, Castro JL.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4998-5002.


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

Atack JR, Alder L, Cook SM, Smith AJ, McKernan RM.

Neuropharmacology. 2005 Aug;49(2):220-9. Epub 2005 Apr 26.


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.

Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL.

J Med Chem. 2005 Mar 10;48(5):1367-83.


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

Atack JR, Hutson PH, Collinson N, Marshall G, Bentley G, Moyes C, Cook SM, Collins I, Wafford K, McKernan RM, Dawson GR.

Br J Pharmacol. 2005 Feb;144(3):357-66.


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.

Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM.

J Med Chem. 2004 Jul 1;47(14):3642-57.


2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.

Mitchinson A, Atack JR, Blurton P, Carling RW, Castro JL, Curley KS, Russell MG, Marshall G, McKernan RM, Moore KW, Narquizian R, Smith A, Street LJ, Thompson SA, Wafford K.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.


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.

Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL.

J Med Chem. 2004 Mar 25;47(7):1807-22.


NMDA receptor pathways as drug targets.

Kemp JA, McKernan RM.

Nat Neurosci. 2002 Nov;5 Suppl:1039-42. Review.


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

Collinson N, Kuenzi FM, Jarolimek W, Maubach KA, Cothliff R, Sur C, Smith A, Otu FM, Howell O, Atack JR, McKernan RM, Seabrook GR, Dawson GR, Whiting PJ, Rosahl TW.

J Neurosci. 2002 Jul 1;22(13):5572-80.


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

Collins I, Moyes C, Davey WB, Rowley M, Bromidge FA, Quirk K, Atack JR, McKernan RM, Thompson SA, Wafford K, Dawson GR, Pike A, Sohal B, Tsou NN, Ball RG, Castro JL.

J Med Chem. 2002 Apr 25;45(9):1887-900.


Retinoic acid evoked-differentiation of neuroblastoma cells predominates over growth factor stimulation: an automated image capture and quantitation approach to neuritogenesis.

Simpson PB, Bacha JI, Palfreyman EL, Woollacott AJ, McKernan RM, Kerby J.

Anal Biochem. 2001 Nov 15;298(2):163-9.


Anxiolytic-like action of diazepam: which GABA(A) receptor subtype is involved?

Reynolds DS, McKernan RM, Dawson GR.

Trends Pharmacol Sci. 2001 Aug;22(8):402-3. No abstract available.


alpha4beta3delta GABA(A) receptors characterized by fluorescence resonance energy transfer-derived measurements of membrane potential.

Adkins CE, Pillai GV, Kerby J, Bonnert TP, Haldon C, McKernan RM, Gonzalez JE, Oades K, Whiting PJ, Simpson PB.

J Biol Chem. 2001 Oct 19;276(42):38934-9. Epub 2001 Aug 8.


Loss of the major GABA(A) receptor subtype in the brain is not lethal in mice.

Sur C, Wafford KA, Reynolds DS, Hadingham KL, Bromidge F, Macaulay A, Collinson N, O'Meara G, Howell O, Newman R, Myers J, Atack JR, Dawson GR, McKernan RM, Whiting PJ, Rosahl TW.

J Neurosci. 2001 May 15;21(10):3409-18.


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.

Smith AJ, Alder L, Silk J, Adkins C, Fletcher AE, Scales T, Kerby J, Marshall G, Wafford KA, McKernan RM, Atack JR.

Mol Pharmacol. 2001 May;59(5):1108-18.


Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor.

Dawson GR, Wafford KA, Smith A, Marshall GR, Bayley PJ, Schaeffer JM, Meinke PT, McKernan RM.

J Pharmacol Exp Ther. 2000 Dec;295(3):1051-60.


N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.

Collins I, Davey WB, Rowley M, Quirk K, Bromidge FA, McKernan RM, Thompson SA, Wafford KA.

Bioorg Med Chem Lett. 2000 Jun 19;10(12):1381-4.


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

McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR, Farrar S, Myers J, Cook G, Ferris P, Garrett L, Bristow L, Marshall G, Macaulay A, Brown N, Howell O, Moore KW, Carling RW, Street LJ, Castro JL, Ragan CI, Dawson GR, Whiting PJ.

Nat Neurosci. 2000 Jun;3(6):587-92.


theta, a novel gamma-aminobutyric acid type A receptor subunit.

Bonnert TP, McKernan RM, Farrar S, le Bourdellès B, Heavens RP, Smith DW, Hewson L, Rigby MR, Sirinathsinghji DJ, Brown N, Wafford KA, Whiting PJ.

Proc Natl Acad Sci U S A. 1999 Aug 17;96(17):9891-6.


Age-related changes in GABA(A) receptor subunit composition and function in rat auditory system.

Caspary DM, Holder TM, Hughes LF, Milbrandt JC, McKernan RM, Naritoku DK.

Neuroscience. 1999;93(1):307-12.


Molecular and functional diversity of the expanding GABA-A receptor gene family.

Whiting PJ, Bonnert TP, McKernan RM, Farrar S, Le Bourdellès B, Heavens RP, Smith DW, Hewson L, Rigby MR, Sirinathsinghji DJ, Thompson SA, Wafford KA.

Ann N Y Acad Sci. 1999 Apr 30;868:645-53. Review.


Preferential coassembly of alpha4 and delta subunits of the gamma-aminobutyric acidA receptor in rat thalamus.

Sur C, Farrar SJ, Kerby J, Whiting PJ, Atack JR, McKernan RM.

Mol Pharmacol. 1999 Jul;56(1):110-5.


Stoichiometry of a ligand-gated ion channel determined by fluorescence energy transfer.

Farrar SJ, Whiting PJ, Bonnert TP, McKernan RM.

J Biol Chem. 1999 Apr 9;274(15):10100-4.


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

Sur C, Fresu L, Howell O, McKernan RM, Atack JR.

Brain Res. 1999 Mar 20;822(1-2):265-70.


Comparison of native 5-HT3 receptors purified from various neuroblastoma-derived cell lines and bovine brain with recombinant 5-HT3-AL receptors purified after expression in HEK293 cells.

Boess FG, Creighton RM, Phipps BA, McKernan RM, Reid J, Martin IL.

Ann N Y Acad Sci. 1998 Dec 15;861:276-7. No abstract available.


Evidence that porcine native 5-HT3 receptors do not contain nicotinic acetylcholine receptor subunits.

Fletcher S, Lindstrom JM, McKernan RM, Barnes NM.

Neuropharmacology. 1998;37(3):397-9.


Ligand-gated ion channel subunit partnerships: GABAA receptor alpha6 subunit gene inactivation inhibits delta subunit expression.

Jones A, Korpi ER, McKernan RM, Pelz R, Nusser Z, Mäkelä R, Mellor JR, Pollard S, Bahn S, Stephenson FA, Randall AD, Sieghart W, Somogyi P, Smith AJ, Wisden W.

J Neurosci. 1997 Feb 15;17(4):1350-62.


Generation and characterisation of stable cell lines expressing recombinant human N-methyl-D-aspartate receptor subtypes.

Grimwood S, Le Bourdellès B, Atack JR, Barton C, Cockett W, Cook SM, Gilbert E, Hutson PH, McKernan RM, Myers J, Ragan CI, Wingrove PB, Whiting PJ.

J Neurochem. 1996 Jun;66(6):2239-47.


Which GABAA-receptor subtypes really occur in the brain?

McKernan RM, Whiting PJ.

Trends Neurosci. 1996 Apr;19(4):139-43. Review.


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