Current Pharmaceutical Design - Volume 20, Issue 32, 2014

N-methyl-D-aspartate receptor (NMDAR) serves for both high cortical function and fundamental CNS mechanisms. NMDAR-mediated neurotransmission is the molecular engine for CNS development and plasticity; it is also the molecular underpin of learning, memory and cognition. Due to its critical role in CNS function, either over- or under-activation of NMDAR-mediated neurotransmission contributes significantly to Read More

Schizophrenia, a multifactorial mental disorder with polygenic inheritance as well as environmental influences, encompasses a characteristic group of symptoms. Negative and cognitive symptoms which respond poorly to currently available antipsychotics remain a great clinical challenge. Aggressive studies are ongoing to explore the etiological mechanisms of this disease. Among them, one of the primary causal factors is Read More

Schizophrenia is a serious neuropsychiatric disease characterized by positive symptoms, negative symptoms and cognitive impairment. Evidence have shown that cognitive impairment sustains in every clinical stage, may relate with the liability, may predict functional outcome in schizophrenia and could be the core symptom of schizophrenia. The treatment of cognitive impairment in schizophrenia could alleviate the burden of t Read More

Schizophrenia and other psychiatric disorders are generally diagnosed based on a collection of symptoms defined by a combination of an individual’s feelings, perceptions, and behaviors. Many of these disorders are characterized by specific cognitive and social deficits. Although it is nearly impossible to recapitulate the full phenotypic spectrum of schizophrenia in mice, mouse models play an indispensable role in und Read More

Major depressive disorder (MDD) is a common, recurrent mental illness that affects millions of people worldwide. Accumulating evidence suggests that the N-methyl-D-aspartate (NMDA) receptor, a subtype of glutamate receptors, plays an important role in the neurobiology and treatment of this disease. Currently, the non-competitive NMDA receptor antagonist ketamine is considered as one of the most attractive candidate d Read More

The world population is growing older and age-related cognitive decline is becoming a burden of societal importance. D-serine is an endogenous amino acid that activates the co-agonist site of the NMDA-glutamate receptor, which is related to cognitive functions, such as learning and memory. Studies in aged rodents have shown a marked decrease in the levels of D-serine in brain regions such as the hippocampus, a key region Read More

The prevalence of Alzheimer’s disease (AD) in the elderly is growing rapidly worldwide, and the deteriorating clinical course of AD places a heavy burden on both the patients and their families. Early detection and intervention of mild cognitive impairment in the early phase of AD is vital for the purpose of improving the cognitive performance of patients and preventing the existing deficits from worsening. However, the main co Read More

Attention deficit hyperactivity disorder (ADHD) is a long recognized and common childhood disorder. ADHD adolescents tend to encounter more difficulties in school and peer relationships, whereas ADHD adults have more occupational and interpersonal difficulties. However, with the treatment of central nervous system (CNS) stimulants, 10-20 % of the patients still remain poor responders to treatment. Among hypoth Read More

Autism spectrum disorders (ASD) are developmental disorders that are characterized by deficits in reciprocal social interactions and communication, as well as by the presence of impairing repetitive behaviors and restricted interests. Prior work examining human pathology, and model systems and genetic studies have all led to the current conceptualization of ASD as a disorder of synaptic formation and functioni Read More

Synaptic plasticity is now known to occur at glutamate synapses throughout the brain, including the neocortex, and to play a role in neurodevelopment as well as in a broad spectrum of adult neural functions. Here the hypothesis that synaptic plasticity, specifically long term depression, is the neural substrate that mediates adolescent synaptic pruning is re-examined in the context of its ramifications for neuro Read More

In silico prediction of the new drug-target interactions from existing databases is of important value for the drug discovery process. Currently, the amount of protein targets that have been identified experimentally is still very small compared with the entire human proteins. In order to predict protein-ligand interactions in an accurate manner, we have developed a support vector machine (SVM) model based on the chemical-pr Read More

Glimepiride sulfonamide (GS) is a drug intermediate to synthesize glimepiride (antidiabetic drug). We hypothesized that GS exerts gluco-regulatory effect because GS is comprised of the structural components of dipeptidyl peptidase-IV (DPP-IV) inhibitors sitagliptin and DPP-728and glimepiride (sulfonylurea based antidiabetic drug).We analyzed the drug-likeness and docking efficiency of GS with DPP-IV using in silico tools. Also D Read More

Many tumors express one or more proteins that are either absent or hardly present in normal tissues, and which can be targeted by radiopharmaceuticals for either visualization of tumor cells or for targeted therapy. Radiopharmaceuticals can consist of a radionuclide and a carrier molecule that interacts with the tumor target and as such guides the attached radionuclide to the right spot. Radiopharmaceutic Read More