202 results match your criteria Recent Patents on CNS Drug Discovery [Journal]


Editorial (Thematic Issue: From Old Cannabinoids to Emerging New Synthetic Derivatives with Potential Therapeutic Application in Neurological Disorders).

Authors:
Anna M Malfitano

Recent Pat CNS Drug Discov 2016 ;10(2):75

Dep. of Medicine and Surgery, University of Salerno, Italy.

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September 2018
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Beyond the Direct Activation of Cannabinoid Receptors: New Strategies to Modulate the Endocannabinoid System in CNS-Related Diseases.

Recent Pat CNS Drug Discov 2016 ;10(2):122-141

Institute of Biochemistry and Molecular Medicine, National Center of Competence in Research TransCure, University of Bern, CH 3012 Bern, Switzerland.

Background: Anandamide (AEA) and 2-arachidonoyl glycerol (2-AG) are signalling lipids which belong to the class of endocannabinoids (ECs) and exert their actions by activating cannabinoid receptor type-1 (CB1) and type-2 (CB2). These receptors are involved in many physiological and pathological processes in the central nervous system (CNS) and in peripheral organs. Despite many potent and selective ligands for cannabinoid receptors have been generated over the last two decades, this class of compounds achieved only a very limited therapeutic success, mainly because of the CB1- mediated side effects. Read More

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July 2017
4 Reads

Endocannabinoid System in Neurological Disorders.

Recent Pat CNS Drug Discov 2016 ;10(2):90-112

Department of Medicine and Surgery, University of Salerno, Via Salvatore Allende, Baronissi, 84081 Salerno, Italy and Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 84084 Fisciano (Salerno)- Italy.

Background: Several studies support the evidence that the endocannabinoid system and cannabimimetic drugs might have therapeutic potential in numerous pathologies. These pathologies range from neurological disorders, atherosclerosis, stroke, cancer to obesity/metabolic syndrome and others.

Methods: In this paper we review the endocannabinoid system signaling and its alteration in neurodegenerative disorders like multiple sclerosis, Alzheimer's disease, Parkinson's disease and Huntington's disease and discuss the main findings about the use of cannabinoids in the therapy of these pathologies. Read More

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July 2017
12 Reads

Cannabimimetic Drugs: Recent Patents in Central Nervous System Disorders.

Recent Pat CNS Drug Discov 2016 Jun 19. Epub 2016 Jun 19.

Department of Medicine and Surgery, University of Salerno, Via Salvatore Allende, Baronissi, 84081 Salerno, Italy.

Agents acting via cannabinoid receptors have been widely developed; starting from the chemical structure of phytocannabinoids isolated from cannabis sativa plant, specific and selective compounds of these receptors have been produced ranging from partial to full agonists and /or antagonists endowed with different potency. The enhanced interest on developing such classes of drugs is due to the beneficial properties widely reported by both anecdotal reports and scientific studies describing the potential medicinal use of cannabinoids and their derivatives in numerous pathological conditions in both in vitro and in vivo models. The use of these drugs has been found to be of benefit in a wide number of neurological and neuropsychiatric disorders, and in many other diseases ranging from cancer, atherosclerosis, stroke, hypertension, inflammatory related disorders, and autoimmune diseases, just to mention some. Read More

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Cannabinoids and Neuro-Inflammation: Regulation of Brain Immune Response.

Recent Pat CNS Drug Discov 2016 ;10(2):178-203

Department of Medicine and Surgery, University of Salerno, Via Salvatore Allende, Baronissi, 84081 Salerno, Italy and Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 84084 Fisciano (Salerno)- Italy.

Background: Cannabinoid receptors are involved in the neuro-pathogenic mechanisms of inflammatory conditions of the central nervous system and their expression can be modulated during diseases.

Methods: In this manuscript we highlight the function of cannabinoid receptors, their signalling and expression at peripheral and central levels in order to understand their implication in neuro-inflammation and review the effects of cannabinoids in neuro-inflammatory disorders.

Results: Brain inflammatory processes are characterized by infiltration of numerous types of cells: both peripheral and brain resident immune cells and other neuronal cells. Read More

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July 2017
11 Reads

Neuropharmacological Properties of Withania somnifera - Indian Ginseng: An Overview on Experimental Evidence with Emphasis on Clinical Trials and Patents.

Recent Pat CNS Drug Discov 2016 ;10(2):204-215

DBT-Visiting Research Professor, Drosophila Neurobiology laboratory, Department of Zoology, Nagaland University (Central), Lumami, 798627, Nagaland, India.

Background: Owing to the increasing aged population globally, disorders and diseases of the CNS are anticipated to increase and profoundly impact the health care. As these neurodegenerative diseases (NDD) are complex, multifactorial and do not have identified etiological factors, unfortunately, drugs developed for the purpose have not met with the expected success. Hence, there has been a constant demand for the development of natural therapeutic adjuvants which are safe and possess the potential to attenuate multiple pathways. Read More

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July 2017
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Synthetic Cannabinoid Receptor Agonists and Antagonists: Implication in CNS Disorders.

Recent Pat CNS Drug Discov 2016 ;10(2):142-156

Department of Pharmacy, University of Pisa, via Bonanno 6, 56126 Pisa, Italy.

Background: Since the discovery of the cannabinoid receptors, numerous studies associate the endocannabinoid system with several physiological and pathological processes including cancer, appetite, fertility, memory, neuropathic and inflammatory pain, obesity, and neurodegenerative diseases. Over the last two decades, several researches have been dedicated extensively on the cannabinoid receptors ligands since the direct activation of cannabinoid receptors results in several beneficial effects, in the brain and in the periphery. The cannabinoid CB1 and CB2 receptor synthetic ligands reported in this review have been collected by a wide research of scientific literature in particular in public database for patents and clinical trials. Read More

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July 2017
26 Reads

Phytocannabinoids and Cannabimimetic Drugs: Recent Patents in Central Nervous System Disorders.

Recent Pat CNS Drug Discov 2016 ;10(2):157-177

Department of Medicine and Surgery, University of Salerno, Via Salvatore Allende, Baronissi, 84081 Salerno, Italy and Department of Pharmacy, University of Salerno, Via Giovanni Paolo II 84084 Fisciano (Salerno)- Italy.

Background: Starting from the chemical structure of phytocannabinoids, isolated from Cannabis sativa plant, research groups designed numerous cannabimimetic drugs. These compounds according to their activities can be partial, full agonists and antagonists of cannabinoid receptors. Anecdotal reports and scientific studies described beneficial properties of cannabinoids and their derivatives in several pathological conditions like neurological and neuropsychiatric disorders, and in many other diseases ranging from cancer, atherosclerosis, stroke, hypertension, inflammatory related disorders, and autoimmune diseases. Read More

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July 2017
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Peptide Agonists and Antagonists with Potential Application in Neurological Disorders.

Recent Pat CNS Drug Discov 2016 ;10(2):76-89

Department of Pharmacy, CIRPEB: Centro Interuniversitario di Ricerca sui Peptidi Bioattivi- University of Naples "Federico II", 80134, Naples, Italy.

Background: Peptides are usually used to investigate regulatory networks and protein function. They can also be used in therapeutic research: They are employed both to identify and later to validate therapeutical target and in drug discovery processes. Their development enables the identification of several protein surfaces as crucial therapeutic targets and to promote the discovery of small drugs specific for these molecular interfaces. Read More

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July 2017
4 Reads

Immuno-Modulatory Properties of a Quinolin-2-(1H)-on-3-Carboxamide Derivative: Relevance in Multiple Sclerosis.

Recent Pat CNS Drug Discov 2016 ;10(2):113-121

Background: We have recently released the structure of a class of quinolin-2-(1H)-on-3-carboxamide derivatives and among them; the drug A2 has the highest CB2 receptor selectivity.

Objective: In this work we assessed the immuno-modulatory properties of A2 in lymphocytes isolated from peripheral blood of multiple sclerosis patients and healthy donors.

Methods: Cell proliferative response was measured by 3H-thymidine incorporation, cell viability and apoptosis by trypan blue, annexin V staining and western blot. Read More

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Opinion Paper: Post-surgical Delirium, Consciousness, and Therapy.

Authors:
Miao-Kun Sun

Recent Pat CNS Drug Discov 2015 ;10(1)

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April 2016
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Exosome-based strategies for Diagnosis and Therapy.

Recent Pat CNS Drug Discov 2015 ;10(1):10-27

University of Perugia, Department of Chemistry, Biology and Biotechnology Via del Giochetto, Perugia, Italy.

Exosomes are small extracellular vesicles (30-120 nm) of endosomal origin, which are gaining the attention of the scientific community. Originally considered only a waste disposal system, they are now emerging as another class of signal mediators. Exosomes are secreted by any cell type and retrieved in every body fluid, such as blood, urine, saliva and amniotic liquid. Read More

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April 2016
3 Reads

Reperfusion Therapies in Acute Ischemic Stroke.

Recent Pat CNS Drug Discov 2015 ;10(1):45-54

Division of Neurology, Department of Medicine, 5 Lower Kent Ridge Road, National University Hospital, Singapore 119074.

Acute Ischemic stroke (IS) remains a leading cause of mortality and long-term disability. Owing to the time-constraints, only a fraction of acute IS patients receive the established and approved thrombolytic therapy and a sizeable proportion of acute IS stroke survivors remain permanently disabled. Rapid advances in various recanalization strategies have aimed at improving functional outcome and reducing mortality. Read More

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April 2016
5 Reads

Scientific Prediction and Prophetic Patenting in Drug Discovery.

Recent Pat CNS Drug Discov 2015 ;10(1):34-44

P.O. Box 24733, Rochester, NY 14624, USA.

Pharmaceutical patenting involves writing claims based on both discoveries already made, and on prophesy of future developments in an ongoing project. This is necessitated by the very different timelines involved in the drug discovery and product development process on the one hand, and successful patenting on the other. If patents are sought too early there is a risk that patent examiners will disallow claims because of lack of enablement. Read More

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April 2016
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Histamine H₄ Receptor Antagonists: A New Approach for Tinnitus Treatment?

Recent Pat CNS Drug Discov 2015 ;10(1):6-9

Heinrich Heine University, Institute of Pharmaceutical and Medicinal Chemistry, Universitaetsstr. 1, 40225 Duesseldorf, Germany.

Tinnitus, a disorder with disruptive sound perception in the head without an external source, affects around 15 % of the worldwide adult population. Since there is no approved drug for the treatment for this symptom, novel strategies need to be developed to provide relief for the patient. A patent from the small French start-up company Sensorion suggests the use of histamine H4 receptor (H4R) inhibitors as potential treatment. Read More

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April 2016
3 Reads

Midkine and Pleiotrophin in the Treatment of Neurodegenerative Diseases and Drug Addiction.

Recent Pat CNS Drug Discov 2015 ;10(1):28-33

Lab. Pharmacology, Faculty of Pharmacy, Universidad CEU San Pablo, Urb. Montepríncipe, 28668 Boadilla del Monte, Madrid, Spain.

Pleiotrophin (PTN) and Midkine (MK) are neurotrophines with documented protective actions in experimental models of neurodegenerative diseases and beneficial effects on toxicity and addictive behaviours related to drug abuse. Concerning the latter, both PTN and MK prevent the neurotoxic effects of amphetamine on nigrostriatal pathways and endogenous PTN also limits amphetamine reward. Moreover, endogenous PTN overexpression in the prefontral cortex abolishes alcohol- induced conditioned place preference. Read More

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April 2016
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The Prevention and Treatment of Delirium in Elderly Patients Following Hip Fracture Surgery.

Recent Pat CNS Drug Discov 2015 ;10(1):55-64

S.Andrea Hospital, Via di Grottarossa 1035, 00189 Rome, Italy.

Osteoporotic hip fracture needs a specific approach and treatment, since elderly patients are at high risk for adverse outcomes after surgery. In particular, delirium often occurs in the peri-operative period, and it is associated with death, hospital-acquired complications, persistent cognitive impairments, poor functional recovery after surgery and increased healthcare costs. The pre-operative assessment of the risk factors for delirium improves the preventive measures. Read More

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April 2016
14 Reads

Treatment of chronic migraine with intramuscular pericranial injections of onabotulinumtoxin a.

Recent Pat CNS Drug Discov 2014 ;9(3):181-92

Department of Neurology, Quiron Dexeus University Hospital, C/ Sabino Arana Nº 5-19, 08028 Barcelona, Spain.

Chronic migraine is the most frequent and disabling complication of migraine. To date, only two drugs have been specifically analysed for the treatment of chronic migraine, topiramate and onabotulinumtoxin A, and in the evidence-based medicine categories, they have achieved level of evidence I and as such, a grade of recommendation A according to current guidelines. Following the PREEMPT paradigm, pericranial intramuscular onabotulinumtoxin A injections show a good efficacy and safety in chronic migraine patients, both in phase III randomized clinical trials and in a pooled data analyses. Read More

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November 2015
2 Reads

Pathophysiology and treatment of nonfamilial hyperparathyroidism.

Recent Pat CNS Drug Discov 2014 ;9(3):164-72

Department of Surgery, Oncology and Gastroenterology (DiSCOG), University of Padua, School of Medicine, via Giustiniani 2, 35128 Padova, Italy.

Primary hyperparathyroidism (HPT) is the main cause of hypercalcemia and the most common parathyroid glands disease. The diagnosis is easy in patients with hypercalcemia and elevated PTH serum level. Minimally invasive parathyroidectomy (PTx) represents the treatment of choice for symptomatic patients, leading to several advantages, including immediate normalization of hypercalcemia and significant improvement of bone mineral density, cardiovascular dysfunctions, neuropsychological symptoms and quality of life. Read More

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November 2015
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Liver growth factor as a tissue regenerating factor in neurodegenerative diseases.

Recent Pat CNS Drug Discov 2014 ;9(3):173-80

Servicio de Neurobiologia- Investigacion, Instituto Ramon y Cajal de Investigacion Sanitaria (IRYCIS). Madrid, 28034, Spain.

Liver growth factor (LGF) is a hepatic mitogen purified by our group in 1986. In the following years we demonstrated its activity both in "in vivo" and "in vitro" systems, stimulating hepatocytes mitogenesis as well as liver regeneration in several models of liver injury. Furthermore, we established its chemical composition (albumin-bilirubin complex) and its mitogenic actions in liver. Read More

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4485410PMC
November 2015
7 Reads

Drug-drug interactions: antiretroviral drugs and recreational drugs.

Recent Pat CNS Drug Discov 2014 ;9(3):153-63

Department of Neurology, Annunziata Hospital, Via F. Migliori, 1 - 87100 Cosenza, Italy.

With the advances in antiretroviral (ARV) therapy, patients with Human Immunodeficiency Virus (HIV) infection are living longer, however, some patients encounter co- morbidities which sometimes require treatment. Therefore, during the treatment with ARV drugs these patients could take several recreational drugs (e.g. Read More

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November 2015
17 Reads

Pharmacological approaches to targeting muscarinic acetylcholine receptors.

Recent Pat CNS Drug Discov 2014 ;9(2):85-100

Dept. of Biology and Biotechnologies Charles Darwin, Research Center of Neurobiology Daniel Bovet, Sapienza, University of Rome, P.le A. Moro, 5 - 00185 Roma, Italy.

The presence of cholinergic system markers and muscarinic receptor subtypes in several tissues also of nonneuronal type has been largely demonstrated. Acetylcholine, synthesized in the nervous system, can locally contribute to modulate cell proliferation, survival and apoptosis. Considering that the cholinergic system functions are impaired in a number of disorders, the identification of new drugs regulating these functions appears of great clinical relevance. Read More

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August 2015
3 Reads

Possible physiopathological effects of the transglutaminase activity on the molecular mechanisms responsible for human neurodegenerative diseases.

Recent Pat CNS Drug Discov 2014 ;9(2):76-84

Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via Costantinopoli 16, 80138 Naples, Italy.

Transglutaminases are a class of ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). Read More

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Advancing drug therapy for brain tumours: a current review of the pro-inflammatory peptide Substance P and its antagonists as anti-cancer agents.

Recent Pat CNS Drug Discov 2014 ;9(2):110-21

Division of Health Sciences, University of South Australia, South Australia, 5001, Australia.

Evidence for the involvement of the Substance P (SP)/NK1 receptor system in the development and progression of cancer strongly supports its potential as a therapeutic target in malignancies. Novel strategies for approaching cancer treatment are urgently required particularly with regard to tumours of the central nervous system (CNS), which are notoriously difficult to effectively treat and associated with extremely poor prognosis for many patients. This is due, in part, to the presence of the highly specialised blood-brain barrier, which is known to restrict common treatments such as chemotherapy and hinder early tumour diagnosis. Read More

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August 2015
15 Reads

Patents on potential drugs to treat Alzheimer's disease: special emphasis on small peptides.

Recent Pat CNS Drug Discov 2014 ;9(2):71-5

Recombinant Technologies, LLC, 1090 Meriden Waterbury Road, Suite 1, Cheshire, CT 06410, USA.

The primary objective of this article is to review patents and the related scientific work on naturally occurring compounds, heterocyclic compounds and small peptides that are being explored for their utility for the treatment of Alzheimer's disease (AD). In this review, a special emphasis is given to the patents, including our patent issued in 2013, on peptides that bind to A. Utility of the peptides that prevent aggregation or those that help in clearance of Aβ is discussed as the latter can be considered as an important arm in combination therapy for AD. Read More

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August 2015
6 Reads

Possible physiopathological roles of the transglutaminase activity in the etiopathogenesis of human neurodegenerative diseases.

Recent Pat CNS Drug Discov 2014 ;9(2):101-9

Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via Costantinopoli 16, 80138 Naples, Italy.

Transglutaminases are ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). Read More

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Recent patents on novel MCH1 receptor antagonists as potential anti-obesity drugs.

Recent Pat CNS Drug Discov 2014 ;9(2):122-40

Gyomroi u. 24, 1103 Budapest, Hungary.

Today, the 'obesity pandemic' is one of the biggest health issues around the world. Melanin-concentrating hormone (MCH), a hypothalamic neuropeptide, is one of the most potent, central stimulators of feeding and it also attenuates energy expenditure. Inhibitions of the MCH receptor, the melanin-concentrating hormone receptor-1 (MCHR1), has attracted considerable attention as a potential anti-obesity drug, during the last decade. Read More

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August 2015
11 Reads

This first 2014 issue of Recent Patents in CNS Drug Discovery covers a range of rather diverse, but not necessarily unrelated topics. Introduction.

Recent Pat CNS Drug Discov 2014 Apr;9(1)

Endocannabinoid Research Group (ERG) Institute of Biomolecular Chemistry Consiglio Nazionale delle Ricerche Via Campi Flegrei 34 Comprensorio Olivetti 80078 Pozzuoli (NA) Italy.

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April 2014
2 Reads

Treatment of insulin resistance in the neurodegeneration.

Recent Pat CNS Drug Discov 2014 Apr;9(1):54-63

S.Andrea Hospital, Sapienza University of Rome, Via di Grottarossa 1035, 00189 Rome, Italy.

The association between diabetes and neurodegenerative diseases is increasing with aging. Several common mechanisms are involved in both these diseases. The endothelial cells of the blood brain barrier, neurons and glia express typical and different receptors of the glucose metabolism (glucose transporters, insulin receptors and glucagon-like peptide-1 receptors). Read More

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April 2014
6 Reads

Antisense oligonucleotides in the treatment of cerebral gliomas. Review of concerning patents.

Recent Pat CNS Drug Discov 2014 Apr;9(1):2-12

Neurosurgical Clinic, Department of Neuroscience, A.O.U. Policlinico "G. Martino", via Consolare Valeria, 1, 98125 Messina, Italy.

Gliomas are the most common and malignant primary brain tumors in the adult population. Despite the intensive research on cancer pathology, real mechanisms concerning glioma progression are not completely understood. The prognosis in patients affected by malignant gliomas is still very unfavorable. Read More

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April 2014
1 Read

Migraine attack treatment : a tailor-made suit, not one size fits all.

Recent Pat CNS Drug Discov 2014 Apr;9(1):26-40

Department of Neurology. Quiron Dexeus University Hospital. Address; C/ Sabino Arana n°5-19, cp 08028, Barcelona; Spain.

About 15% of people in the world suffer migraine attacks. Migraine can induce a great impact in the quality of life, and the costs of medical care and loss of productivity can be also high. Non-steroidal anti-inflammatory drugs (NSAIDs) are the best treatment in mild-to-moderate migraine attacks and triptans are the first line option in the acute treatment of moderate-to-severe migraine attacks. Read More

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April 2014
3 Reads

Therapeutic potential of cannabinoids in schizophrenia.

Recent Pat CNS Drug Discov 2014 Apr;9(1):13-25

CEITEC (Central European Institute of Technology) Masaryk University, Kamenice 5, 625 00 Brno, Czech Republic.

Increasing evidence suggests a close relationship between the endocannabinoid system and schizophrenia. The endocannabinoid system comprises of two G protein-coupled receptors (the cannabinoid receptors 1 and 2 [CB1 and CB2] for marijuana's psychoactive principle Δ(9)-tetrahydrocannabinol), their endogenous small lipid ligands (namely anandamide [AEA] and 2-arachidonoylglycerol [2-AG], also known as endocannabinoids), and proteins for endocannabinoid biosynthesis and degradation. It has been suggested to be a pro-homeostatic and pleiotropic signalling system activated in a time- and tissue-specific manner during pathophysiological conditions. Read More

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April 2014
1 Read

Recent advances in the treatment of neurogenic erectile dysfunction.

Recent Pat CNS Drug Discov 2014 Apr;9(1):41-53

Neurorehabilitation Unit, IRCCS Centro Neurolesi "Bonino Pulejo" , via Palermo, S.S. 113, C.da Casazza, 98124 Messina, Italy.

Neurogenic erectile dysfunction (ED) can be broadly defined as an inability to sustain or maintain a penile erection owing to a neurological impairment, either centrally or peripherally or both. Although significant advances in the pharmacological treatment of ED have occurred in recent years, especially after the introduction of oral selective phosphodiesterase type 5 inhibitor, the treatment of neurological patients with ED may be challenging for prescribers, given poor data available on this topic and the variety of etiologic factors (iatrogenic, endocrine, psychiatric and psychosocial) to consider. At the same time, several, new oral, local and surgical treatments are available and their efficacy and safety depend on the specific cases. Read More

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April 2014
3 Reads

Cerebrovascular ultrasonography for selecting patients for stroke intervention.

Recent Pat CNS Drug Discov 2013 Dec;8(3):205-19

Division of Neurology, Department of Medicine, National University Hospital, Tower Block, Level 10, 1E Kent Ridge Road Singapore 119228.

Currently employed diagnostic ultrasonography provides clinically relevant information about cerebral hemodynamic changes in patients with cerebrovascular ischemia. The information thus obtained is often helpful to the physician for establishing or confirming the diagnosis and prognosis as well as in taking appropriate therapeutic decisions. It is associated with a high temporal resolution and can be performed bedside for rapid diagnosis as well as prolonged monitoring. Read More

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December 2013
3 Reads

Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions.

Recent Pat CNS Drug Discov 2013 Dec;8(3):180-204

Endocannabinoid Research Group, Institute of Biomolecular Chemistry, CNR, Pozzuoli, Italy.

The transient receptor potential vanilloid-1 cat ion channel (TRPV1) is a nonspecific cation channel that can be activated by multiple endogenous stimuli and is expressed predominantly in sensory neurons, where it serves as a key nodal point in pain transmission pathways. In mammals, TRPV1 displays a wide tissue and cellular expression including both the peripheral and central nervous system, and in the latter it is now recognized to have a broader distribution and function. The pharmacological modulation of TRPV1 represents a strategy for the treatment of a variety of disease states, particularly those requiring chronic pain management. Read More

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December 2013
5 Reads

Patents on brain permeable nanoparticles.

Recent Pat CNS Drug Discov 2013 Dec;8(3):220-34

Department of Pharmaceutical Sciences, Punjabi University, Patiala - 147 002, India.

The blood-brain barrier (BBB) presents a combination of physical and electrostatic barriers. It is a highly complex structure that tightly regulates the movement of molecules from the blood to brain, protecting it from injuries and diseases. However, the BBB also significantly precludes the delivery of drugs to the brain, thus, preventing the therapy of a number of neurological disorders like brain cancer, epilepsy, Alzheimer's disease, schizophrenia etc. Read More

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December 2013
6 Reads

Transglutaminase activity as a possible therapeutical target in neurodegenerative diseases.

Recent Pat CNS Drug Discov 2013 Dec;8(3):235-42

Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, via Costantinopoli 16, 80138 Naples, Italy.

Transglutaminases are ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). Read More

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December 2013
1 Read

An ion channel chip for diagnosis and prognosis of autoimmune neurological disorders.

Recent Pat CNS Drug Discov 2013 Dec;8(3):171-9

PMC CNRS, 660 Route des Lucioles, 06560 Valbonne Sophia Antipolis, France.

Autoantibodies directed against ion channels and ionotropic receptors are associated with neuromuscular and neurological disorders. Their detection has proven to be useful for diagnosis, prognosis and treatment of these autoimmune syndromes. We have designed an ion channel chip for the systematic and rapid screening of antibodies directed against tens of different ion channels. Read More

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December 2013
10 Reads

The role of Cnidaria in drug discovery. A review on CNS implications and new perspectives.

Recent Pat CNS Drug Discov 2013 Aug;8(2):110-22

Department of Earth, Environment and Life Sciences, University of Genova, Italy.

Many organisms produce bioactive substances used in the production of drugs. In this context, Cnidaria occupy a major position; for this reason, research on new bioactive substances has focused upon them as an interesting target. As a matter of fact, substances and extracts able to fight human diseases have been found in cnidarians, several of which have been studied in laboratories using animal models or cell cultures and, at present, some are in the pre-clinical phase. Read More

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August 2013
5 Reads

Therapeutic approaches for lysosomal storage diseases: a patent update.

Recent Pat CNS Drug Discov 2013 Aug;8(2):91-109

Department of Experimental Medicine and Biochemical Sciences, University of Perugia, Perugia, Italy.

Lysosomal Storage Diseases (LSDs) are inherited metabolic disorders caused by specific lysosomal protein deficiencies, which lead to abnormal storage of macromolecular substrates. Most LSDs are characterized by central nervous system (CNS) pathology, intracellular deposition and protein aggregation, events also found in age-related neurodegenerative diseases. Over the past two decades, a few approaches for the cure of these disorders have been approved for clinical use, i. Read More

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August 2013
4 Reads

Transglutaminase inhibition as a possible therapeutical approach to protect cells from death in neurodegenerative diseases.

Recent Pat CNS Drug Discov 2013 Aug;8(2):161-8

Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, Naples, Italy.

Transglutaminases are ubiquitous enzymes which catalyze post-translational modifications of proteins. The main activity of these enzymes is the cross-linking of glutaminyl residues of a protein/peptide substrate to lysyl residues of a protein/peptide co-substrate. In addition to lysyl residues, other second nucleophilic co-substrates may include monoamines or polyamines (to form mono- or bi-substituted /crosslinked adducts) or -OH groups (to form ester linkages). Read More

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August 2013
4 Reads

Insulin-like growth factor-1 and its derivatives: potential pharmaceutical application for treating neurological conditions.

Recent Pat CNS Drug Discov 2013 Aug;8(2):142-60

The Liggins Institute, the University of Auckland, New Zealand.

Ischemic brain damage remains a major cause of disability at all ages. This review examines the efficacy, mode of action and mechanisms of insulin-like growth factor (IGF)-1 and its derivatives in animal models of acute brain injury and neurodegenerative conditions, their potential in pharmaceutical developments. IGF-1 reduces cell loss and improves long-term neurological function in animal models. Read More

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August 2013
1 Read

New pharmacological approaches to the cholinergic system: an overview on muscarinic receptor ligands and cholinesterase inhibitors.

Recent Pat CNS Drug Discov 2013 Aug;8(2):123-41

Drug Design and Development Section, Translational Gerontology Branch, Intramural Research Program, National Institute on Aging, Baltimore, MD 21224, USA.

The cholinergic system is expressed in neuronal and in non-neuronal tissues. Acetylcholine (ACh), synthesized in and out of the nervous system can locally contribute to modulation of various cell functions (e.g. Read More

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5831731PMC
August 2013
7 Reads

Targets of anti-glucocorticoid therapy for stress-related diseases.

Recent Pat CNS Drug Discov 2013 Apr;8(1):79-87

Geriatric Unit, Faculty of Medicine and Psychology, Sapienza University of Rome, S. Andrea Hospital, Rome, Italy.

The stress response during chronic conditions increases vulnerability to diseases through the activation of adaptive systems, in particular, the hypothalamus-pituitary-adrenal (HPA) axis. Dysregulation in HPA activity (central and peripheral) has been reported in chronic diseases, like metabolic syndrome, type-2 diabetes mellitus, atherosclerosis-related disease, essential hypertension, dementia, depression, particularly during comorbid conditions. Different targets of anti-glucocorticoid treatment have been proposed, acting at supra-hypothalamic, HPA axis, glucocorticoid receptor and post-receptor levels. Read More

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April 2013
7 Reads

The role of cerebrospinal fluid biomarkers for Alzheimer's disease diagnosis. where are we now?

Recent Pat CNS Drug Discov 2013 Apr;8(1):70-8

Third Department of Neurology, G Papanikolaou Hospital, Thessaloniki, Greece.

Alzheimer's disease (AD) is a rapidly growing disease that is estimated to affect about 36 million people worldwide, therefore there is an immediate need for its' early diagnosis and treatment. A number of research studies are performed on possible accurate and reliable diagnostic biomarkers of AD. This review study provides an update on the cerebrospinal fluid (CSF) proteins that are being currently used in clinical practice and studied as biomarkers for early AD diagnosis and their future prospects, as well as relevant patents. Read More

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Different classes of CB2 ligands potentially useful in the treatment of pain.

Recent Pat CNS Drug Discov 2013 Apr;8(1):42-69

Department of Chemistry and Pharmacy, University of Sassari, Sassari, Italy.

The search of new drugs and targets to treat the pain is an intriguing challenge both for several companies and researchers from academia. In this context, since the modulation of the endocannabinoid system with the non selective phytocannabinoid Δ9-THC produces analgesia and potentiates opioid analgesia in animal models, CB2 ligands studies aimed to explore the involvement of endocannabinoid system in management of pain were started. Several selective CB2 receptor agonists exhibited analgesic activity in preclinical models of acute, inflammatory and neuropathic pain, therefore this class of modulators could be useful as analgesic agents for pain, migraine, inflammation and osteoarthritis. Read More

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April 2013
14 Reads

Anti-seizure medications and estradiol for neuroprotection in epilepsy: the 2013 update.

Recent Pat CNS Drug Discov 2013 Apr;8(1):24-41

Department of Cell Biology & Anatomy, New York Medical College, Valhalla, NY 10595, USA.

Current epilepsy therapy is still symptomatic using anti-seizure, rather than anti-epileptic, medications. This therapy may control the seizure activity but does not prevent or even cure epilepsy. Treatment strategies that could interfere with the process leading to epilepsy (epileptogenesis) would have significant benefits over the current approaches. Read More

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April 2013
8 Reads

The potential for substance P antagonists as anti-cancer agents in brain tumours.

Recent Pat CNS Drug Discov 2013 Apr;8(1):13-23

Discipline of Anatomy and Pathology, School of Medical Sciences, The University of Adelaide, South Australia 5005, Australia.

Despite recent advances in cancer treatment and diagnosis, the prognosis for patients with CNS tumours remains extremely poor. This is, in part, due to the difficulty in completely removing tumours surgically, and also because of the presence of the blood brain barrier, which can prevent the entry of chemotherapeutic agents typically used in cancer treatment. Despite the presence of the blood brain barrier, tumour cells are capable of entering and colonising the brain to form secondary brain tumours. Read More

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