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- Volume 4, Issue 2, 2004
Current Medicinal Chemistry - Central Nervous System Agents - Volume 4, Issue 2, 2004

Volume 4, Issue 2, 2004
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5-HT3 Serotonin Receptor Agonists: A Pharmacophoric Journey
More LessIt has been nearly 50 years since Gaddum and Picarelli characterized serotonin M-receptors using an isolated guinea pig ileum preparation; M-receptors, known today as 5-HT3 receptors, are just one of about fifteen different types of serotonin receptors. The discovery of this new class of serotonin receptors evoked a necessity for new ligands to study their pharmacological activity. Today, several 5-HT3 ligands are employe Read More
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New Trends in the Development of Positive Allosteric Modulators of AMPA Receptors
Authors: E. Graindorge, P. Francotte, S. Boverie, P. d. Tullio and B. PirotteThe 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propanoic acid (AMPA) receptors, a subtype of glutamate receptors, are involved in important neuronal functions such as long-term memory. A decrease of the number and activity of these receptors seems to play a role in schizophrenia and in the impairment of cognitive function associated to Alzheimer's disease. Therefore, research has been focused on the development of Read More
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Signal Pathways Mediating Antidepressant and Antipsychotic Drugs on Neuronal Cell Survival
Authors: Anke Post, Osborne F.X. Almeida and Florian HolsboerAntidepressants and antipsychotic drugs comprise the most common groups of prescribed drugs in psychiatry. Despite their efficacy in terms of remission of the primary clinical symptoms, many of them are associated with neurotoxic effects in experimental settings: tricyclic antidepressants and, in particular, typical neuroleptics have been causally linked to neuronal death in vitro that may account for the extrapyramidal effe Read More
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Primary and Secondary Insomnia: Prevalence, Causes and Current Therapeutics
More LessSleep-related complaints are common in the general population. Prevalence rates are significantly higher among women and the older age groups. About 10% of those experiencing insomnia state that the complaint is chronic. Chronic primary insomnia results from the reaction to an emotional trigger or stressful event, which leads to the further development of sleep-preventing associations. Chronic secondary insomnia is that r Read More
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Pompilidotoxins: Novel Peptide Neurotoxins Blocking Sodium Channel Inactivation from Solitary Wasp Venom
Authors: Katsuhiro Konnoa and Nobufumi KawaiSolitary wasps are known to inject their venoms into insects or spiders and paralyze the prey to feed their larvae. Therefore, the solitary wasp venoms should contain a variety of components acting on nervous systems. Until recently, however, only a few solitary wasp venoms have been studied. We have surveyed bioactive substances in solitary wasp venoms and recently found novel peptide neurotoxins, α- and β-pompili Read More
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Glutamate Hypothesis of Schizophrenia and Approach for Possible Therapeutic Drugs
Authors: Kenji Hashimoto, Naoe Okamura, Eiji Shimizu and Masaomi IyoL-Glutamic acid (glutamate) is a major excitatory amino acid in the nervous system, and it is known that glutamate plays a major role in brain development, affecting neuronal migration, neuronal differentiation, axon genesis, and neuronal survival. Several lines of evidence suggest that a dysfunction in glutamatergic neurotransmission via the Nmethyl- D-aspartate (NMDA) subtype of glutamate receptors might be involved Read More
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