Search Results - "WAFFORD, K. A"

Longitudinal changes in EEG power, sleep cycles and behaviour in a tau model of neurodegeneration by Holton, C. M, Hanley, N, Shanks, E, Oxley, P, McCarthy, A, Eastwood, B. J, Murray, T. K, Nickerson, A, Wafford, K. A

“…Abstract Background Disturbed sleep is associated with cognitive decline in neurodegenerative diseases such as Alzheimer’s disease (AD) and frontotemporal…”
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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 by Jensen, M L, Wafford, K A, Brown, A R, Belelli, D, Lambert, J J, Mirza, N R

“…Most GABA(A) receptor subtypes comprise 2α, 2β and 1γ subunit, although for some isoforms, a δ replaces a γ-subunit. Extrasynaptic δ-GABA(A) receptors are…”
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MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans by 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

“…MRK-409 binds to α1-, α2-, α3- and α5-containing human recombinant GABAA receptors with comparable high affinity (0.21–0.40 nM). However, MRK-409 has greater…”
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Differential effects of NMDA antagonists on high frequency and gamma EEG oscillations in a neurodevelopmental model of schizophrenia by Phillips, K.G., Cotel, M.C., McCarthy, A.P., Edgar, D.M., Tricklebank, M., O’Neill, M.J., Jones, M.W., Wafford, K.A.

“…Neuroanatomical, electrophysiological and behavioural abnormalities following timed prenatal methylazoxymethanol acetate (MAM) treatment in rats model changes…”
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The Cys-loop superfamily of ligand-gated ion channels: the impact of receptor structure on function by Connolly, C N, Wafford, K A

“…The Cys-loop receptors constitute an important superfamily of LGICs (ligand-gated ion channels) comprising receptors for acetylcholine, 5-HT3…”
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The role of K2P channels in anaesthesia and sleep by Steinberg, E. A., Wafford, K. A., Brickley, S. G., Franks, N. P., Wisden, W.

“…Tandem two-pore potassium channels (K 2P s) have widespread expression in the central nervous system and periphery where they contribute to background membrane…”
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Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist by Atack, JR, Hallett, DJ, Tye, S, Wafford, KA, Ryan, C, Sanabria-Bohórquez, SM, Eng, Wai-si, 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

“…In the accompanying paper we describe how MRK-409 unexpectedly produced sedation in man at relatively low levels of GABAA receptor occupancy (∼10%). Since it…”
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Barbiturate interactions at the human GABAA receptor: dependence on receptor subunit combination by Thompson, S.A., Whiting, P.J., Wafford, K.A.

“…1 Human GABAA receptors containing different α and β subunits with a γ2s subunit were expressed in Xenopus oocytes and the effects of pentobarbitone on these…”
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Role of the beta subunit in determining the pharmacology of human gamma-aminobutyric acid type A receptors by Hadingham, K L, Wingrove, P B, Wafford, K A, Bain, C, Kemp, J A, Palmer, K J, Wilson, A W, Wilcox, A S, Sikela, J M, Ragan, C I

“…A cDNA encoding the human gamma-aminobutyric acid (GABA)A receptor beta 2 subunit has been cloned and sequenced. The deduced amino acid sequence of this cDNA…”
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Differences in affinity and efficacy of benzodiazepine receptor ligands at recombinant gamma-aminobutyric acidA receptor subtypes by Wafford, K A, Whiting, P J, Kemp, J A

“…Two forms of the multisubunit gamma-aminobutyric acid (GABA)A receptor were expressed in Xenopus oocytes by injecting mRNA encoding the bovine GABAA receptor…”
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Novel compounds selectively enhance delta subunit containing GABA A receptors and increase tonic currents in thalamus by Wafford, K A, van Niel, M B, Ma, Q P, Horridge, E, Herd, M B, Peden, D R, Belelli, D, Lambert, J J

“…Inhibition in the brain is dominated by the neurotransmitter gamma-aminobutyric acid (GABA); operating through GABA(A) receptors. This form of neural…”
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Differentiating the role of gamma-aminobutyric acid type A (GABAA) receptor subtypes by Wafford, K A, Macaulay, A J, Fradley, R, O'Meara, G F, Reynolds, D S, Rosahl, T W

“…The inhibitory tone maintained throughout the central nervous system relies predominantly on the activity of neuronal GABAA (gamma-aminobutyric acid type A)…”
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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 by Witkin, J M, Mitchell, S N, Wafford, K A, Carter, G, Gilmour, G, Li, J, Eastwood, B J, Overshiner, C, Li, X, Rorick-Kehn, L, Rasmussen, K, Anderson, W H, Nikolayev, A, Tolstikov, V V, Kuo, M-S, Catlow, J T, Li, R, Smith, S C, Mitch, C H, Ornstein, P L, Swanson, S, Monn, J A

“…The ability of the -methyl-d-aspartate receptor antagonist ketamine to alleviate symptoms in patients suffering from treatment-resistant depression (TRD) is…”
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Novel compounds selectively enhance δ subunit containing GABAA receptors and increase tonic currents in thalamus by Wafford, K.A., van Niel, M.B., Ma, Q.P., Horridge, E., Herd, M.B., Peden, D.R., Belelli, D., Lambert, J.J.

“…Inhibition in the brain is dominated by the neurotransmitter γ-aminobutyric acid (GABA); operating through GABAA receptors. This form of neural inhibition was…”
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The modulatory action of loreclezole at the gamma-aminobutyric acid type A receptor is determined by a single amino acid in the beta 2 and beta 3 subunit by Wingrove, P B, Wafford, K A, Bain, C, Whiting, P J

“…Type A gamma-aminobutyric acid (GABAA) receptors of the mammalian nervous system are a family of ligand-gated ion channels probably formed from the coassembly…”
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Identification of amino acids in the N-methyl-D-aspartate receptor NR1 subunit that contribute to the glycine binding site by Wafford, K A, Kathoria, M, Bain, C J, Marshall, G, Le Bourdellès, B, Kemp, J A, Whiting, P J

“…The mammalian N-methyl-D-aspartate (NMDA) receptor complex is though to consist of an NR1 subunit in combination with one or more of the four NR2 subunits (A,…”
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A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABAA receptors by Jensen, ML, Wafford, KA, Brown, AR, Belelli, D, Lambert, JJ, Mirza, NR

“…Background and Purpose Most GABAA receptor subtypes comprise 2α, 2β and 1γ subunit, although for some isoforms, a δ replaces a γ‐subunit. Extrasynaptic δ‐GABAA…”
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Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors by Brown, N, Kerby, J, Bonnert, T P, Whiting, P J, Wafford, K A

“…1: The pharmacology of the stable cell line expressing human alpha(4)beta(3)delta GABA(A) receptor was investigated using whole-cell patch-clamp techniques. 2:…”
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Development and pharmacological characterization of a model of sleep disruption-induced hypersensitivity in the rat by Wodarski, R., Schuh-Hofer, S., Yurek, D.A., Wafford, K.A., Gilmour, G., Treede, R.-D., Kennedy, J.D.

“…Background Sleep disturbance is a commonly reported co‐morbidity in chronic pain patients, and conversely, disruption of sleep can cause acute and long‐lasting…”
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Functional comparison of the role of gamma subunits in recombinant human gamma-aminobutyric acidA/benzodiazepine receptors by Wafford, K A, Bain, C J, Whiting, P J, Kemp, J A

“…The effect of benzodiazepines on the activity of gamma-aminobutyric acid (GABA)A receptors has been shown to be influenced by different alpha subunits and can…”
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