An update on peptide drugs for voltage-gated calcium channels.
Authors: Gao L Abstract Voltage-gated calcium channels are one of the major ion channels distributed in the human central nervous system, and mediate an influx of extracellular Ca(2+) in response to membrane depolarization. Calcium channels are of particular interest in a broad range of cellular functions including cell proliferation and differentiation, gene expression, neurite outgrowth, transmitter and hormone release, and brain plasticity. The dysfunction of calcium channels is related to a variety of clinical disorders such as migraine, hemiplegia, and epilepsy. Therefore, calcium channels have gained...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Toward the management of inflammation: recent developments of mPGES-1 inhibitors.
Authors: Dallaporta M, Pecchi E, Thirion S, Jean A, Troadec JD Abstract For decades, the struggle against inflammation and related disorders has constituted an important field in medical practice, with strategies mainly aimed at inhibiting compounds produced through the arachidonic acid pathway. Thus, specific COX-2 inhibitors or "coxibs", were recently designed, that play an increasing but controversial role in reducing inflammatory phenomenon. Lately, several patents have been generated which target the specific inhibition of the microsomal Prostanglandin E synthase-1 (mPGES-1). This enzyme, which was cl...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

New frontiers in alcoholism and addiction treatment.
Authors: Nava F, Vendramin A, Manzato E, Cibin M, Lucchini A Abstract Drug addiction and alcoholism are behavioural disorders characterized by a profound alteration of several brain circuits induced by chronic drug use. Their treatment is yet based on empiricism and today only few pharmacological strategies are fully effective to control both drug use and relapse. The present paper reviews the most updated pharmacotherapies able to contrast both alcoholism and drug addiction including the new patented drugs and the future therapeutic trends. PMID: 19751210 [PubMed - indexed for MEDLINE] (Source: Re...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Pharmacology and toxicology of Cannabis derivatives and endocannabinoid agonists.
Authors: Gerra G, Zaimovic A, Gerra ML, Ciccocioppo R, Cippitelli A, Serpelloni G, Somaini L Abstract For centuries Cannabis sativa and cannabis extracts have been used in natural medicine. Delta(9)-tetrahydrocannabinol (THC) is the main active ingredient of Cannabis. THC seems to be responsible for most of the pharmacological and therapeutic actions of cannabis. In a few countries THC extracts (i.e. Sativex) or THC derivatives such as nabilone, and dronabinol are used in the clinic for the treatment of several pathological conditions like chemotherapy-induced nausea and vomiting, multiple sclerosis and gl...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Highly pure phospholipids based brain docosahexaenoic acid transporters.
Authors: Chen S Abstract The most common age-dependent neurodegenerative disorders such as dementia and Alzheimer's disease have become an urgent public health problem in the most areas of the world. The strategy of the current therapy focuses on increasing availability of brain acetylcholine concentration, and use of acetylcholinesterase inhibitors has become the main approach to symptomatic treatment. However, an ideal drug for the disorders should enable to both simultaneously delay or halt the underlying pathological process and improve memory. The present paper describes an alterative cholinergic stra...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Antisense oligonucleotides as innovative therapeutic strategy in the treatment of high-grade gliomas.
Authors: Caruso G, Caffo M, Raudino G, Alafaci C, Salpietro FM, Tomasello F Abstract Despite the intensive recent research in cancer therapy, the prognosis in patients affected by high-grade gliomas is still very unfavorable. The efficacy of classical anti-cancer strategies is seriously limited by lack of specific therapies against malignant cells. The extracellular matrix plays a pivotal role in processes such as differentiation, apoptosis, and migration in both the normal and the pathologic nervous system. Glial tumors seem to be able to create a favorable environment for the invasion of glioma cells in ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Recent patents on positive allosteric modulators of the metabotropic glutamate 5 receptor as a potential treatment for schizophrenia.
Authors: Kanuma K, Aoki T, Shimazaki Y Abstract The glutamate hypothesis of schizophrenia suggests that hypofunction of N-methyl-D-aspartate (NMDA) receptors may be critical for schizophrenic symptoms; therefore, pharmacological approaches that enhance NMDA function may be beneficial for the treatment of schizophrenia. Several lines of evidence indicate that NMDA and metabotropic glutamate (mGlu) 5 receptors are closely associated signaling partners and that a selective mGlu5 receptor agonist might provide a viable approach for increasing NMDA receptor function in the treatment of schizophrenia. The orthos...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

New perspectives for the diagnosis of Alzheimer's disease.
Authors: Urbanelli L, Magini A, Ciccarone V, Trivelli F, Polidoro M, Tancini B, Emiliani C Abstract Alzheimer's disease is the most common cause of dementia in the elderly. Currently its clinical assessment is based on the exclusion of other forms of dementia and a definitive diagnosis requires a confirmation by examination of post-mortem brains. Therefore, there is a strong need to find easy measurable AD biomarkers that could facilitate the early diagnosis and monitoring the efficacy of the few therapies currently available. This would favor the development of further therapeutic approaches. Recently, do...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Transcription factors as therapeutic targets in CNS disorders.
Authors: Kane MJ, Citron BA Abstract Disorders affecting the central nervous system frequently involve programmed neuronal loss. There are well-established changes in gene expression that occur in neurodegenerative diseases, and traumatic and ischemic injuries. Yet, we currently lack sufficient knowledge of the underlying mechanisms leading to the altered gene expression profiles affecting cell survival in the brain and spinal cord. The cell loss is accelerated by the induction of pro-cell death gene expression profiles through an altered balance of pro- and anti-apoptotic transcription factors. Dysregulat...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Therapeutic approaches of leptin in Alzheimer's disease.
Authors: Carro EM Abstract Novel approaches in the understanding of the neurodegeneration observed in Alzheimer's disease (AD), involving neurochemical as well as biochemical techniques are being developed, opening up new possibilities in the direction of a metabolic degeneration. Indeed, brain lipids are closely involved in amyloid beta-related pathogenic pathways. An important modulator of lipid homeostasis is the pluripotent peptide leptin, which has been shown to reduce amyloid beta levels and tau-related pathological pathways, the major pathological hallmarks of AD. These data suggest that leptin hold...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Anti-copper therapies in Alzheimer's disease: new concepts.
Authors: Squitti R, Zito G Abstract Alzheimer's disease (AD) is a heterogeneous and progressive neurodegenerative disorder. The recent Metal Hypothesis states that the interaction of Amyloid beta (Abeta, the main constituent of senile plaques) with transition metals is at the basis of AD neurodegeneration. This hypothesis is based on in vitro studies demonstrating that metals (copper, zinc) accelerate the aggregation and precipitation into plaques of Abeta, ultimately leading to synaptic dysfunction and accelerated amyloidogenesis. Recently, we have identified in AD patients a specific 'copper disease' mar...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Novel therapies for schizophrenia: understanding the glutamatergic synapse and potential targets for altering N-methyl-D-aspartate neurotransmission.
Authors: Hui C, Wardwell B, Tsai GE Abstract For over fifteen years, N-methyl-D-aspartate receptor (NMDAR) mediated glutamatergic neurotransmission has generated interest because of its putative role in the pathophysiology of schizophrenia. Thus far, all antipsychotic medications have centered on manipulating the dopamine receptor to treat psychosis. These medications have limited efficacy, especially in treating the cognitive and negative symptoms of schizophrenia, and serious side effects. The NMDAR now provides an entirely new array of targets around which to focus new drug development. This paper first...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Role of dietary polyphenols in attenuating brain edema and cell swelling in cerebral ischemia.
Authors: Panickar KS, Anderson RA Abstract Polyphenols are natural substances with variable phenolic structures and are enriched in vegetables, fruits, grains, bark, roots, tea, and wine. There are over 8000 polyphenolic structures identified in plants, but edible plants contain only several hundred polyphenolic structures. Recent interest in polyphenols has increased greatly due to their potential antioxidant effects. In addition, some polyphenols also have insulin-potentiating, anti-inflammatory, anti-carcinogenic, anti-viral, anti-ulcer, and anti-apoptotic properties although some of these properties ma...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Herbals and natural dietary supplements in psychiatric practice.
Authors: Chiappedi M, Bejor M Abstract There is some evidence that links the increase of mental disorders' prevalence with a deterioration of Western countries' nutritional habits and it is found that the use of herbal and "natural" food supplements to treat different disorders is increasing. With factors such as chronic illness, poor health, emotional distress, and quality of life influencing the desire for complementary medicine, patients with comorbid medical and psychiatric problems seem likely to turn to this approach. We reviewed the most commonly used herbal and dietary supplements for which a certa...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

The injured cochlea as a target for inflammatory processes, initiation of cell death pathways and application of related otoprotectives strategies.
Authors: Abi-Hachem RN, Zine A, Van De Water TR Abstract One of the causes of sensorineural hearing loss is the loss of auditory hair cells following exposure to environmental stresses. Auditory hair cell death in response to cochlear trauma occurs via both necrosis and apoptosis. Apoptosis of hair cells involves the caspase and MAPK/JNK pathways which are activated by oxidative stress and secretion of inflammatory cytokines in response to trauma. Identification of the pathways that lead to apoptosis provides therapeutic targets for the conservation of hearing. Antioxidants reduce the level of reactive oxy...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research