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Current Neuropharmacology

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https://www.readbyqxmd.com/read/27928949/from-leflunomide-to-teriflunomide-drug-development-and-immunosuppressive-oral-drugs-in-the-treatment-of-multiple-sclerosis
#1
Lilian Aly, Bernhard Hemmer, Thomas Korn
Immunosuppressive drugs have been used in the treatment of multiple sclerosis (MS) for a long time. Today, the increased number of approved substances and the possibility of an oral availability of some immunomodulators improve the therapeutic repertory and increase patient satisfaction and compliance. Teriflunomide is indicated as first line oral disease modifying therapy (DMT) in relapsing-remitting MS (RRMS). Its immunosuppressive capacity results from an inhibition of de novo pyrimidine synthesis in rapidly proliferating lymphocytes...
December 8, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27928948/revisiting-antipsychotic-induced-akathisia-current-issues-and-prospective-challenges
#2
Haitham Salem, Caesa Nagpal, Teresa Pigott, Antonio Lucio Teixeira
Akathisia continues to be a significant challenge in current neurological and psychiatric practice. Prompt and accurate detection is often difficult and there is a lack of consensus concerning the neurobiological basis of akathisia. No definitive treatment has been established for akathisia despite numerous preclinical and clinical studies. With these issues in mind, we reviewed antipsychotic-induced akathisia including its clinical presentation, proposed underlying pathophysiology, and an update of potential treatment strategies...
December 8, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27919211/development-of-mlr-and-svm-aided-qsar-models-to-identify-common-sar-of-gaba-uptake-herbal-inhibitors-used-in-the-treatment-of-schizophrenia
#3
Sahila Mohammed Marunnan, Babitha Pallikkara Pulikka, V K Gopalakrishnan, Srinivas Bandaru, Mukesh Yadav, Anuraj Nayarisseri, Victor Arokia Doss
Deficits in GABAnergic system is implicated in the pathophysiology of schizophrenia. Available antipsychotics that target GABA receptor form a desirable therapeutic strategy in the treatment regimen of schizophrenia but, unfortunately, suffers serious setback due to their prolonged side effects. The present investigation focuses on developing QSAR models from the biological activity of herbal compounds and their derivatives that promise to be alternative candidates to GABA uptake inhibitors. Three sets of compounds were undertaken in the study to develop the QSAR models...
December 5, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27919210/three-dimensional-modelling-of-the-voltage-gated-sodium-ion-channel-from-anopheles-gambiae-reveals-spatial-clustering-of-evolutionarily-conserved-acidic-residues-at-the-extracellular-sites
#4
Rithvik S Vinekar, Ramanathan Sowdhamini
The eukaryotic voltage-gated sodium channel(e-Nav) is a large asymmetric transmembrane protein with important functions concerning neurological function. No structure has been resolved at high resolution for this protein. A homology model of the transmembrane and extracellular regions of an Anopheles gambiae para-like channel with emphasis on the pore entrance has been constructed, based upon the templates provided by a prokaryotic sodium channel and a potassium two-pore channel. The latter provides a template for the extracellular regions, which are located above the entrance to the pore, which is likely to open at a side of a dome formed by these loops...
December 5, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27908258/neurotoxicity-induced-by-mephedrone-an-up-to-date-review
#5
Flaminia Pantano, Roberta Tittarelli, Giulio Mannocchi, Roberta Pacifici, Alessandro di Luca, Francesco Paolo Busardò, Enrico Marinelli
Mephedrone is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. The aim of this review was to examine the emerging scientific literature on the possible mephedrone-induced neurotoxicity, yet not well defined due to the limited number of experimental studies, mainly carried on animal models. Relevant scientific articles were identified from international literature databases (Medline, Scopus, etc...
November 30, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27855594/when-chems-meet-sex-a-rising-phenomenon-called-chemsex
#6
Raffaele Giorgetti, Adriano Tagliabracci, Fabrizio Schifano, Simona Zaami, Enrico Marinelli, Francesco Paolo Busardò
BACKGROUND: The term "chemsex" was coined to indicate the voluntary intake of psychoactive and non psychoactive drugs in the context of recreational settings to facilitate and/or to enhance sexual intercourses mostly among men who have sex with other men (MSM). OBJECTIVE: The authors aimed to review the mechanisms of action, the toxicity and the pattern of use and abuse of substances involved in "chemsex" practice together with the sociocultural background underlying it and the health-related consequences that they may have...
November 17, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27834146/recent-trends-in-analytical-methods-to-determine-new-psychoactive-substances-in-hair
#7
Chrystalla Kyriakou, Manuela Pellegrini, Oscar García-Algar, Enrico Marinelli, Simona Zaami
New Psychoactive Substances (NPS) belong to several chemical classes, including phenethylamines, piperazines, synthetic cathinones and synthetic cannabinoids. Development and validation of analytical methods for the determination of NPS both in traditional and alternative matrices is of crucial importance to study drug metabolism and to associate consumption to clinical outcomes and eventual intoxication symptoms. Among different biological matrices, hair is the one with the widest time window to investigate drug-related history and demonstrate past intake...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27834145/pharmacogenetics-and-pharmacotherapy-of-military-personnel-suffering-from-posttraumatic-stress-disorder
#8
Janine Naß, Thomas Efferth
BACKGROUND: Posttraumatic stress disorder (PTSD) is a severe problem among soldiers with combat experience and still difficult to treat. The pathogenesis is still not fully understood at the psychological level. Therefore, genetic research became a focus of interest. The identification of single nucleotide polymorphisms (SNPs) may help to predict, which persons are at high risk to develop PTSD as a starting point to develop novel targeted drugs for treatment. METHODS: We conducted a systematic review on SNPs in genes related to PTSD pathology and development of targeted pharmacological treatment options based on PubMed database searches...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27834144/evolutionary-considerations-on-the-emerging-subculture-of-the-e-psychonauts-and-the-novel-psychoactive-substances-a-comeback-to-the-shamanism
#9
Laura Orsolini, Paul St John-Smith, Daniel McQueen, Duccio Papanti, John Corkery, Fabrizio Schifano
BACKGROUND: Evolutionary research on drug abuse has hitherto been restricted to proximate studies, considering aetiology, mechanism, and ontogeny. However, in order to explain the recent emergency of a new behavioral pattern (e.g. 'the e-psychonaut style') of novel psychoactive substances' (NPS) intake, a complementary evolutionary model may be needed. OBJECTIVE: A range of evolutionary interpretations on the 'psychonaut style' and the recent emergency of NPS was here considered...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27834143/distribution-of-synthetic-cannabinoids-jwh-210-rcs-4-and-%C3%A2-9-tetrahydrocannabinol-after-intravenous-administration-to-pigs
#10
Nadine Schaefer, Mattias Kettner, Matthias W Laschke, Julia Schlote, Andreas H Ewald, Michael D Menger, Hans H Maurer, Peter H Schmidt
Synthetic cannabinoids (SCs) have become an increasing issue in forensic toxicology. Controlled human studies evaluating pharmacokinetic data of SCs are lacking and only few animal studies have been published. Thus, an interpretation of analytical results found in intoxicated or poisoned individuals is difficult. Therefore, the distribution of two selected SCs, namely 4-ethylnaphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-210) and 2-(4-methoxyphenyl)-1-(1-pentyl-indol-3-yl)methanone (RCS-4) as well as ∆9-tetrahydrocannabinol (THC) as reference were examined in pigs...
November 11, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27829332/in-vitro-metabolite-profiling-of-adb-fubinaca-a-new-synthetic-cannabinoid
#11
Jeremy Carlier, Xingxing Diao, Ariane Wohlfarth, Karl Scheidweiler, Marilyn A Huestis
Metabolite profiling of novel psychoactive substances (NPS) is critical for documenting drug consumption. N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide (ADB-FUBINACA) is an emerging synthetic cannabinoid whose toxicological and metabolic data are currently unavailable. We aimed to determine optimal markers for identifying ADB-FUBINACA intake. Metabolic stability was evaluated with human liver microsome incubations. Metabolites were identified after 1 and 3 h incubation with pooled human hepatocytes, liquid chromatography- high resolution mass spectrometry in positive-ion mode (5600+ TripleTOF®, Sciex) and several data mining approaches (MetabolitePilot™, Sciex)...
November 8, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27804884/opioids-resistance-in-chronic-pain-management
#12
Luigi Antonio Morrone, Damiana Scuteri, Laura Rombolà, Hirokazu Mizoguchi, Giacinto Bagetta
Chronic pain management represents a serious healthcare problem worldwide. Chronic pain affects approximately 20% of the adult European population and is more frequent in women and older people. Unfortunately, its management in the community remains generally unsatisfactory and rarely under the control of currently available analgesics. Opioids have been used as analgesics for a long history and are among the most used drugs; however, while there is no debate over their short term use for pain management, limited evidence supports their efficacy of long-term treatment for chronic non-cancer pain...
October 31, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27804883/pros-and-cons-of-medical-cannabis-use-by-people-with-chronic-brain-disorders
#13
Uma Suryadevara, Dawn M Bruijnzeel, Meena Nuthi, Darin A Jagnarine, Rajiv Tandon, Adriaan W Bruijnzeel
BACKGROUND: Cannabis is the most widely used illicit drug in the world and there is growing concern about the mental health effects of cannabis use. These concerns are at least partly due to the strong increase in recreational and medical cannabis use and the rise in tetrahydrocannabinol (THC) levels. Cannabis is widely used to self-medicate by older people and people with brain disorders such as amyotrophic lateral sclerosis (ALS), multiple sclerosis (MS), Alzheimer's disease (AD), Parkinson's disease (PD), bipolar disorder, and schizophrenia...
October 31, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27799032/herbal-highs-review-on-psychoactive-effects-and-neuropharmacology
#14
Silvia Graziano, Laura Orsolini, Maria Concetta Rotolo, R Tittarelli, Fabrizio Schifano, Simona Pichini
BACKGROUND: A new trend among users of new psychoactive substances' the consumption of "herbal highs": plant parts containing psychoactive substances. Most of the substances extracted from herbs, in old centuries were at the centre of religious ceremonies of ancient civilizations. Currently, these herbal products are mainly sold by internet web sites and easily obtained since some of them have no legal restriction. OBJECTIVE: We reviewed psychoactive effects and neuropharmacology of the most used "herbal highs" with characterized active principles, with studies reporting mechanisms of action, pharmacological and subjective effects, eventual secondary effects including intoxications and/or fatalities Method: The PubMed database was searched using the following key...
October 31, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27799033/non-allowed-pharmacologically-active-substances-in-physical-and-sexual-performance-enhancing-products
#15
Manuela Pellegrini, Maria Concetta Rotolo, Francesco Paolo Busardò, Roberta Pacifici, Simona Pichini
Recently, a large amount of physical and sexual performance enhancing products have started to be freely sold mainly on internet web sites as dietary supplements. However, there a high suspicion that pharmacologically active substance, prohibited in these products, can be present to provide the expected effect. A simple and rapid systematic toxicological analysis by gas chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry has been applied after a liquid-liquid extraction at acidic, neutral and alkaline pH with chloroform-isopropanol (9:1 v/v)...
October 28, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27784226/evidence-of-2-populations-of-mephedrone-abusers-by-hair-testing-application-to-4-forensic-expertises
#16
Pascal Kintz
New psychoactive substances are conquering the drug scene. Among these substances, cathinone derivatives have been observed since late in the year 2000. At that time, an increasing use of the synthetic cathinone mephedrone (4-methylmethcathinone) started to be observed, particularly among night clubbers. Although these new psychoactive drugs showed an appearance of safety, a growing amount of experiences on their secondary effects has been reported. Mephedrone for example is known to induce psychosis. Given the potential negative effects of mephedrone, the laboratory was asked to test for the drug in hair, a cumulative matrix that can document single, occasional or repetitive abuse of xenobiotics...
October 26, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27784225/polyphenols-beyond-barriers-a-glimpse-into-the-brain
#17
Inês Figueira, Regina Menezes, Diana Macedo, Inês Costa, Cláudia Nunes Dos Santos
BACKGROUND: Ageing can be simply defined as the process of becoming older, which is genetically determined but also environmentally modulated. With the continuous increase of life expectancy, quality of life during ageing has become one of the biggest challenges of developed countries. The quest for a healthy ageing has led to the extensive study of plant polyphenols with the aim to prevent age-associated deterioration and diseases, including neurodegenerative diseases. The world of polyphenols has fascinated researchers over the past decades, and in vitro, cell-based, animal and human studies have attempted to unravel the mechanisms behind dietary polyphenols neuroprotection...
October 26, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27774881/introductory-considerations-athanasios-koukopoulos-the-man-the-psychiatrist-the-original-thinker
#18
Hagop S Akiskal
What I uttered in Athens moved with apparent emotion [that seem to have not escaped Jules Angst's concern] was spontaneous, except for what is printed in the program book, which has somehow vanished from my office, unlike him with his larger than life figure whose memory will live for as long as he lives in the minds and hearts of all those who were privileged to be his family, colleagues, patients, friends, and… countless others, plus those whose email addresses I cannot locate right now sitting in the sunshine of La Jolla-far away from my loved ones-and wondering what ethnic, genetic and environmental factors-perhaps even several Greek gods combined-to produce the original mind and heart of our Athenian friend who, nonetheless, lived in Rome-and now resting not in the 'atheist' cemetery [it took me 5 minutes to spell this word]-but in our hearts for as long as they will beat-perhaps eventually in another realm, 'from whose bourn'-according to Hamlet-no one has ever returned-that's the promise of the Eternal City-where Athanasios is lying...
October 21, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27774880/editorial-the-concept-of-mania-across-centuries
#19
Gabriele Sani, Georgios D Kotzalidis, Paolo Girardi
No abstract text is available yet for this article.
October 21, 2016: Current Neuropharmacology
https://www.readbyqxmd.com/read/27758707/new-psychoactive-substances-3-methoxyphencyclidine-3-meo-pcp-and-3-methoxyrolicyclidine-3-meo-pcpy-metabolic-fate-elucidated-with-rat-urine-and-human-liver-preparations-and-their-detectability-in-urine-by-gc-ms-lc-high-resolution-msn-and-lc-high-resolution
#20
Julian A Michely, Sascha K Manier, Achim T Caspar, Simon D Brandt, Jason Wallach, Hans H Maurer
3-Methoxyphencyclidine (3-MeO-PCP) and 3-methoxyrolicyclidine (3-MeO-PCPy) are two new psychoactive substances (NPS). The aims of the present study were the elucidation of their metabolic fate in rat and pooled human liver microsomes (pHLM), the identification of the cytochrome P450 (CYP) isoenzymes involved, and the detectability using standard urine screening approaches (SUSA) after intake of common users' doses using gas chromatography-mass spectrometry (GC-MS), liquid chromatography-multi-stage mass spectrometry (LC-MSn), and liquid chromatography-high-resolution tandem mass spectrometry (LC-HR-MS/MS)...
October 18, 2016: Current Neuropharmacology
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