Cannabinoids: novel medicines for the treatment of Huntington's disease.
Authors: Sagredo O, Pazos MR, Valdeolivas S, Fernandez-Ruiz J Abstract Cannabinoid pharmacology has experienced a notable increase in the last 3 decades which is allowing the development of novel cannabinoid-based medicines for the treatment of different human pathologies, for example, Cesamet® (nabilone) or Marinol® (synthetic Δ9-tetrahydrocannabinol for oral administration) that were approved in 80s for the treatment of nausea and vomiting associated with chemotherapy treatment in cancer patients and in 90s for anorexiacachexia associated with AIDS therapy. Recently, the british company GW Pharmaceuti...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Inhibitors of the endocannabinoid-degrading enzymes, or how to increase endocannabinoid's activity by preventing their hydrolysis.
Authors: Feledziak M, Lambert DM, Marchand-Brynaert J, Muccioli GG Abstract Endocannabinoids are lipid transmitters binding and activating the cannabinoid receptors. Both cannabinoid receptors and endocannabinoids, such as 2-arachidonoylglycerol and anandamide, have been shown to control numerous physiological and pathological processes, including in the central nervous system. Thus regulating endocannabinoid levels in-vivo represents an interesting therapeutic perspective in several CNS-related diseases. To date four enzymes - Fatty Acid Amide Hydrolase (FAAH), N-Acylethanolamine-hydrolyzing Acid Amidase ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Lipid-based nanocarriers for CNS-targeted drug delivery.
Authors: Micheli MR, Bova R, Magini A, Polidoro M, Emiliani C Abstract Nanotechnology exerts an increasing impact on the development of more effective tools for the diagnosis and treatment of human diseases. This applies in particular to central nervous system (CNS) disorders. Development of therapeutics for CNS is, in fact, one of the most challenging areas in drug development, mainly due to the presence of the blood-brain barrier (BBB) which separates the blood from the cerebral parenchyma thus limiting the brain uptake of the vast majority of neurotherapeutic agents. Among the several strategies which h...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

In this issue of Recent Patents on CNS Drug Discovery, focus is laid upon the potential development of new therapeutic drugs for neurological and affective disorders through targeting the endocannabinoid system. Introduction.
Authors: PMID: 22384488 [PubMed - indexed for MEDLINE] (Source: Recent Patents on CNS Drug Discovery)
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

The tachykinergic system as avenues for drug intervention.
This report discusses promising applications for targeting the NK receptors. The discussion proposes potential mechanisms that could occur when substance P interacts with HGFIN as well as the role of HGFIN when antagonists are used to block the NK receptors. This review is relevant for central and peripheral nervous system drug development and cancer targets and also discusses the indications for current patents. PMID: 22472024 [PubMed - indexed for MEDLINE] (Source: Recent Patents on CNS Drug Discovery)
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Nutraceuticals in psychiatric practice.
Authors: Chiappedi M, de Vincenzi S, Bejor M Abstract Nutraceuticals can be defined as food components or active principles present in aliments which have positive effects for health and quality of life, including preventing or treating disorders. Herbal and "natural" food supplements are increasingly used to treat different psychiatric disorders, often as "self-prescribed" therapies. 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...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Polyamine modulation of NMDARs as a mechanism to reduce effects of alcohol dependence.
Authors: Barron S, Lewis B, Wellmann K, Carter M, Farook J, Ring J, Rogers DT, Holley R, Crooks P, Littleton J Abstract Relapse and neurodegeneration are two of the major therapeutic targets in alcoholism. Fortuitously, the roles of glutamate/NMDA receptors (NMDARs) in withdrawal, conditioning and neurotoxicity mean that NMDAR inhibitors are potentially valuable for both targets. Preclinical studies further suggest that inhibitory modulators that specifically reduce the co-agonist effects of polyamines on NMDARs are potential non-toxic medications. Using agmatine as a lead compound, over 1000 novel compoun...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Cholinergic receptor system as a target for treating alcohol abuse and dependence.
Authors: Rahman S, Prendergast MA Abstract Alcohol dependence and other alcohol use disorders are major public health problems. Due to the limitations in efficacy with current medications for the management of alcohol abuse and dependence, there is a need for alterantive pharmacotherapies. Emerging preclinical and clinical data indicate that brain nicotinic acetylcholine receptors (nAChRs), a heterogeneous family of ion channels expressed in the mammalian brain, are critical targets for the development of pharmacotherapies for alcohol abuse and dependence. Evidence suggests that the effects of nAChR partia...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Novel medication targets for the treatment of alcoholism: preclinical studies.
Authors: Rezvani AH, Lawrence AJ, Arolfo MP, Levin ED, Overstreet DH Abstract Alcoholism is a complex heterogeneous disease and a number of neurotransmitter and neuromodulator systems have been implicated in its manifestation. Consequently, it is unlikely that existing medications such as disulfiram (Antabuse®), naltrexone (ReVia®), acamprosate (Campral®)) can be efficacious in every individual. Thus, the development of novel therapeutic agents with greater selectivity and less unwanted effects for the treatment of this disease is one of the major objectives of alcohol research. This review summarizes t...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

The development of medications for alcohol-use disorders targeting the GABAB receptor system.
Authors: Agabio R, Maccioni P, Carai MA, Gessa GL, Froestl W, Colombo G Abstract The present paper summarizes experimental and clinical data suggesting the therapeutic potential of the prototypic GABAB receptor agonist, baclofen, for the treatment of alcohol-use disorders (AUDs). Numerous studies have reported baclofen-induced suppression of alcohol drinking, relapse-like drinking, and alcohol reinforcing, rewarding, stimulating, and motivational properties in rats and mice. The majority of clinical surveys conducted to date have demonstrated the capacity of baclofen to suppress alcohol consumption, cravin...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Introduction to the special issue "Pharmacotherapies for the treatment of alcohol abuse and dependence" and a summary of patents targeting other neurotransmitter systems.
Authors: Bell RL, Franklin KM, Hauser SR, Zhou FC Abstract This paper introduces the Special Section: Pharmacotherapies for the Treatment of Alcohol Abuse and Dependence and provides a summary of patents targeting neurotransmitter systems not covered in the other four chapters. The World Health Organization notes that alcoholic-type drinking results in 2.5 million deaths per year, and these deaths occur to a disproportionately greater extent among adolescents and young adults. Developing a pharmacological treatment targeting alcohol abuse and dependence is complicated by (a) the heterogeneous nature of the...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Editorial: Pharmacotherapies for the treatment of alcohol abuse and dependence.
Authors: Zhou FC, Bell RL PMID: 22650966 [PubMed - indexed for MEDLINE] (Source: Recent Patents on CNS Drug Discovery)
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

The Nrf2-ARE pathway: a valuable therapeutic target for the treatment of neurodegenerative diseases.
Authors: Joshi G, Johnson JA Abstract Modulation of NF-E2 related factor 2 (Nrf2) has been shown in several neurodegenerative disorders. The overexpression of Nrf2 has become a potential therapeutic avenue for various neurodegenerative disorders such as Parkinson, Amyotrophic lateral sclerosis, and Alzheimer's disease. The expression of phase II detoxification enzymes is governed by the cis-acting regulatory element known as antioxidant response element (ARE). The transcription factor Nrf2 binds to ARE thereby transcribing multitude of antioxidant genes. Keap1, a culin 3-based E3 ligase that targets Nrf2 f...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Curcuminoids in neurodegenerative diseases.
Authors: Kim DS, Kim JY, Han Y Abstract Neurodegeneration is a term used to describe progressive deterioration of structure and/or function of neurons that affects different parts of the central nervous system and leads to eventual death. Neurodegenerative diseases include Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), Huntington's disease (HD), and Down's syndrome (DS), multiple sclerosis (MS), glaucoma, age-related macular degeneration (AMD), and diabetic encephalopathy (DE). Although the initial events that trigger these disorders may be different from each othe...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

In the rush for green gold: Can green tea delay age-progressive brain neurodegeneration?
Authors: Mandel SA, Youdim MB Abstract It is evident that brain aging engages changes in biological systems linked to synaptic function and cell metabolism and in the capacity to cope with different stresses that are either idiopathic in nature, or subject to environmental insults. In a substantial segment of the aging population there is a pathological transition to cognitive and behavioral dysfunction and thus, age constitutes the primary risk factor for Alzheimer's disease and other neurodegenerative disorders. To address the etiological complexity of aging and age-associated conditions, a new paradigm ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research