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Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.
SB-277011-A (trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolininecarboxamide), is a brain-penetrant, high-affinity, and selective dopamine D(3) receptorExpand
In vitro and in vivo profile of SB 206553, a potent 5‐HT2C/5‐HT2B receptor antagonist with anxiolytic‐like properties
1 SB 206553 (5‐methyl‐1‐(3‐pyridylcarbamoyl)‐1,2,3,5‐tetrahydropyrrolo[2,3‐f]indole) displays a high affinity (pK1 7.9) for the cloned human 5‐HT2C receptor expressed in HEK 293 cells and the 5‐HT2BExpand
GSK189254, a Novel H3 Receptor Antagonist That Binds to Histamine H3 Receptors in Alzheimer's Disease Brain and Improves Cognitive Performance in Preclinical Models
6-[(3-Cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide hydrochloride (GSK189254) is a novel histamine H3 receptor antagonist with high affinity for human (pKi =Expand
Long-term evaluation of isolation-rearing induced prepulse inhibition deficits in rats: an update
RationaleRats reared in social isolation from weaning show prepulse inhibition (PPI) deficits which are thought to model the sensorimotor gating deficits seen in schizophrenia and other psychiatricExpand
Preclinical investigations into the antipsychotic potential of the novel histamine H3 receptor antagonist GSK207040
ObjectivesTo 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 ofExpand
Reversal of isolation-rearing-induced PPI deficits by an α7 nicotinic receptor agonist
RationaleThe 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 ofExpand
Medial prefrontal cortex volume loss in rats with isolation rearing-induced deficits in prepulse inhibition of acoustic startle
Rearing rats in isolation produces perturbations in behavior and brain neurochemistry suggested to resemble those of schizophrenia. In particular, isolation-reared rats display deficits in prepulseExpand
Marmoset Conspecific Confrontation: An Ethologically-Based Model of Anxiety
  • J. Cilia, D. Piper
  • Medicine, Psychology
  • Pharmacology Biochemistry and Behavior
  • 1 September 1997
A method of measuring confrontation-induced behavioural changes in common marmosets (Callithrix jacchus) together with automated monitoring of locomotor activity has been developed as a possibleExpand
Antipsychotic treatment alters protein expression associated with presynaptic function and nervous system development in rat frontal cortex.
Haloperidol and olanzapine are widely used antipsychotic drugs in the treatment of schizophrenia and other psychotic disorders. Despite extensive research efforts within the biopharmaceuticalExpand
Differential expression of IEG mRNA in rat brain following acute treatment with clozapine or haloperidol: a semi-quantitative RT—PCR study
Antipsychotic drugs have been shown to modulate immediate early gene (IEG) expression in rat brain regions that are associated with schizophrenia, which may be directly linked to their immediateExpand