Search results for: Eric Southam

Items from 1 to 9 out of 9 results

article

In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics

Lee A. Dawson, Christopher J. Langmead, Adeshola Dada, Jeannette M. Watson, more

European Journal of Pharmacology > 2010 > 627 > 1-3 > 106-114

Clinical evaluation of tachykinin NK ₃ receptor antagonists has provided support for the therapeutic utility of this target in schizophrenia. However, these studies have not been entirely conclusive, possibly because of the pharmacokinetic limitations of these molecules. In the search for tachykinin NK ₃ receptor antagonists with improved properties, we have discovered GSK172981 and...

article

Activation of 5-HT₆ receptors facilitates attentional set shifting

Katherine E. Burnham, Mark G. Baxter, John R. Bainton, Eric Southam, more

Psychopharmacology > 2010 > 208 > 1 > 13-21

Rationale Prefrontal cortex (PFC)-dependent executive function is disrupted in a range of psychiatric disorders and can be modelled in non-human primates and rodents using attentional set-shifting paradigms. There are few current pharmacological strategies for enhancing attentional set shifting, although the PFC is rich in relevant neurotransmitter targets, including 5-hydroxytryptamine (5-HT). Although...

article

In vitro and in vivo characterization of PheTQS, a novel α7 nAChR positive allosteric modulator

James N.C. Kew, Selina Mok, Annette Weil, Caterina Virginio, more

Biochemical Pharmacology > 2009 > 78 > 7 > 913

article

Preclinical investigations into the antipsychotic potential of the novel histamine H₃ receptor antagonist GSK207040

Eric Southam, Jackie Cilia, Jane E. Gartlon, Marie L. Woolley, more

Psychopharmacology > 2009 > 201 > 4 > 483-494

Objectives To test the novel nonimidazole histamine H₃ receptor antagonist 5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazapin-7-yl)oxy]-N-methyl-2-pyrazinecarboxamide (GSK207040) in a series of behavioral and neurochemical paradigms designed to evaluate its antipsychotic potential. Materials and methods Acute orally administered GSK207040 was investigated for its capacity to reverse a 24-h-induced...

article

Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain

Eric Southam, Andrew Lloyd, Carol A. Jennings, Jane E. Cluderay, more

Brain Research > 2007 > 1149 > Complete > 50-57

SB-277011-A is a dopamine D ₃ receptor antagonist that exhibits over 100-fold selectivity over dopamine D ₂ receptors and a broad spectrum of other receptor, ion channels, and enzymes. We employed c-Fos immunohistochemistry to characterise the functional neuroanatomical effects of acute administration of SB-277011-A and observed a time-dependent increase in the density of c-Fos-like...

article

Effect of lamotrigine on the activities of monoamine oxidases A and B in vitro and on monoamine disposition in vivo

Eric Southam, Rui Pereira, Sharon C. Stratton, Rebecca Sargent, more

European Journal of Pharmacology > 2005 > 519 > 3 > 237-245

Recent clinical evidence indicates that the broad spectrum anticonvulsant drug lamotrigine is effective against the depressive phase of bipolar illness and the difficult to treat rapid cycling form of the disorder. However, the molecular mechanism underlying this therapeutic action remains uncertain. Given that inhibition of the A-type of monoamine oxidase (MAO) is a proven antidepressant mechanism,...

article

A comparison of possible markers for chandelier cartridges in rat medial prefrontal cortex and hippocampus

Claire Hardwick, Sarah Jane French, Eric Southam, Susan Totterdell

Brain Research > 2005 > 1031 > 2 > 238-244

Chandelier neurons and their characteristic arrays of axonal terminals, known as cartridges, have been implicated in a variety of psychiatric and neurological disorders including schizophrenia and epilepsy. As a result, these neurons have been extensively examined in the brains of several species using a range of markers. However, these markers have not been systematically compared in a single species...

article

Reversal of isolation-rearing-induced PPI deficits by an α7 nicotinic receptor agonist

Jackie Cilia, Jane E. Cluderay, Melanie J. Robbins, Charlie Reavill, more

Psychopharmacology > 2005 > 182 > 2 > 214-219

Rationale The α7 subtype of the nicotinic receptor plays an important role in auditory sensory gating. Schizophrenics show deficient sensory gating and abnormalities in the number and regulation of nicotinic receptors. Prepulse inhibition (PPI) deficits exhibited by isolation-reared rats are thought to model the sensorimotor gating deficits seen in schizophrenia. Objective To examine the role of...

article

Broad spectrum anticonvulsant activity of BW534U87: possible role of an adenosine-dependent mechanism

Eric Southam, Sharon C. Stratton, Rebecca S. Sargent, Kim T. Brackenborough, more

Pharmacology, Biochemistry and Behavior > 2002 > 74 > 1 > 111-118

The novel putative anticonvulsant drug 1-[2,6-difluorophenyl)-methyl]-1H-1,2,3-triazolo[4,5-c]) pyridine-4-amine monohydrochloride (BW534U87) effectively reduced seizures induced in rodents by threshold maximal and supramaximal electroshock, electrical kindling, pentylenetetrazole (PTZ) infusion and by vestibular stimulation in the genetically seizure-prone epilepsy-like (EL) mouse. The range of animal...

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Search results for: Eric Southam

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