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Neuropharmacology

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https://www.readbyqxmd.com/read/27909988/predicting-the-abuse-liability-of-entactogen-class-new-and-emerging-psychoactive-substances-via-preclinical-models-of-drug-self-administration
#1
Shawn M Aarde, Michael A Taffe
Animal models of drug self-administration are currently the gold standard for making predictions regarding the relative likelihood that a recreational drug substance will lead to continued use and addiction. Such models have been found to have high predictive accuracy and discriminative validity for a number of drug classes including ethanol, nicotine, opioids, and psychostimulants such as cocaine and methamphetamine. Members of the entactogen class of psychostimulants (drugs that produce an "open mind state" including feelings of interpersonal closeness, intimacy and empathy) have been less frequently studied in self-administration models...
December 2, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27908258/neurotoxicity-induced-by-mephedrone-an-up-to-date-review
#2
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/27890469/methamphetamine-addiction-vulnerability-the-glutamate-the-bad-and-the-ugly
#3
Karen K Szumlinski, Kevin D Lominac, Rianne R Campbell, Matan Cohen, Elissa K Fultz, Chelsea N Brown, Bailey W Miller, Sema G Quadir, Douglas Martin, Andrew B Thompson, Georg von Jonquieres, Matthias Klugmann, Tamara J Phillips, Tod E Kippin
BACKGROUND: The high prevalence and severity of methamphetamine (MA) abuse demands greater neurobiological understanding of its etiology. METHODS: We conducted immunoblotting and in vivo microdialysis procedures in MA high/low drinking mice, as well as in isogenic C57BL/6J mice that varied in their MA preference/taking, to examine the glutamate underpinnings of MA abuse vulnerability. Neuropharmacological and Homer2 knockdown approaches were also used in C57BL/6J mice to confirm the role for nucleus accumbens (NAC) glutamate/Homer2 expression in MA preference/aversion...
October 13, 2016: Biological Psychiatry
https://www.readbyqxmd.com/read/27858095/-new-aspects-of-neurorehabilitation-motor-and-language
#4
J Liepert, C Breitenstein
Advancements in medical care over the last decades have contributed to a continuous decline in immediate post-stroke mortality. The flipside of this development is that patients surviving the initial stroke are forced to live with sometimes extreme functional motor and/or language limitations for the remaining life span. The following overview presents evidence-based neurorehabilitative interventions to promote motor and language recovery in the acute and chronic post-stroke stages. Therapeutic approaches comprise intensive training, neuropharmacological drugs and non-invasive brain stimulation techniques, such as transcranial magnetic stimulation (TMS) or direct current stimulation (tDCS)...
November 17, 2016: Der Nervenarzt
https://www.readbyqxmd.com/read/27834390/varenicline-reduces-context-induced-relapse-to-alcohol-seeking-through-actions-in-the-nucleus-accumbens
#5
F Lacroix, A Pettorelli, J-Mn Maddux, A Heidari-Jam, N Chaudhri
Varenicline, a pharmacotherapy for tobacco addiction, reduces alcohol consumption in humans and rodents. The therapeutic potential of varenicline would escalate if it also diminished conditioned responses elicited by alcohol-predictive cues, which can precipitate relapse in abstinent individuals. We investigated this application, along with the underlying neural substrates, using a robust preclinical assay in which relapse to alcohol-seeking was triggered by re-exposure to an alcohol-associated environmental context...
November 11, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27830575/neuropharmacology-of-3-4-methylenedioxypyrovalerone-mdpv-its-metabolites-and-related-analogs
#6
Michael H Baumann, Mohammad O Bukhari, Kurt R Lehner, Sebastien Anizan, Kenner C Rice, Marta Concheiro, Marilyn A Huestis
3,4-Methylenedioxypyrovalerone (MDPV) is a psychoactive component of so-called bath salts products that has caused serious medical consequences in humans. In this chapter, we review the neuropharmacology of MDPV and related analogs, and supplement the discussion with new results from our preclinical experiments. MDPV acts as a potent uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET) in nervous tissue. The MDPV formulation in bath salts is a racemic mixture, and the S isomer is much more potent than the R isomer at blocking DAT and producing abuse-related effects...
November 10, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27809820/effect-of-root-extracts-of-ficus-benghalensis-banyan-in-memory-anxiety-muscle-co-ordination-and-seizure-in-animal-models
#7
Dipesh Raj Panday, G P Rauniar
BACKGROUND: Ficus benghalensis L. (Banyan) is a commonly found tree in Eastern Nepal. Its different plant parts are used for various neurological ailments. This study was performed in mice to see its effects in various neuropharmacological parameters. METHODS: Passive-avoidance (memory), Open-field (anxiety), Pentobarbital-induced Sleep potentiation (sleep), Rota-rod (muscle-co-ordination), Pentylenetetrazol-Induced and Maximal Electroshock Seizure Tests were performed...
November 3, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27799032/herbal-highs-review-on-psychoactive-effects-and-neuropharmacology
#8
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/27781077/neuroprotective-effects-of-a%C3%A3-a%C3%A3-euterpe-oleracea-mart-against-rotenone-in-vitro-exposure
#9
Alencar Kolinski Machado, Ana Cristina Andreazza, Tatiane Morgana da Silva, Aline Augusti Boligon, Vanusa do Nascimento, Gustavo Scola, Angela Duong, Francine Carla Cadoná, Euler Esteves Ribeiro, Ivana Beatrice Mânica da Cruz
Neuropsychiatric diseases, such as bipolar disorder (BD) and schizophrenia (SCZ), have a very complex pathophysiology. Several current studies describe an association between psychiatric illness and mitochondrial dysfunction and consequent cellular modifications, including lipid, protein, and DNA damage, caused by cellular oxidative stress. Euterpe oleracea (açaí) is a powerful antioxidant fruit. Açaí is an Amazonian palm fruit primarily found in the lowlands of the Amazonian rainforest, particularly in the floodplains of the Amazon River...
2016: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/27756689/neuroadaptations-to-antipsychotic-drugs-insights-from-pre-clinical-and-human-post-mortem-studies
#10
Davide Amato, Clare L Beasley, Margaret K Hahn, Anthony C Vernon
Antipsychotic drugs, all of which block the dopamine D2 receptor to a greater or lesser extent, are the mainstay for the pharmacological treatment of schizophrenia. Engaging in a deeper understanding of how antipsychotics act on the brain and body, at the cellular, molecular and physiological level is vital to comprehend both the beneficial and potentially harmful actions of these medications and stimulate development of novel therapeutics. To address this, we review recent advances in our understanding of neuroadaptations to antipsychotics, focusing on (1) treatment efficacy, (2) impact on brain volume and (3) evidence from human post-mortem studies that attempt to dissect neuropathological effects of antipsychotic drugs from organic schizophrenia neurobiology and (4) cardio-metabolic side effects...
October 15, 2016: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/27753008/neurotoxicology-of-synthetic-cathinone-analogs
#11
Mariana Angoa-Pérez, John H Anneken, Donald M Kuhn
The present review briefly explores the neurotoxic properties of methcathinone, mephedrone, methylone, and methylenedioxypyrovalerone (MDPV), four synthetic cathinones most commonly found in "bath salts." Cathinones are β-keto analogs of the commonly abused amphetamines and display pharmacological effects resembling cocaine and amphetamines, but despite their commonalities in chemical structures, synthetic cathinones possess distinct neuropharmacological profiles and produce unique effects. Among the similarities of synthetic cathinones with their non-keto analogs are their targeting of monoamine systems, the release of neurotransmitters, and their stimulant properties...
October 18, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27746708/comparative-study-of-neuropharmacological-analgesic-properties-and-phenolic-profile-of-ajwah-safawy-and-sukkari-cultivars-of-date-palm-phoenix-dactylifera
#12
Bassem Yousef Sheikh, S M Neamul Kabir Zihad, Nazifa Sifat, Shaikh J Uddin, Jamil A Shilpi, Omer A A Hamdi, Hemayet Hossain, Razina Rouf, Ismet Ara Jahan
In addition to the rich nutritional value, date palm is also used in various ethnobotanical practices for the treatment of various disease conditions. Present investigation was undertaken to examine the neuropharmacological and antinociceptive effect of the ethanol extract of three date cultivars growing in Saudi Arabia, namely Ajwah, Safawy and Sukkari. Neuropharmacological effect was observed by pentobarbitone induced sleeping time, open field, and hole board test. Antinociceptive activity was tested by acetic acid induced writhing and hot plate test...
2016: Oriental Pharmacy and Experimental Medicine
https://www.readbyqxmd.com/read/27742467/electrophysiological-properties-of-neurons-derived-from-human-stem-cells-and-ineurons-in-vitro
#13
Robert F Halliwell
Functional studies of neurons have traditionally used nervous system tissues from a variety of non-human vertebrate and invertebrate species, even when the focus of much of this research has been directed at understanding human brain function. Over the last decade, the identification and isolation of human stem cells from embryonic, tissue (or adult) and induced pluripotent stem cells (iPSCs) has revolutionized the availability of human neurons for experimental studies in vitro. In addition, the direct conversion of terminally differentiated fibroblasts into Induced neurons (iN) has generated great excitement because of the likely value of such human stem cell derived neurons (hSCNs) and iN cells in drug discovery, neuropharmacology, neurotoxicology and regenerative medicine...
October 11, 2016: Neurochemistry International
https://www.readbyqxmd.com/read/27739164/evidence-for-gaba-a-receptor-dysregulation-in-gambling-disorder-correlation-with-impulsivity
#14
Inge Mick, Anna C Ramos, Jim Myers, Paul R Stokes, Samantha Chandrasekera, David Erritzoe, Maria A Mendez, Roger N Gunn, Eugenii A Rabiner, Graham E Searle, José C F Galduróz, Adam D Waldman, Henrietta Bowden-Jones, Luke Clark, David J Nutt, Anne R Lingford-Hughes
As a behavioural addiction, gambling disorder (GD) provides an opportunity to characterize addictive processes without the potentially confounding effects of chronic excessive drug and alcohol exposure. Impulsivity is an established precursor to such addictive behaviours, and GD is associated with greater impulsivity. There is also evidence of GABAergic dysregulation in substance addiction and in impulsivity. This study therefore investigated GABAA receptor availability in 15 individuals with GD and 19 healthy volunteers (HV) using [(11) C]Ro15-4513, a relatively selective α5 benzodiazepine receptor PET tracer and its relationship with impulsivity...
October 13, 2016: Addiction Biology
https://www.readbyqxmd.com/read/27731825/anxiolytic-and-antidepressant-activity-of-different-methanolic-extracts-of-melia-azedarach-linn
#15
Humera Ishaq
Present study was planned to search for neuropharmacological properties of methanolic extracts of different parts of Melia azedarach Linn. because conventional medicine shows adverse effects. Recently natural products are studied worldwide, as safer alternatives, which are not duly supported with scientifically proved data. Melia azedarach (Bakayan, China berry tree) is medium sized tree belonging to family Meliaceae. Traditional use of plant is as anthelmintic, antilithic and diuretic. Topical application of oil for cramps and rheumatism is beneficial...
September 2016: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27729239/scorpion-toxin-peptide-action-at-the-ion-channel-subunit-level
#16
David M Housley, Gary D Housley, Michael J Liddell, Ernest A Jennings
This review categorizes functionally validated actions of defined scorpion toxin (SCTX) neuropeptides across ion channel subclasses, highlighting key trends in this rapidly evolving field. Scorpion envenomation is a common event in many tropical and subtropical countries, with neuropharmacological actions, particularly autonomic nervous system modulation, causing significant mortality. The primary active agents within scorpion venoms are a diverse group of small neuropeptides that elicit specific potent actions across a wide range of ion channel classes...
October 8, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27713495/allosteric-regulation-in-nmda-receptors-revealed-by-the-genetically-encoded-photo-cross-linkers
#17
Meilin Tian, Shixin Ye
Allostery is essential to neuronal receptor function, but its transient nature poses a challenge for characterization. The N-terminal domains (NTDs) distinct from ligand binding domains are a major locus for allosteric regulation of NMDA receptors (NMDARs), where different modulatory binding sites have been observed. The inhibitor ifenprodil, and related phenylethanoamine compounds specifically targeting GluN1/GluN2B NMDARs have neuroprotective activity. However, whether they use differential structural pathways than the endogenous inhibitor Zn(2+) for regulation is unknown...
October 7, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27703431/cistanches-herba-a-neuropharmacology-review
#18
Caimei Gu, Xianying Yang, Linfang Huang
Cistanches Herba (family Orobanchaceae), commonly known as "desert ginseng" or Rou Cong Rong, is a global genus and commonly used for its neuroprotective, immunomodulatory, anti-oxidative, kidney impotence, laxative, anti-inflammatory, hepatoprotective, anti-bacterial, anti-viral, and anti-tumor effects in traditional herbal formulations in North Africa, Arabic, and Asian countries. The major bioactive compound present in this plant is phenylethanoid glycosides. In recent years, there has been great important in scientific investigation of the neuropharmacological effects of the bioactive compounds...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27703042/the-iccam-platform-study-an-experimental-medicine-platform-for-evaluating-new-drugs-for-relapse-prevention-in-addiction-part-b-fmri-description
#19
John McGonigle, Anna Murphy, Louise M Paterson, Laurence J Reed, Liam Nestor, Jonathan Nash, Rebecca Elliott, Karen D Ersche, Remy Sa Flechais, Rexford Newbould, Csaba Orban, Dana G Smith, Eleanor M Taylor, Adam D Waldman, Trevor W Robbins, Jf William Deakin, David J Nutt, Anne R Lingford-Hughes, John Suckling
OBJECTIVES: We aimed to set up a robust multi-centre clinical fMRI and neuropsychological platform to investigate the neuropharmacology of brain processes relevant to addiction - reward, impulsivity and emotional reactivity. Here we provide an overview of the fMRI battery, carried out across three centres, characterizing neuronal response to the tasks, along with exploring inter-centre differences in healthy participants. EXPERIMENTAL DESIGN: Three fMRI tasks were used: monetary incentive delay to probe reward sensitivity, go/no-go to probe impulsivity and an evocative images task to probe emotional reactivity...
October 4, 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/27664773/neuropharmacological-evaluation-of-a-novel-5-ht3-receptor-antagonist-4-benzylpiperazin-1-yl-3-methoxyquinoxalin-2-yl-methanone-6g-on-lipopolysaccharide-induced-anxiety-models-in-mice
#20
Shvetank Bhatt, Radhakrishnan Mahesh, Thangaraj Devadoss, Ankur Jindal
BACKGROUND: 5-HT3 receptor antagonists play a key role in the management of psychiatric disorders such as, depression and anxiety. They may act through modulation of serotonergic transmission. In the present study, a novel and potential 5-HT3 receptor antagonist, 6g (4-benzylpiperazin-1-yl)(3-methoxyquinoxalin-2-yl) methanone, which exhibited good log P (3.08) and pA2 (7.5) values was screened for its anxiolytic property in lipopolysaccharide (LPS) induced anxiety models. METHODS: LPS, an endotoxin, present in the cell wall of Gram negative bacteria was injected 0...
September 24, 2016: Journal of Basic and Clinical Physiology and Pharmacology
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