Search Results - "MCKERNAN, R. M"

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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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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Age-related changes in GABA A receptor subunit composition and function in rat auditory system by Caspary, D.M, Holder, T.M, Hughes, L.F, Milbrandt, J.C, McKernan, R.M, Naritoku, D.K

“…A decline in the ability to discriminate speech from noise due to age-related hearing loss (presbycusis) may reflect impaired auditory information processing…”
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Anticonvulsant and adverse effects of avermectin analogs in mice are mediated through the gamma-aminobutyric acid(A) receptor by Dawson, G R, Wafford, K A, Smith, A, Marshall, G R, Bayley, P J, Schaeffer, J M, Meinke, P T, McKernan, R M

“…Twenty-five avermectin analogs were assessed in a mouse seizure model. The ED(50) against pentylenetetrazole-induced tonic seizures ranged from 0.48 mg/kg…”
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NMDA receptor pathways as drug targets by Kemp, John A, McKernan, Ruth M

“…Since the mid 1980s, there has been a great deal of enthusiasm within both academia and industry about the therapeutic potential of drugs targeting the NMDA…”
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Model of subunit composition of gamma-aminobutyric acid A receptor subtypes expressed in rat cerebellum with respect to their alpha and gamma/delta subunits by QUIRK, K, GILLARD, N. P, RAGAN, C. I, WHITING, P. J, MCKERNAN, R. M

“…Antibodies specific for subunits of the gamma-aminobutyric acid A (GABAA) receptor have been used to immunoprecipitate [3H]muscimol, [3H]Ro 15-4513, and [3H]Ro…”
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Which GABAA-receptor subtypes really occur in the brain ? by MCKERNAN, R. M, WHITING, P. J

“…GABAA receptors are a heterogeneous family of ligand-gated ion channels responsible for mediating inhibitory neurotransmission in the CNS. Since the…”
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Characterization of [ 35 S] t ‐butylbicyclophosphorothionate ([ 35 S]TBPS) binding to GABA A receptors in postmortem human brain by Atack, J R, Ohashi, Y, McKernan, R M

“…Background and purpose: The aim of the present study was to determine whether binding of [ 35 S] t ‐butylbicyclophosphorothionate ([ 35 S]TBPS) to the…”
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Stable Expression of Mammalian type A γ-Aminobutyric Acid Receptors in Mouse Cells: Demonstration of Functional Assembly of Benzodiazepine- Responsive Sites by Hadingham, Karen L., Harkness, Patricia C., McKernan, Ruth M., Quirk, Kathleen, Le Bourdelles, Beatrice, Horne, Anthony L., Kemp, John A., Barnard, Eric A., Ragan, C. Ian, Whiting, Paul J.

“…The differential sensitivity of type A γ-aminobutyric acid (GABAA) receptors to benzodiazepine ligands seen in the mammalian nervous system is thought to be…”
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gamma-Aminobutyric acid type A receptors in the rat brain can contain both gamma 2 and gamma 3 subunits, but gamma 1 does not exist in combination with another gamma subunit by Quirk, K, Gillard, N P, Ragan, C I, Whiting, P J, McKernan, R M

“…Antibodies specific for the gamma 1, gamma 2, and gamma 3 subunits of the gamma-aminobutyric acid (GABA)A receptor have been used to probe the composition of…”
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Localization of 5-HT3 receptors in the rat spinal cord: immunohistochemistry and in situ hybridization by Kia, H K, Miquel, M C, McKernan, R M, Laporte, A M, Lombard, M C, Bourgoin, S, Hamon, M, Vergé, D

“…Specific antibodies raised against a fusion protein containing the amino acid sequence of the putative second intracellular loop of the cloned 5-HT3-A receptor…”
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CSF neuron-specific enolase as a quantitative marker of neuronal damage in a rat stroke model by Hatfield, R H, McKernan, R M

“…A technique for chronic cisternal cerebrospinal fluid (CSF) sampling in conscious rats was used to obtain multiple 50 microliters samples before and up to 7…”
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MRK-409 (MK-0343), a GABA A 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 GABA A receptors with comparable high affinity (0.21–0.40 nM). However, MRK-409 has greater…”
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Generation and characterisation of stable cell lines expressing recombinant human N-methyl-D-aspartate receptor subtypes by Grimwood, S, Le Bourdellès, B, Atack, J R, Barton, C, Cockett, W, Cook, S M, Gilbert, E, Hutson, P H, McKernan, R M, Myers, J, Ragan, C I, Wingrove, P B, Whiting, P J

“…Transfection of mouse L(tk-) cells with human N-methyl-D-aspartate (NMDA) receptor subunit cDNAs under the control of a dexamethasone-inducible promoter has…”
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Differential expression of GABAA receptor α-subunits in rat brain during development by McKernan, R.M., Cox, P., Gillard, N.P., Whiting, P.

“…Unique cytoplasmic loop regions of the α1, α2, α3 and α5 subunits of the GABAA receptor have been expressed in E. coli and used to generate polyclonal antisera…”
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Stoichiometry of a Ligand-gated Ion Channel Determined by Fluorescence Energy Transfer by Farrar, S J, Whiting, P J, Bonnert, T P, McKernan, R M

“…We have developed a method to determine the stoichiometry of subunits within an oligomeric cell surface receptor using fluorescently tagged antibodies to the…”
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Loss of the major GABA(A) receptor subtype in the brain is not lethal in mice by Sur, C, Wafford, K A, Reynolds, D S, Hadingham, K L, Bromidge, F, Macaulay, A, Collinson, N, O'Meara, G, Howell, O, Newman, R, Myers, J, Atack, J R, Dawson, G R, McKernan, R M, Whiting, P J, Rosahl, T W

“…The alpha1beta2gamma2 is the most abundant subtype of the GABA(A) receptor and is localized in many regions of the brain. To gain more insight into the role of…”
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θ , a Novel γ -Aminobutyric Acid Type A Receptor Subunit by Bonnert, Timothy P., McKernan, Ruth M., Farrar, Sophie, le Bourdellès, Béatrice, Heavens, Robert P., Smith, David W., Hewson, Louise, Rigby, Michael R., Dalip J. S. Sirinathsinghji, Brown, Nicola, Wafford, Keith A., Whiting, Paul J.

“…γ -Aminobutyric acid type A (GABA-A) receptors are a major mediator of inhibitory neurotransmission in the mammalian central nervous system, and the site of…”
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Molecular and Functional Diversity of the Expanding GABA-A Receptor Gene Family by WHITING, PAUL J., BONNERT, TIMOTHY P., MCKERNAN, RUTH M., FARRAR, SOPHIE, BOURDELLES, BEATRICE LE, HEAVENS, ROBERT P., SMITH, DAVID W., HEWSON, LOUISE, RIGBY, MICHAEL R., SIRINATHSINGHJI, DALIP J. S., THOMPSON, SALLY A., WAFFORD, KEITH A.

“…Fast inhibitory neurotransmission in the mammalian CNS is mediated primarily by the neurotransmitter γ‐aminobutyric acid (GABA), which, upon binding to its…”
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Which GABA A-receptor subtypes really occur in the brain? by McKernan, Ruth M., Whiting, Paul J.

“…GABA A receptors are a heterogeneous family of ligand-gated ion channels responsible for mediating inhibitory neurotransmission in the CNS. Since the…”
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