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Neuropharmacology

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https://www.readbyqxmd.com/read/28416445/%C3%AE-o-conotoxin-gexiva-disulfide-bond-isomers-exhibit-differential-sensitivity-for-various-nicotinic-acetylcholine-receptors-but-retain-potency-and-selectivity-for-the-human-%C3%AE-9%C3%AE-10-subtype
#1
Dongting Zhangsun, Xiaopeng Zhu, Quentin Kaas, Yong Wu, David J Craik, J Michael McIntosh, Sulan Luo
Nicotinic acetylcholine receptor (nAChR) subtypes exhibit distinct neuropharmacological properties that are involved in a range of neuropathological conditions, including pain, addiction, epilepsy, autism, schizophrenia, Tourette's syndrome, Alzheimer's and Parkinson's diseases, as well as many types of cancer. The α9α10 nAChR is a potential target in chronic pain, wound healing, the pathophysiology of the auditory system, and breast and lung cancers. αO-conotoxin GeXIVA is a potent antagonist of rat α9α10 nAChRs, with the 'bead' disulfide bond isomer displaying the lowest IC50 of the three possible isomers...
April 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28415443/3-month-parenteral-plga-microsphere-formulations-of-risperidone-fabrication-characterization-and-neuropharmacological-assessments
#2
Sundeep Chaurasia, Kuchukuntla Mounika, Vasudha Bakshi, Vure Prasad
The study aims at formulation and characterization of three months parenteral risperidone loaded polymeric microspheres (p-RLPMs) as a sustained delivery system and established their in vitro and in vivo assessments. The p-RLPMs formulations were prepared by solvent extraction and diffusion method. The optimized p-RLPMs (batch RPLGA-1) formulation demonstrated favorable different physicochemical properties such as mean particle size (104±5.34μm), percent porosity (44.56±3.11%) and percent drug loading (38...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28385956/deconstructing-behavioral-neuropharmacology-with-cellular-specificity
#3
Brenda C Shields, Elizabeth Kahuno, Charles Kim, Pierre F Apostolides, Jennifer Brown, Sarah Lindo, Brett D Mensh, Joshua T Dudman, Luke D Lavis, Michael R Tadross
Behavior has molecular, cellular, and circuit determinants. However, because many proteins are broadly expressed, their acute manipulation within defined cells has been difficult. Here, we combined the speed and molecular specificity of pharmacology with the cell type specificity of genetic tools. DART (drugs acutely restricted by tethering) is a technique that rapidly localizes drugs to the surface of defined cells, without prior modification of the native target. We first developed an AMPAR antagonist DART, with validation in cultured neuronal assays, in slices of mouse dorsal striatum, and in behaving mice...
April 7, 2017: Science
https://www.readbyqxmd.com/read/28377723/multiple-psychopharmacological-effects-of-the-traditional-japanese-kampo-medicine-yokukansan-and-the-brain-regions-it-affects
#4
REVIEW
Kazushige Mizoguchi, Yasushi Ikarashi
Yokukansan (YKS), a traditional Japanese Kampo medicine, has indications for use in night crying and irritability in children, as well as neurosis and insomnia. It is currently also used for the remedy of the behavioral and psychological symptoms of dementia (BPSD), such as aggressiveness, agitation, and hallucinations. In parallel with clinical evidence, a significant amount of fundamental researches have been undertaken to clarify the neuropsychopharmacological efficacies of YKS, with approximately 70 articles, including our own, being published to date...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28349209/phenytoin-a-step-by-step-insight-into-its-multiple-mechanisms-of-action-80%C3%A2-years-of-mechanistic-studies-in-neuropharmacology
#5
Jan M Keppel Hesselink
No abstract text is available yet for this article.
March 27, 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28347784/a-programmable-smoke-delivery-device-for-pet-imaging-with-cigarettes-containing-11-c-nicotine
#6
Yantao Zuo, Pradeep K Garg, Rachid Nazih, Sudha Garg, Jed E Rose, Thangaraju Murugesan, Alexey G Mukhin
INTRODUCTION: PET imaging with (11)C-nicotine-loaded cigarettes is a valuable tool to directly assess fast nicotine kinetics and its neuropharmacological role in tobacco dependence. To eliminate variations among puffs inhaled by subjects, this work aimed to develop a programmable smoke delivery device (SDD) to produce highly reproducible and adjustable puffs of cigarette smoke for PET experiments. NEW METHOD: The SDD was built around a programmable syringe pump as a smoking machine to draw a puff of smoke from a (11)C-nicotine-loaded cigarette and make it available for a subject to take the smoke into the mouth and then inhale it during PET data acquisition...
March 25, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28259728/neurobiology-and-neuropharmacology-of-monoaminergic-systems
#7
EDITORIAL
Philippe De Deurwaerdère, Rona R Ramsay, Giuseppe Di Giovanni
No abstract text is available yet for this article.
April 2017: Progress in Neurobiology
https://www.readbyqxmd.com/read/28250733/a-new-computational-approach-for-modeling-diffusion-tractography-in-the-brain
#8
REVIEW
Harsha T Garimella, Reuben H Kraft
Computational models provide additional tools for studying the brain, however, many techniques are currently disconnected from each other. There is a need for new computational approaches that span the range of physics operating in the brain. In this review paper, we offer some new perspectives on how the embedded element method can fill this gap and has the potential to connect a myriad of modeling genre. The embedded element method is a mesh superposition technique used within finite element analysis. This method allows for the incorporation of axonal fiber tracts to be explicitly represented...
January 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28237670/commentary-toshio-narahashi-life-and-legacy-of-the-founding-father-of-cellular-neuropharmacology
#9
Vincent L Salgado, Xilong Zhao
No abstract text is available yet for this article.
February 22, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/28219076/effect-of-n-benzylpiperazine-its-metabolite-n-benzylethylenediamine-and-its-disubstituted-analogue-n-n-dibenzylpiperazine-on-the-acquisition-formation-and-consolidation-of-memory-in-mice
#10
Juan Carlos Castillo-Hernández, Josué A Velázquez-Moyado, Adelfo Reyes-Ramírez, Elena G Ramírez-López, Martín González-Andrade, Andrés Navarrete
BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. These compounds increase the release of dopamine and serotonin. BZP mimics the psychoactive effects of 3,4-methylenedioxymethylamphetamine. BZP is metabolized to N-benzylethylenediamine (BEDA) and benzylamine. The compound N,N'-dibenzylpiperazine (DBZP) is obtained as a byproduct during the synthesis of BZP. Some PZDs have shown effects on memory; however, there are no previous reports on the activity of BZP, BEDA, and DBZP on memory or on a description of their neuropharmacological profile...
2017: Pharmacology
https://www.readbyqxmd.com/read/28217866/zebrafish-models-in-neuropsychopharmacology-and-cns-drug-discovery
#11
REVIEW
Kanza M Khan, Adam D Collier, Darya A Meshalkina, Elana V Kysil, Sergey L Khatsko, Tatyana Kolesnikova, Yury Yu Morzherin, Jason E Warnick, Allan V Kalueff, David J Echevarria
Despite the high prevalence of neuropsychiatric disorders, their aetiology and molecular mechanisms remain poorly understood. The zebrafish (Danio rerio) is increasingly utilized as a powerful animal model in neuropharmacology research and in vivo drug screening. Collectively, this makes zebrafish a useful tool for drug discovery and the identification of disordered molecular pathways. Here, we discuss zebrafish models of selected human neuropsychiatric disorders and drug-induced phenotypes. As well as covering a broad range of brain disorders (from anxiety and psychoses to neurodegeneration), we also summarize recent developments in zebrafish genetics and small molecule screening, which markedly enhance the disease modelling and the discovery of novel drug targets...
February 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28199192/convergence-of-neurotransmissions-at-synapse-on-ieg-regulation-in-nucleus
#12
Mamoru Fukuchi, Masaaki Tsuda
There is no doubt that synaptic activity-regulated expression of immediate early genes (IEGs) contributes to long-lasting changes in neural functions, including learning and memory. Consequently, dysregulation of IEG expression has been involved in the conditions of neural and psychiatric disorders and cognitive dysfunction. This has mainly been demonstrated using genetically modified animal models and neuropharmacological analyses. The regulatory mechanisms of IEG expression have been investigated recently and have re-emphasized the role of IEG expression in plasticity-related processes as well as elucidating molecular mechanisms and drug targets for neurological and psychiatric disorders...
March 1, 2017: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/28186121/astrocyte-deletion-of-bmal1-alters-daily-locomotor-activity-and-cognitive-functions-via-gaba-signalling
#13
Olga Barca-Mayo, Meritxell Pons-Espinal, Philipp Follert, Andrea Armirotti, Luca Berdondini, Davide De Pietri Tonelli
Circadian rhythms are controlled by a network of clock neurons in the central pacemaker, the suprachiasmatic nucleus (SCN). Core clock genes, such as Bmal1, are expressed in SCN neurons and in other brain cells, such as astrocytes. However, the role of astrocytic clock genes in controlling rhythmic behaviour is unknown. Here we show that ablation of Bmal1 in GLAST-positive astrocytes alters circadian locomotor behaviour and cognition in mice. Specifically, deletion of astrocytic Bmal1 has an impact on the neuronal clock through GABA signalling...
February 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/28178362/determination-of-the-neuropharmacological-drug-nodakenin-in-rat-plasma-and-brain-tissues-by-liquid-chromatography-tandem-mass-spectrometry-application-to-pharmacokinetic-studies
#14
Yingshi Song, Huiyu Yan, Jingbo Xu, Hongxi Ma
A rapid and sensitive liquid chromatography tandem mass spectrometry detection using SRM in positive ionization mode was developed and validated for the quantification of nodakenin in rat plasma and brain. Pareruptorin A was used as internal standard. A single step liquid-liquid extraction was used for plasma and brain sample preparation. The method was validated with respect to selectivity, precision, accuracy, linearity, limit of quantification, recovery, matrix effect and stability. Lower limit of quantification of nodakenin was 2...
February 8, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28134302/implication-of-dorsostriatal-d3-receptors-in-motivational-processes-a-potential-target-for-neuropsychiatric-symptoms-in-parkinson-s-disease
#15
Mathieu Favier, Carole Carcenac, Guillaume Drui, Yvan Vachez, Sabrina Boulet, Marc Savasta, Sebastien Carnicella
Beyond classical motor symptoms, motivational and affective deficits are frequently observed in Parkinson's disease (PD), dramatically impairing the quality of life of patients. Using bilateral 6-hydroxydopamine (6-OHDA) lesions of the substantia nigra pars compacta (SNc) in rats, we have been able to reproduce these neuropsychiatric/non-motor impairments. The present study describes how bilateral 6-OHDA SNc lesions affect the function of the main striatal dopaminergic (DA) receptor subtypes. Autoradiography was used to measure the levels of striatal DA receptors, and operant sucrose self-administration and neuropharmacological approaches were combined to investigate the causal implication of specific DA receptors subtypes in the motivational deficits induced by a dorsostriatal DA denervation...
January 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28132813/the-fabric-of-meaning-and-subjective-effects-in-lsd-induced-states-depend-on-serotonin-2a-receptor-activation
#16
Katrin H Preller, Marcus Herdener, Thomas Pokorny, Amanda Planzer, Rainer Kraehenmann, Philipp Stämpfli, Matthias E Liechti, Erich Seifritz, Franz X Vollenweider
A core aspect of the human self is the attribution of personal relevance to everyday stimuli enabling us to experience our environment as meaningful [1]. However, abnormalities in the attribution of personal relevance to sensory experiences are also critical features of many psychiatric disorders [2, 3]. Despite their clinical relevance, the neurochemical and anatomical substrates enabling meaningful experiences are largely unknown. Therefore, we investigated the neuropharmacology of personal relevance processing in humans by combining fMRI and the administration of the mixed serotonin (5-HT) and dopamine receptor (R) agonist lysergic acid diethylamide (LSD), well known to alter the subjective meaning of percepts, with and without pretreatment with the 5-HT2AR antagonist ketanserin...
February 6, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28131721/effects-of-acetylcholine-and-cholinergic-antagonists-on-the-activity-of-nucleus-of-the-solitary-tract-neurons
#17
Werner I Furuya, Eduardo Colombari, Alastair V Ferguson, Débora S A Colombari
Previously we have demonstrated that microinjection of acetylcholine (ACh) into the intermediate nucleus of the solitary tract (iNTS) induced sympatho-inhibition combined with a decrease in the phrenic nerve activity (PNA), whereas in the commissural NTS (cNTS), ACh did not change sympathetic nerve activity (SNA), but increased the PNA. In view of these demonstrated distinctive effects of ACh in different subnuclei of the NTS the current studies were undertaken to examine, using patch clamp techniques, the specific effects of ACh on the excitability of individual neurons in the NTS, as well as the neuropharmacology of these actions...
January 25, 2017: Brain Research
https://www.readbyqxmd.com/read/28125955/editorial-thematic-selection-spinal-neuropharmacological-agents-for-the-management-of-pain
#18
EDITORIAL
Rui V Duarte, Jon H Raphael, Sam Eldabe
No abstract text is available yet for this article.
2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28100828/an-integrated-modelling-framework-for-neural-circuits-with-multiple-neuromodulators
#19
Alok Joshi, Vahab Youssofzadeh, Vinith Vemana, T M McGinnity, Girijesh Prasad, KongFatt Wong-Lin
Neuromodulators are endogenous neurochemicals that regulate biophysical and biochemical processes, which control brain function and behaviour, and are often the targets of neuropharmacological drugs. Neuromodulator effects are generally complex partly owing to the involvement of broad innervation, co-release of neuromodulators, complex intra- and extrasynaptic mechanism, existence of multiple receptor subtypes and high interconnectivity within the brain. In this work, we propose an efficient yet sufficiently realistic computational neural modelling framework to study some of these complex behaviours...
January 2017: Journal of the Royal Society, Interface
https://www.readbyqxmd.com/read/28078250/effects-of-mimosa-pudica-l-leaves-extract-on-anxiety-depression-and-memory
#20
Ganesh Patro, Subrat Kumar Bhattamisra, Bijay Kumar Mohanty
OBJECTIVE: The present study was carried out to investigate the neuropharmacological activities of ethyl acetate extract of Mimosa pudica (EAMP) leaves on anxiety, depression and memory in a mouse model. MATERIALS AND METHODS: Anti-anxiety potential of EAMP was evaluated by elevated plus maze (EPM), light-dark box (LDB) and social interaction (SI) tests in mice.Anti-depressant potential of EAMP was evaluated by forced swimming (FST), tail suspension (TST), and open field tests (OFT)...
November 2016: Avicenna Journal of Phytomedicine
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