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Neuropharmacology

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https://www.readbyqxmd.com/read/28694764/2-pyrazoline-derivatives-in-neuropharmacology-synthesis-adme-prediction-molecular-docking-and-in-vivo-biological-evaluation
#1
Savita Upadhyay, Avinash C Tripathi, Sarvesh Paliwal, Shailendra K Saraf
A novel series of 1,3,5-trisubstituted-2-pyrazoline derivatives (PFC-1 to PFC-16) were synthesized in a three step reaction using conventional and microwave assisted green chemistry approach. The synthesized derivatives were characterized and their chemical structures were established by various physicochemical methods such as IR, Mass, (1)H-NMR, (13)C-NMR and elemental analysis. The synthesized compounds were tested for their neuropharmacological potential. The compounds exhibited significant antidepressant and anti-anxiety activities against various behavioral in vivo models...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28690441/drugs-the-brain-case-based-instruction-for-an-undergraduate-neuropharmacology-course
#2
Anastasia Nagel, Andrea Nicholas
In order to transform a traditional large non-majors general education (GE) neurobiology lecture (Drugs & the Brain) into an active learning course, we developed a series of directed mini-cases targeting major drug classes. Humorous and captivating case-based situations were used to better engage and motivate students to solve problems related to neuropharmacology and physiology. Here we provide directed cases, questions and learning outcomes for our opiates mini-cases. In addition, we describe how case studies were incorporated into our course and assessed using peer review and online quizzing...
2017: Journal of Undergraduate Neuroscience Education: JUNE: a Publication of FUN, Faculty for Undergraduate Neuroscience
https://www.readbyqxmd.com/read/28690434/don-t-believe-the-gripe-increasing-course-structure-in-a-large-non-majors-neuroscience-course
#3
Anastasia Nagel, Andrea Nicholas
Active teaching is increasingly accepted as a better option for higher education STEM courses than traditional lecture-based instruction. However, concerns remain regarding student preferences and the impact of increased course structure on teaching evaluations. Undergraduates in a non-majors neuropharmacology course were enrolled in an enriched blended course format, providing online case-based learning opportunities in a large lecture hall setting. Students working in small assigned groups solved weekly case studies developed to teach basic neuropharmacology concepts...
2017: Journal of Undergraduate Neuroscience Education: JUNE: a Publication of FUN, Faculty for Undergraduate Neuroscience
https://www.readbyqxmd.com/read/28687902/decreased-brain-serotonin-turnover-rate-following-administration-of-sharbat-e-ahmed-shah-produces-antidepressant-and-anxiolytic-effect-in-rats
#4
Muhammad Ahmed, Aisha Azmat
Sharbat-e-Ahmed Shah (SAS) has usually been used in Traditional Unani Medicine (TUM) for depression and insomnia but still not evaluated for its anti-depressant and Neuropharmacological activity. In the present study, a Human dose of SAS (0.6 ml/kg/d) was administered orally to the rats for 15 consecutive days. Antidepressant and anxiolytic were screened scientifically in rats by using Forced swim test and light and dark box test. At the end of study high-performance liquid chromatographic (HPLC) method with electrochemical (EC) detector was used for the measurement of blood and brain tryptophan and brain serotonin levels...
July 7, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28677669/section-1-neuropharmacology
#5
(no author information available yet)
No abstract text is available yet for this article.
July 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28646714/synthetic-cathinones-and-stereochemistry-s-enantiomer-of-mephedrone-reduces-anxiety-and-depressant-like-effects-in-cocaine-or-mdpv-abstinent-rats
#6
Helene L Philogene-Khalid, Callum Hicks, Allen B Reitz, Lee-Yuan Liu-Chen, Scott M Rawls
BACKGROUND AND PURPOSE: The neuropharmacological profile of the synthetic cathinone mephedrone (MEPH) is influenced by stereochemistry. Both MEPH enantiomers are monoamine transporter substrates, but R-MEPH is primarily responsible for rewarding effects of MEPH as it produces greater locomotor activation and intracranial self-stimulation than S-MEPH. S-MEPH is a 50-fold more potent 5-HT releaser than R-MEPH and does not place preference in rats. MEPH is also structurally similar to the cathinone derivative bupropion, an antidepressant and smoking cessation medication, suggesting MEPH has therapeutic and addictive properties...
June 13, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28626759/sertraline-induces-toxicity-and-behavioral-alterations-in-planarians
#7
Isabela Salvador Thumé, Marcos Emílio Frizzo
Toxicity attributed to sertraline has been demonstrated recently in different cell types and also in some organisms. We investigated the effect of sertraline on planarians, which are considered suitable for investigations in neurotoxicology and currently are widely used as an animal model in neuropharmacological studies. Planarians treated with 10 µM sertraline showed a rapid reduction in their spontaneous movement until they became completely motionless and then showed a series of asynchronous paroxysms (seizures) followed by progressive tissue damage, beginning 48 h after the sertraline treatment, and died approximately 72 h later...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28624433/the-highs-and-lows-of-the-human-brain-on-dopaminergics-evidence-from-neuropharmacology
#8
REVIEW
Daniel Martins, Mitul A Mehta, Diana Prata
Rewards are appetitive events that elicit approach. Ground-breaking findings from neurophysiological experiments in animals, alongside neuropharmacology and neuroimaging research in human samples have identified dopamine as the main neurochemical messenger of global reward processing in the brain. However, dopamine's contribution to the different components of reward processing remains to be precisely defined. To facilitate the informed design and interpretation of reward studies in humans, we have systematically reviewed all existing human pharmacological studies investigating how drug manipulation of the dopamine system affects reward-related behaviour and its neural correlates...
June 15, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28599850/tobacco-and-alcohol-use-during-adolescence-interactive-mechanisms-in-animal-models
#9
REVIEW
Yael Abreu-Villaça, Alex C Manhães, Thomas E Krahe, Claudio C Filgueiras, Anderson Ribeiro-Carvalho
There is a strong association between tobacco smoking and the consumption of alcoholic beverages. When compared to the effects of either drug on its own, the combined use may lead to worsened outcomes, such as less successful quitting attempts and increased likelihood of developing mood disorders. Co-consumption most frequently begins during adolescence, a developmental period that is characterized by an increased risk for substance use disorders. However, to date, most studies that have contributed to the current state of knowledge on the mechanisms that underlie tobacco or alcohol use/abuse, and their consequences, adopted adult animal models...
June 6, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28592904/non-motor-features-of-parkinson-disease
#10
REVIEW
Anthony H V Schapira, K Ray Chaudhuri, Peter Jenner
Many of the motor symptoms of Parkinson disease (PD) can be preceded, sometimes for several years, by non-motor symptoms that include hyposmia, sleep disorders, depression and constipation. These non-motor features appear across the spectrum of patients with PD, including individuals with genetic causes of PD. The neuroanatomical and neuropharmacological bases of non-motor abnormalities in PD remain largely undefined. Here, we discuss recent advances that have helped to establish the presence, severity and effect on the quality of life of non-motor symptoms in PD, and the neuroanatomical and neuropharmacological mechanisms involved...
July 2017: Nature Reviews. Neuroscience
https://www.readbyqxmd.com/read/28588463/looking-for-the-self-phenomenology-neurophysiology-and-philosophical-significance-of-drug-induced-ego-dissolution
#11
Raphaël Millière
There is converging evidence that high doses of hallucinogenic drugs can produce significant alterations of self-experience, described as the dissolution of the sense of self and the loss of boundaries between self and world. This article discusses the relevance of this phenomenon, known as "drug-induced ego dissolution (DIED)", for cognitive neuroscience, psychology and philosophy of mind. Data from self-report questionnaires suggest that three neuropharmacological classes of drugs can induce ego dissolution: classical psychedelics, dissociative anesthetics and agonists of the kappa opioid receptor (KOR)...
2017: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/28584928/effects-of-the-serotonin-2c-receptor-agonist-way163909-on-the-abuse-related-effects-and-mesolimbic-dopamine-neurochemistry-induced-by-abused-stimulants-in-rhesus-monkeys
#12
Laís F Berro, Maylen Perez Diaz, Eric Maltbie, Leonard L Howell
RATIONALE: Accumulating evidence shows that the serotonergic system plays a major role in psychostimulant abuse through its interactions with the dopaminergic system. Studies indicate that serotonin 5-HT2C receptors are one of the main classes of receptors involved in mediating the influence of serotonin in drug abuse. OBJECTIVE: The aim of the present study was to evaluate the effects of the selective serotonin 5-HT2C receptor agonist WAY163909 on the behavioral neuropharmacology of cocaine and methamphetamine in adult rhesus macaques...
June 5, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28580629/three-dimensional-patterning-in-biomedicine-importance-and-applications-in-neuropharmacology
#13
REVIEW
Ajay Vikram Singh, Tanmay Gharat, Madu Batuwangala, Byung-Wook Park, Thomas Endlein, Metin Sitti
Nature manufactures biological systems in three dimensions with precisely controlled spatiotemporal profiles on hierarchical length and time scales. In this article, we review 3D patterning of biological systems on synthetic platforms for neuropharmacological applications. We briefly describe 3D versus 2D chemical and topographical patterning methods and their limitations. Subsequently, an overview of introducing a third dimension in neuropharmacological research with delineation of chemical and topographical roles is presented...
June 5, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
https://www.readbyqxmd.com/read/28552344/neurochemical-and-neuropharmacological-characterization-of-asp2905-a-novel-potent-selective-inhibitor-of-the-potassium-channel-kcnh3
#14
Shinji Takahashi, Kohei Inamura, Junko Yarimizu, Mayako Yamazaki, Nobuhito Murai, Keni Ni
KCNH3 (BEC1) is a member of the ether-à-go-go (KCNH) family of voltage-gated K(+) channels. The aim of this study was to determine the pharmacological profiles in vitro and in vivo of a KCNH3 inhibitor N-(4-fluorophenyl)-N'-phenyl-N''-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (ASP2905). We analyzed the effects of ASP2905 on channel activity in vitro and its neuropharmacological properties in young and aged rats as well as in mice. ASP2905 potently inhibited potassium currents in CHO cells expressing KCNH3 (IC50 = 9...
May 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28549933/orexin-exerts-excitatory-effects-on-reticulospinal-neurons-in-the-rat-gigantocellular-reticular-nucleus-through-the-activation-of-postsynaptic-orexin-1-and-orexin-2-receptors
#15
Nian Yang, Guan-Zhong Wang, Si-Yi Wen, Qi-Cheng Qiao, Yu-Hui Liu, Jun Zhang
Previous studies have revealed that orexin may actively participate in central motor control. The gigantocellular reticular nucleus (Gi) is a key element of the brainstem motor inhibitory system. The descending orexinergic projections also reach Gi region, and microinjection of orexin into Gi causes robust muscle tone inhibition. However, the modulation effects of orexin on Gi neurons remain unclear. In the present study, using whole-cell patch-clamp recordings, we initially observed that orexin elicited an inward current in Gi neurons at a holding potential of -70mV in a concentration-dependent manner...
July 13, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28539997/interaction-between-the-cannabinoid-and-vanilloid-systems-on-anxiety-in-male-rats
#16
Nafiseh Faraji, Alireza Komaki, Iraj Salehi
INTRODUCTION: Previous studies have shown that the cannabinoid system is involved in anxiety. In addition, transient receptor potential vanilloid type-1 (TRPV1) channels are new targets for the development of anxiolytics. The present study investigated the possible interaction between the cannabinoid and vanilloid systems on anxiety-like behavior in rats. METHODS: Four different groups of male Wistar rats received intraperitoneal (IP) injections of (1) vehicle (DMSO+saline), (2) cannabinoid receptor agonist WIN55212-2 (WIN) (1 mg/kg), (3) TRPV1 receptor antagonist capsazepine (CPZ) (5 mg/kg), or (4) combined WIN (1 mg/kg) and CPZ (5 mg/kg) treatment 30 minutes before testing in the elevated plus maze...
March 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28518109/assessment-of-neuronal-viability-using-fluorescein-diacetate-propidium-iodide-double-staining-in-cerebellar-granule-neuron-culture
#17
Lin Jiajia, Mak Shinghung, Zheng Jiacheng, Wang Jialing, Xu Dilin, Hu Shengquan, Zhang Zaijun, Wang Qinwen, Han Yifan, Cui Wei
Primary cultured Cerebellar Granule Neurons (CGNs) have been widely used as an in vitro model in neuroscience and neuropharmacology research. However, the co-existence of glial cells and neurons in CGN culture might lead to biases in the accurate assessment of neuronal viability. Fluorescein diacetate (FDA) and Propidium Iodide (PI) double staining has been used to measure cell viability by simultaneously evaluating the viable and dead cells. We used FDA-PI double staining to improve the sensitivities of the colorimetric assays and to evaluate neuronal viability in CGNs...
May 10, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28495376/gabaa-receptor-positive-allosteric-modulators-modify-the-abuse-related-behavioral-and-neurochemical-effects-of-methamphetamine-in-rhesus-monkeys
#18
Laís F Berro, Monica L Andersen, Sergio Tufik, Leonard L Howell
GABAA receptor positive allosteric modulators (GABAA receptor modulators) are commonly used for the treatment of insomnia. Nevertheless, the effects of these compounds on psychostimulant-induced sleep impairment are poorly understood. Because GABAA receptor modulators have been shown to decrease the abuse-related effects of psychostimulants, the aim of the present study was to evaluate the effects of temazepam (0.3, 1.0 or 3.0 mg/kg) and eszopiclone (0.3, 1.0 or 3.0 mg/kg), two GABAA receptor modulators, on the behavioral neuropharmacology of methamphetamine in adult rhesus macaques (n = 5)...
September 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28480400/isolation-of-novel-para-pentyl-phenyl-benzoate-from-mondia-whitei-hook-f-skeels-periplocaceae-its-structure-synthesis-and-neuropharmacological-evaluation
#19
Taiwo Bamigboye J, Osasan Josephine Y, Olubiyi Olujide O, Oyemitan Idris A, Atoyebi Shakir A M, Elsegood Mark R J, Jones Raymond C F
BACKGROUND: Mondia whitei L. (Hook. F.) Skeels (Periplocaceae) is a medicinal plant used locally in managing pain, fever, loss of appetite and as aphrodiasc in the South-Western states of Nigeria. However, the fruit is consumed habitually in the South-Eastern states of Nigeria, leading to speculation that it may possess some central nervous system effect but which has not been scientifically investigated, hence this study. METHODOLOGY: Fresh fruits of Mondia whitei were collected and identified by a taxonomist...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28472675/toxic-essential-oils-part-v-behaviour-modulating-and-toxic-properties-of-thujones-and-thujone-containing-essential-oils-of-salvia-officinalis-l-artemisia-absinthium-l-thuja-occidentalis-l-and-tanacetum-vulgare-l
#20
Niko S Radulović, Marija S Genčić, Nikola M Stojanović, Pavle J Randjelović, Zorica Z Stojanović-Radić, Nenad I Stojiljković
Neurotoxic thujones (α- and β-diastereoisomers) are common constituents of plant essential oils. In this study, we employed a statistical approach to determine the contribution of thujones to the overall observed behaviour-modulating and toxic effects of essential oils (Salvia officinalis L., Artemisia absinthium L., Thuja occidentalis L. and Tanacetum vulgare L.) containing these monoterpene ketones. The data from three in vivo neuropharmacological tests on rats (open field, light-dark, and diazepam-induced sleep), and toxicity assays (brine shrimp, and antimicrobial activity against a panel of microorganisms), together with the data from detailed chemical analyses, were subjected to a multivariate statistical treatment to reveal the possible correlation(s) between the content of essential-oil constituents and the observed effects...
May 1, 2017: Food and Chemical Toxicology
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