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Do we need a new procedure for the assessment of adverse events in anti-migraine clinical trials?
Authors: Amanzio M Abstract The large number of randomized controlled clinical trials on migraine have drawn the attention of some authors to the need to improve the design of such trials. In particular, adequate methodology is a critical issue in their planning and execution, as different methodological approaches can translate into different results. The side-effects observed in both the active medication arm and the placebo arm--considering anti-migraine randomized clinical trials--are often influenced by non specific factors. This issue can be quantified by using a systematic review approach to study t...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Patented in vitro blood-brain barrier models in CNS drug discovery.
Authors: Tóth A, Veszelka S, Nakagawa S, Niwa M, Deli MA Abstract The blood-brain barrier (BBB) is a regulatory interface between the circulation and the central nervous system (CNS). Therapy of neurological diseases is limited due to restricted penetration of pharmacons across the BBB. Models for screening the brain penetration of drug candidates are needed early in drug discovery. Culture-based models are useful tools for both basic research on BBB, and testing the permeability of new therapeutical molecules. This review focuses on patented in vitro BBB models and their potential application in CNS drug...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Potential drugs and methods for preventing or delaying the progression of Huntington's disease.
Authors: Sari Y Abstract Huntington's disease (HD) is an autosomal dominant inherited and progressive neurodegenerative disorder with motor dysfunction and cognitive deficits. Although there are no treatments to delay the appearance and the progression of HD, there are potential drugs currently in preclinical and clinical trials that are focused on HD therapy. The signaling pathways involved in HD are not yet clearly elucidated; however, expression of mutant huntingtin protein is considered a key factor in the induction and/or progression of HD. The demonstration that the onset and progression of HD in mod...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

BACE inhibitors as potential drugs for the treatment of Alzheimer's disease: focus on bioactivity.
Authors: Evin G, Lessene G, Wilkins S Abstract Current drug development for the treatment of Alzheimer's Disease is principally based on the amyloid cascade theory, and aims to reduce the levels of Aβ amyloid peptide in the brain. This can be achieved, either by decreasing peptide production through inhibition of β-secretase (also known as BACE-1) or γ-secretase, or by interfering with Aβ aggregation, or by promoting Aβ clearance. Targeting BACE-1, the proteolytic enzyme that initiates Aβ formation, has generated a lot of research interest recently and is currently thought to be one of the most promi...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Metoclopramide as an analgesic in severe migraine attacks: an open, single-blind, parallel control study.
Authors: Salazar G, Fragoso M, Vergez L, Sergio P, Cuello D Abstract Metoclopramide is a well-known anti-emetic drug with central and peripheral pharmacological effects. Some authors have reported metoclopramide as an adjunct therapy to other analgesics in patients with migraine attacks. Treatment of migraine headache using a mix of metoclopramide and an NSAID has been patented (European Patent EP1014961) as well as a short series showing great efficacy and tolerability of metoclopramide in patients wtih migraine attacks. We decided to conduct an open, single-blind, parallel control study in the emergency ...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Analgesic and antineuropathic drugs acting through central cholinergic mechanisms.
Authors: Bartolini A, Di Cesare Mannelli L, Ghelardini C Abstract The role of muscarinic and nicotinic cholinergic receptors in analgesia and neuropathic pain relief is relatively unknown. This review describes how such drugs induce analgesia or alleviate neuropathic pain by acting on the central cholinergic system. Several pharmacological strategies are discussed which increase synthesis and release of acetylcholine (ACh) from cholinergic neurons. The effects of their acute and chronic administration are described. The pharmacological strategies which facilitate the physiological functions of the choliner...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Promising medications for cocaine dependence treatment.
Authors: Somaini L, Donnini C, Raggi MA, Amore M, Ciccocioppo R, Saracino MA, Kalluppi M, Malagoli M, Gerra ML, Gerra G Abstract Cocaine dependence is characterized by compulsive drug seeking and high vulnerability to relapse. Overall, cocaine remains one of the most used illicit drugs in the world. Given the difficulty of achieving sustained recovery, pharmacotherapy of cocaine addiction remains one of the most important clinical challenges. Recent advances in neurobiology, brain imaging and clinical trials suggest that certain medications show promise in the treatment of cocaine addiction. The pharmacoth...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Recent approaches targeting beta-amyloid for therapeutic intervention of Alzheimer's disease.
Authors: Cho JE, Kim JR Abstract Alzheimer's disease (AD) is a neurodegenerative disorder characterized by neuropathological features comprising amyloid deposits and neuronal losses in brain. In AD, aggregation of a β amyloid peptide (Aβ), produced from proteolytic cleavage of amyloid precursor protein, is believed to be implicated in the pathophysiological cascade leading to neuronal death. Most AD drugs currently available can only alleviate symptoms rather than modify the underlying molecular cause of AD. In this review, we describe and discuss the recent patents issued within the past two years focus...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Pharmacological strategies against glucocorticoid-mediated brain damage during chronic disorders.
In conclusion, the spectrum of molecules interacting at the different levels of HPA axis is exponentially increasing, ranging from supra-hypothalamic targets to post-receptor mechanisms and it includes agents acting on SCN, CRH-R1 receptor, adrenal steroidogenesis, GR and peripheral/central 11β-HSD1 enzyme. This area of research is rapidly advancing in order to develop therapeutic strategies to counteract HPA axis hyperactivity and to reduce the burden of stress-related disorders. The article presented some promising patents on the strategies against glucocorticoid-mediated brain damage. PMID: 21834781 [PubMed - i...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Neurogenic ejaculatory disorders: focus on current and future treatments.
Authors: Calabrò RS, Polimeni G, Ciurleo R, Casella C, Bramanti P Abstract Ejaculation is a complex and still poorly understood neurological mechanism, at both spinal and cerebral levels as it is closely associated with orgasm. Physiologically, ejaculation is defined as the expulsion of seminal fluid from the urethral meatus and consists of two phases, namely emission and expulsion. Ejaculation is mediated by a spinal control center, referred to as a spinal pattern generator that coordinates sympathetic, parasympathetic and motor (somatic) outflows, integrating the latter with the inputs from the supraspi...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

An update in the management of obesity: the weight of CNS targets.
Authors: Bariohay B, Roux JA, Bonnet MS, Dallaporta M, Troadec JD Abstract Obesity is one of the most important and disturbing global epidemic that affects humans, with more than 2 billion people overweight and 700 million obese predicted for 2015 by the World Health Organization. Obesity treatment represents then one of the most exciting challenges for the academic researchers and the pharmaceutical industry. But to date, this community failed to develop safe and effective treatments with a good risk/benefit profile. Indeed, most of the drugs previously used as anti-obesity agents have been withdrawn from...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Role of diagnostic ultrasound in patient selection for stroke intervention.
Authors: Sharma VK, Paliwal PR, Teoh HL, Venketasubramanian N, Chan BP Abstract Ultrasonography provides a unique diagnostic perspective in cerebrovascular disorders, with extremely high temporal resolution and excellent spatial display of extracranial as well as intracranial arteries. Unlike other imaging modalities, cerebrovascular ultrasound provides real-time information about the blood flow in addition to the hemodynamic changes as a result of various physiological as well as pathological states. The information obtained from cerebrovascular ultrasound has diagnostic, therapeutic as well as prognostic...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Editorial [hot topic: cannabinoid receptors ligands (guest editor: Gabriele Murineddu)].
Authors: Murineddu G PMID: 22280337 [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

A survey of recent patents on CB2 agonists in the management of pain.
Authors: Murineddu G, Asproni B, Pinna GA Abstract Pain, a homeostatic and protective mechanism which can go awry in disease states and therefore needs treatment, is a complex and differentiated sensorial perception which may be classified as physiological, inflammatory and neuropathic. Chronic pain represents a major health problem throughout the world, thus several companies and researchers have embarked on the search for new drugs and targets to treat the disease. The different types of receptors in the CNS involved in the mediation of analgesia include the cannabinoid receptors: in particular, CB2 modu...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research

Cannabinoid-related agents in the treatment of anxiety disorders: current knowledge and future perspectives.
Authors: Tambaro S, Bortolato M Abstract Rich evidence has shown that cannabis products exert a broad gamut of effects on emotional regulation. The main psychoactive ingredient of hemp, Δ9-tetrahydrocannabinol (THC), and its synthetic cannabinoid analogs have been reported to either attenuate or exacerbate anxiety and fear-related behaviors in humans and experimental animals. The heterogeneity of cannabis-induced psychological outcomes reflects a complex network of molecular interactions between the key neurobiological substrates of anxiety and fear and the endogenous cannabinoid system, mainly consisting...
Source: Recent Patents on CNS Drug Discovery - November 20, 2014 Category: Drugs & Pharmacology Tags: Recent Pat CNS Drug Discov Source Type: research