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Pharmacological Modulation of Sleep Homeostasis in Rat: Novel Effects of an mGluR2/3 Antagonist.

Hanley N, Paulissen J, Eastwood BJ, Gilmour G, Loomis S, Wafford KA, McCarthy A.

Sleep. 2019 May 18. pii: zsz123. doi: 10.1093/sleep/zsz123. [Epub ahead of print]


REM sleep's unique associations with corticosterone regulation, apoptotic pathways, and behavior in chronic stress in mice.

Nollet M, Hicks H, McCarthy AP, Wu H, Möller-Levet CS, Laing EE, Malki K, Lawless N, Wafford KA, Dijk DJ, Winsky-Sommerer R.

Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2733-2742. doi: 10.1073/pnas.1816456116. Epub 2019 Jan 25.


Disturbances of sleep quality, timing and structure and their relationship with other neuropsychiatric symptoms in Alzheimer's disease and schizophrenia: Insights from studies in patient populations and animal models.

Winsky-Sommerer R, de Oliveira P, Loomis S, Wafford K, Dijk DJ, Gilmour G.

Neurosci Biobehav Rev. 2019 Feb;97:112-137. doi: 10.1016/j.neubiorev.2018.09.027. Epub 2018 Oct 9. Review.


Investigating the role of mGluR2 versus mGluR3 in antipsychotic-like effects, sleep-wake architecture and network oscillatory activity using novel Han Wistar rats lacking mGluR2 expression.

Wood CM, Wafford KA, McCarthy AP, Hewes N, Shanks E, Lodge D, Robinson ESJ.

Neuropharmacology. 2018 Sep 15;140:246-259. doi: 10.1016/j.neuropharm.2018.07.013. Epub 2018 Jul 11.


Effects of Aging on Cortical Neural Dynamics and Local Sleep Homeostasis in Mice.

McKillop LE, Fisher SP, Cui N, Peirson SN, Foster RG, Wafford KA, Vyazovskiy VV.

J Neurosci. 2018 Apr 18;38(16):3911-3928. doi: 10.1523/JNEUROSCI.2513-17.2018. Epub 2018 Mar 26.


Preclinical profile of a dopamine D1 potentiator suggests therapeutic utility in neurological and psychiatric disorders.

Bruns RF, Mitchell SN, Wafford KA, Harper AJ, Shanks EA, Carter G, O'Neill MJ, Murray TK, Eastwood BJ, Schaus JM, Beck JP, Hao J, Witkin JM, Li X, Chernet E, Katner JS, Wang H, Ryder JW, Masquelin ME, Thompson LK, Love PL, Maren DL, Falcone JF, Menezes MM, Zhang L, Yang CR, Svensson KA.

Neuropharmacology. 2018 Jan;128:351-365. doi: 10.1016/j.neuropharm.2017.10.032. Epub 2017 Oct 26.


TaiNi: Maximizing research output whilst improving animals' welfare in neurophysiology experiments.

Jiang Z, Huxter JR, Bowyer SA, Blockeel AJ, Butler J, Imtiaz SA, Wafford KA, Phillips KG, Tricklebank MD, Marston HM, Rodriguez-Villegas E.

Sci Rep. 2017 Aug 14;7(1):8086. doi: 10.1038/s41598-017-08078-8.


Electroencephalographic, cognitive, and neurochemical effects of LY3130481 (CERC-611), a selective antagonist of TARP-γ8-associated AMPA receptors.

Witkin JM, Li J, Gilmour G, Mitchell SN, Carter G, Gleason SD, Seidel WF, Eastwood BJ, McCarthy A, Porter WJ, Reel J, Gardinier KM, Kato AS, Wafford KA.

Neuropharmacology. 2017 Nov;126:257-270. doi: 10.1016/j.neuropharm.2017.07.028. Epub 2017 Jul 28.


Polypharmacological in Silico Bioactivity Profiling and Experimental Validation Uncovers Sedative-Hypnotic Effects of Approved and Experimental Drugs in Rat.

Drakakis G, Wafford KA, Brewerton SC, Bodkin MJ, Evans DA, Bender A.

ACS Chem Biol. 2017 Jun 16;12(6):1593-1602. doi: 10.1021/acschembio.7b00209. Epub 2017 May 1.


Phase-amplitude coupled persistent theta and gamma oscillations in rat primary motor cortex in vitro.

Johnson NW, Özkan M, Burgess AP, Prokic EJ, Wafford KA, O'Neill MJ, Greenhill SD, Stanford IM, Woodhall GL.

Neuropharmacology. 2017 Jun;119:141-156. doi: 10.1016/j.neuropharm.2017.04.009. Epub 2017 Apr 8.


Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression.

Witkin JM, Mitchell SN, Wafford KA, Carter G, Gilmour G, Li J, Eastwood BJ, Overshiner C, Li X, Rorick-Kehn L, Rasmussen K, Anderson WH, Nikolayev A, Tolstikov VV, Kuo MS, Catlow JT, Li R, Smith SC, Mitch CH, Ornstein PL, Swanson S, Monn JA.

J Pharmacol Exp Ther. 2017 Apr;361(1):68-86. doi: 10.1124/jpet.116.238121. Epub 2017 Jan 30.


Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.

Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL.

J Med Chem. 2016 Dec 22;59(24):10974-10993. Epub 2016 Dec 6.


Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.

Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. doi: 10.1016/j.bmcl.2016.10.067. Epub 2016 Oct 25.


Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism.

Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM.

Nat Med. 2016 Dec;22(12):1496-1501. doi: 10.1038/nm.4221. Epub 2016 Nov 7.


Modelling maintenance of wakefulness in rats: comparing potential non-invasive sleep-restriction methods and their effects on sleep and attentional performance.

Mccarthy A, Loomis S, Eastwood B, Wafford KA, Winsky-Sommerer R, Gilmour G.

J Sleep Res. 2017 Apr;26(2):179-187. doi: 10.1111/jsr.12464. Epub 2016 Oct 14.


Erratum: A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies.

Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM.

Neuropsychopharmacology. 2016 Sep;41(10):2624. doi: 10.1038/npp.2016.78. Epub 2016 Aug 11.


REM sleep homeostasis in the absence of REM sleep: Effects of antidepressants.

McCarthy A, Wafford K, Shanks E, Ligocki M, Edgar DM, Dijk DJ.

Neuropharmacology. 2016 Sep;108:415-25. doi: 10.1016/j.neuropharm.2016.04.047. Epub 2016 May 2.


Prevalence and influence of cys407* Grm2 mutation in Hannover-derived Wistar rats: mGlu2 receptor loss links to alcohol intake, risk taking and emotional behaviour.

Wood CM, Nicolas CS, Choi SL, Roman E, Nylander I, Fernandez-Teruel A, Kiianmaa K, Bienkowski P, de Jong TR, Colombo G, Chastagnier D, Wafford KA, Collingridge GL, Wildt SJ, Conway-Campbell BL, Robinson ES, Lodge D.

Neuropharmacology. 2017 Mar 15;115:128-138. doi: 10.1016/j.neuropharm.2016.03.020. Epub 2016 Mar 14. Review.


A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies.

Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM.

Neuropsychopharmacology. 2016 Jun;41(7):1803-12. doi: 10.1038/npp.2015.348. Epub 2015 Nov 20. Erratum in: Neuropsychopharmacology. 2016 Sep;41(10):2624.


The role of K₂p channels in anaesthesia and sleep.

Steinberg EA, Wafford KA, Brickley SG, Franks NP, Wisden W.

Pflugers Arch. 2015 May;467(5):907-16. doi: 10.1007/s00424-014-1654-4. Epub 2014 Dec 9. Review.


Development and pharmacological characterization of a model of sleep disruption-induced hypersensitivity in the rat.

Wodarski R, Schuh-Hofer S, Yurek DA, Wafford KA, Gilmour G, Treede RD, Kennedy JD.

Eur J Pain. 2015 Apr;19(4):554-66. doi: 10.1002/ejp.580. Epub 2014 Sep 5.


SAXS characterization of genetically engineered tobacco mosaic virus nanorods coated with palladium in the absence of external reducing agents.

Freer AS, Guarnaccio L, Wafford K, Smith J, Steilberg J, Culver JN, Harris MT.

J Colloid Interface Sci. 2013 Feb 15;392:213-218. doi: 10.1016/j.jcis.2012.09.072. Epub 2012 Nov 7.


Decoupling of sleep-dependent cortical and hippocampal interactions in a neurodevelopmental model of schizophrenia.

Phillips KG, Bartsch U, McCarthy AP, Edgar DM, Tricklebank MD, Wafford KA, Jones MW.

Neuron. 2012 Nov 8;76(3):526-33. doi: 10.1016/j.neuron.2012.09.016.


A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABA(A) receptors.

Jensen ML, Wafford KA, Brown AR, Belelli D, Lambert JJ, Mirza NR.

Br J Pharmacol. 2013 Mar;168(5):1118-32. doi: 10.1111/bph.12001.


In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat.

Gilmour G, Broad LM, Wafford KA, Britton T, Colvin EM, Fivush A, Gastambide F, Getman B, Heinz BA, McCarthy AP, Prieto L, Shanks E, Smith JW, Taboada L, Edgar DM, Tricklebank MD.

Neuropharmacology. 2013 Jan;64:224-39. doi: 10.1016/j.neuropharm.2012.07.030. Epub 2012 Aug 1.


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

Mirza NR, Atack J, Wafford K.

Adv Pharmacol Sci. 2012;2012:529861. doi: 10.1155/2012/529861. Epub 2012 Apr 18. No abstract available.


Differential effects of NMDA antagonists on high frequency and gamma EEG oscillations in a neurodevelopmental model of schizophrenia.

Phillips KG, Cotel MC, McCarthy AP, Edgar DM, Tricklebank M, O'Neill MJ, Jones MW, Wafford KA.

Neuropharmacology. 2012 Mar;62(3):1359-70. doi: 10.1016/j.neuropharm.2011.04.006. Epub 2011 Apr 19.


N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.

Fell MJ, Witkin JM, Falcone JF, Katner JS, Perry KW, Hart J, Rorick-Kehn L, Overshiner CD, Rasmussen K, Chaney SF, Benvenga MJ, Li X, Marlow DL, Thompson LK, Luecke SK, Wafford KA, Seidel WF, Edgar DM, Quets AT, Felder CC, Wang X, Heinz BA, Nikolayev A, Kuo MS, Mayhugh D, Khilevich A, Zhang D, Ebert PJ, Eckstein JA, Ackermann BL, Swanson SP, Catlow JT, Dean RA, Jackson K, Tauscher-Wisniewski S, Marek GJ, Schkeryantz JM, Svensson KA.

J Pharmacol Exp Ther. 2011 Jan;336(1):165-77. doi: 10.1124/jpet.110.172957. Epub 2010 Oct 14.


Distinct activities of GABA agonists at synaptic- and extrasynaptic-type GABAA receptors.

Mortensen M, Ebert B, Wafford K, Smart TG.

J Physiol. 2010 Apr 15;588(Pt 8):1251-68. doi: 10.1113/jphysiol.2009.182444. Epub 2010 Feb 22.


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.


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.


Novel compounds selectively enhance delta subunit containing GABA A receptors and increase tonic currents in thalamus.

Wafford KA, van Niel MB, Ma QP, Horridge E, Herd MB, Peden DR, Belelli D, Lambert JJ.

Neuropharmacology. 2009 Jan;56(1):182-9. doi: 10.1016/j.neuropharm.2008.08.004. Epub 2008 Aug 13.


Emerging anti-insomnia drugs: tackling sleeplessness and the quality of wake time.

Wafford KA, Ebert B.

Nat Rev Drug Discov. 2008 Jun;7(6):530-40. doi: 10.1038/nrd2464. Epub 2008 May 23. Review.


The expression of GABAA beta subunit isoforms in synaptic and extrasynaptic receptor populations of mouse dentate gyrus granule cells.

Herd MB, Haythornthwaite AR, Rosahl TW, Wafford KA, Homanics GE, Lambert JJ, Belelli D.

J Physiol. 2008 Feb 15;586(4):989-1004. Epub 2007 Dec 13.


Developmental maturation of synaptic and extrasynaptic GABAA receptors in mouse thalamic ventrobasal neurones.

Peden DR, Petitjean CM, Herd MB, Durakoglugil MS, Rosahl TW, Wafford K, Homanics GE, Belelli D, Fritschy JM, Lambert JJ.

J Physiol. 2008 Feb 15;586(4):965-87. Epub 2007 Dec 6.


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

Fradley RL, Guscott MR, Bull S, Hallett DJ, Goodacre SC, Wafford KA, Garrett EM, Newman RJ, O'Meara GF, Whiting PJ, Rosahl TW, Dawson GR, Reynolds DS, Atack JR.

J Psychopharmacol. 2007 Jun;21(4):384-91. Epub 2006 Nov 8.


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.


The role of GABAbeta2 subunit-containing receptors in mediating the anticonvulsant and sedative effects of loreclezole.

Groves JO, Guscott MR, Hallett DJ, Rosahl TW, Pike A, Davies A, Wafford KA, Reynolds DS.

Eur J Neurosci. 2006 Jul;24(1):167-74.


Treating insomnia: Current and investigational pharmacological approaches.

Ebert B, Wafford KA, Deacon S.

Pharmacol Ther. 2006 Dec;112(3):612-29. Epub 2006 Jul 28. Review.


A genetically modified mouse model probing the selective action of ifenprodil at the N-methyl-D-aspartate type 2B receptor.

Rosahl TW, Wingrove PB, Hunt V, Fradley RL, Lawrence JM, Heavens RP, Treacey P, Usala M, Macaulay A, Bonnert TP, Whiting PJ, Wafford KA.

Mol Cell Neurosci. 2006 Sep;33(1):47-56. Epub 2006 Jul 25.


New directions in kinetic high information content assays.

Simpson PB, Wafford KA.

Drug Discov Today. 2006 Mar;11(5-6):237-44. Review. No abstract available.


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

Carling RW, Russell MG, Moore KW, Mitchinson A, Guiblin A, Smith A, Wafford KA, Marshall G, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3550-4. Epub 2006 Apr 18.


A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Lewis RT, Blackaby WP, Blackburn T, Jennings AS, Pike A, Wilson RA, Hallett DJ, Cook SM, Ferris P, Marshall GR, Reynolds DS, Sheppard WF, Smith AJ, Sohal B, Stanley J, Tye SJ, Wafford KA, Atack JR.

J Med Chem. 2006 Apr 20;49(8):2600-10.


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

Cheng VY, Martin LJ, Elliott EM, Kim JH, Mount HT, Taverna FA, Roder JC, Macdonald JF, Bhambri A, Collinson N, Wafford KA, Orser BA.

J Neurosci. 2006 Apr 5;26(14):3713-20.


Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL.

J Med Chem. 2006 Feb 23;49(4):1235-8.


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.


Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.

Blackaby WP, Atack JR, Bromidge F, Castro JL, Goodacre SC, Hallett DJ, Lewis RT, Marshall GR, Pike A, Smith AJ, Street LJ, Tattersall DF, Wafford KA.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1175-9. Epub 2006 Jan 6.


Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.

Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR.

J Med Chem. 2006 Jan 12;49(1):35-8.


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