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The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy…
Findings support the potential utility of mGLUR5 and mGluR1 antagonists for both the treatment of chronic pain and as novel anxiolytics in models of pain and anxiety.
Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348…
- R. Hodgson, R. Bertorelli, +15 authors J. Hunter
- Chemistry, MedicineJournal of Pharmacology and Experimental…
- 1 July 2009
It is demonstrated that preladenant and SCH 412348 are potent and selective A2A receptor antagonists and provide further evidence of the potential therapeutic benefits of A 2A receptor inhibition in PD (with reduced risk of dyskinesias) and depression (one of the primary nonmotor symptoms of PD).
Examination of drug-induced and isolation-induced disruptions of prepulse inhibition as models to screen antipsychotic drugs
Results support the idea that non-drug induced disruptions of PPI, such as social isolation, may be a more viable approach to identify novel antipsychotics.
Centrally administered hemokinin-1 (HK-1), a neurokinin NK1 receptor agonist, produces substance P-like behavioral effects in mice and gerbils
HK-1 is an endogenous agonist at all of the known tachykinin receptors, and is selective for the NK1 receptor over the NK2 and NK3 subtypes, and a comprehensive expression analysis of HK-1 demonstrated that HK- 1 mRNA is much more broadly expressed than previously reported with expression observed in many brain regions.
The Gerbil Elevated Plus-maze II: Anxiolytic-like Effects of Selective Neurokinin NK1 Receptor Antagonists
It is demonstrated that neurokinin NK1 receptor antagonists produce anxiolytic-like effects in a novel gerbil elevated plus-maze, and suggested that this is an appropriate model to test NK1 antagonists for preclinical anxio-lytic activity.
Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders
- R. Hodgson, P. Bédard, +11 authors J. Hunter
- Medicine, PsychologyExperimental Neurology
- 1 October 2010
Data support the use of preladenant for the treatment of PD and antipsychotic-induced movement disorders and targets the A(2A) receptor antagonists for therapeutic potential in diseases of dopaminergic hypofunction.
M100907, a Serotonin 5-HT2A Receptor Antagonist and Putative Antipsychotic, Blocks Dizocilpine-Induced Prepulse Inhibition Deficits in Sprague–Dawley and Wistar Rats
These studies confirm the suggestion that serotonin and glutamate interact in modulating PPI and indicate that the 5-HT2A receptor subtype mediates this interaction.
Procognitive and antipsychotic efficacy of glycine transport 1 inhibitors (GlyT1) in acute and neurodevelopmental models of schizophrenia: latent inhibition studies in the rat
Preclinical data, from acute and neurodevelopmental models, suggest that GlyT1 inhibition may exhibit activity in the positive, negative, and cognitive symptom domains of schizophrenia.
The Gerbil Elevated Plus-Maze I: Behavioral Characterization and Pharmacological Validation
- G. Varty, C. Morgan, M. Cohen-Williams, V. Coffin, G. Carey
- Psychology, MedicineNeuropsychopharmacology
- 1 September 2002
These studies have demonstrated that gerbils exhibit an anxiety–like profile on an elevated plus-maze, and that the gerbil elevated Plus-Maze may have predictive validity for anxiolytics, and antidepressants with potential anxIOlytic-like effects.
Reversal of dizocilpine-induced disruption of prepulse inhibition of an acoustic startle response by the 5-HT2 receptor antagonist ketanserin.
The present studies suggest an interaction between 5-HT2 receptors and glutamatergic systems, which may be important for the antipsychotic profile of drugs having antagonist activity at 5- HT2 receptors.