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Neuropharmacology

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https://www.readbyqxmd.com/read/28734870/elucidation-of-the-neural-circuits-activated-by-a-gabab-receptor-positive-modulator-relevance-to-anxiety
#1
REVIEW
Riccardo Pizzo, Olivia F O'Leary, John F Cryan
Although there is much evidence for a role of GABAB receptors in the pathophysiology of anxiety, the underlying neuronal mechanisms are largely unclear. The GABAB receptor allosteric positive modulator, GS39783, exerts anxiolytic effects without interfering with GABAB-mediated modulation of body temperature, cognitive performance and locomotor activity thus offering advantages over GABAB receptor agonists. However, the precise neural circuits underlying the anxiolytic effects of GS39783 are unknown. The aim of the present study was to identify brain structures and associated neuronal circuits that are modulated by GS39783 under either basal or mild stress conditions...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28734869/p2x-receptors-up-regulate-the-cell-surface-expression-of-the-neuronal-glycine-transporter-glyt2
#2
Lucía Villarejo-López, Esperanza Jiménez, David Bartolomé-Martín, Francisco Zafra, Pablo Lapunzina, Carmen Aragón, Beatriz López-Corcuera
Glycinergic inhibitory neurons of the spinal dorsal horn exert critical control over the conduction of nociceptive signals to higher brain areas. The neuronal glycine transporter 2 (GlyT2) is involved in the recycling of synaptic glycine from the inhibitory synaptic cleft and its activity modulates intra and extracellular glycine concentrations. In this report we show that the stimulation of P2X purinergic receptors with βγ-methylene adenosine 5'-triphosphate induces the up-regulation of GlyT2 transport activity by increasing total and plasma membrane expression and reducing transporter ubiquitination...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28734868/a-single-and-multiple-dose-study-to-investigate-the-pharmacokinetics-and-pharmacodynamics-of-opicapone-a-novel-comt-inhibitor-in-rat
#3
Daniela Gonçalves, Gilberto Alves, Ana Fortuna, Maria João Bonifácio, Patrício Soares-da-Silva, Amílcar Falcão
Opicapone is a novel catechol-O-methyltransferase (COMT) inhibitor that emerged to fulfil the need of a safer and more efficacious COMT inhibitor. The present study was carried out in order to assess and compare the pharmacokinetics and pharmacodynamics (COMT inhibition) of opicapone after single and multiple oral administrations (30 mg/kg) to Wistar rats. For this purpose, at predefined time points up to 72 h post-dosing, blood, liver and kidneys were collected and, then, the concentrations of opicapone and its active metabolite (BIA 9-1079) were determined in plasma and in liver and kidney tissues, as well as the erythrocyte, liver and kidney COMT activity...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28734867/p-q-type-voltage-gated-calcium-channels-mediate-the-ethanol-and-crf-sensitivity-of-central-amygdala-gabaergic-synapses
#4
F P Varodayan, M L Logrip, M Roberto
The central amygdala (CeA) GABAergic system is hypothesized to drive the development of alcohol dependence, due to its pivotal roles in the reinforcing actions of alcohol and the expression of negative emotion, anxiety and stress. Recent work has also identified an important role for the CeA corticotropin-releasing factor (CRF) system in the interaction between anxiety/stress and alcohol dependence. We have previously shown that acute alcohol and CRF each increase action potential-independent GABA release in the CeA via their actions at presynaptic CRF type 1 receptors (CRF1s); however, the shared mechanism employed by these two compounds requires further investigation...
July 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28729222/antiallodynic-effect-of-%C3%AE-caryophyllene-on-paclitaxel-induced-peripheral-neuropathy-in-mice
#5
Gabriela C Segat, Mariane N Manjavachi, Daiane O Matias, Giselle F Passos, Cristina Setim Freitas, Robson Costa, João B Calixto
Painful peripheral neuropathy is a common side effect of paclitaxel (PTX). The use of analgesics is an important component for management of PTX-induced peripheral neuropathy (PINP). However, currently employed analgesics have several side effects and are poorly effective. β-caryophyllene (BCP), a dietary selective CB2 agonist, has shown analgesic effect in neuropathic pain models, but its role in chemotherapy-induced neuropathic pain has not yet been investigated. Herein, we used the mouse model of PINP to show the therapeutic effects of BCP in this neuropathy...
July 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28729221/sensitivity-to-cocaine-in-adult-mice-is-due-to-interplay-between-genetic-makeup-early-environment-and-later-experience
#6
Matteo Di Segni, Diego Andolina, Alessandra Coassin, Alessandra Accoto, Alessandra Luchetti, Tiziana Pascucci, Carla Luzi, Anna Rita Lizzi, Francesca R D'Amato, Rossella Ventura
Although early aversive postnatal events are known to increase the risk to develop psychiatric disorders later in life, rarely they determine alone the nature and outcome of the psychopathology, indicating that interaction with genetic factors is crucial for expression of psychopathologies in adulthood. Moreover, it has been suggested that early life experiences could have negative consequences or confer adaptive value in different individuals. Here we suggest that resilience or vulnerability to adult cocaine sensitivity depends on a "triple interaction" between genetic makeup x early environment x later experience...
July 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28729220/cognitive-enhancement-and-antipsychotic-like-activity-following-repeated-dosing-with-the-selective-m4-pam-vu0467154
#7
Robert W Gould, Michael D Grannan, Barak W Gunter, Jacob Ball, Michael Bubser, Thomas M Bridges, Jurgen Wess, Michael W Wood, Nicholas J Brandon, Mark E Duggan, Colleen M Niswender, Craig W Lindsley, P Jeffrey Conn, Carrie K Jones
Although selective activation of the M1 muscarinic acetylcholine receptor (mAChR) subtype has been shown to improve cognitive function in animal models of neuropsychiatric disorders, recent evidence suggests that enhancing M4 mAChR function can also improve memory performance. Positive allosteric modulators (PAMs) targeting the M4 mAChR subtype have shown therapeutic potential for the treatment of multiple symptoms observed in schizophrenia, including positive and cognitive symptoms when assessed in acute preclinical dosing paradigms...
July 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28720478/monoamine-receptor-interaction-profiles-of-4-thio-substituted-phenethylamines-2c-t-drugs
#8
REVIEW
Dino Luethi, Daniel Trachsel, Marius C Hoener, Matthias E Liechti
BACKGROUND: 4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs. METHODS: We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters...
July 15, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28716449/venom-derived-peptides-inhibiting-kir-channels-past-present-and-future
#9
REVIEW
Craig A Doupnik
Inwardly rectifying K+ (Kir) channels play a significant role in vertebrate and invertebrate biology by regulating the movement of K+ ions involved in membrane transport and excitability. Yet unlike other ion channels including their ancestral K + -selective homologs, there are very few venom toxins known to target and inhibit Kir channels with the potency and selectivity found for the Ca2+-activated and voltage-gated K+ channel families. It is unclear whether this is simply due to a lack of discovery, or instead a consequence of the evolutionary processes that drive the development of venom components towards their targets based on a collective efficacy to 1) elicit pain for defensive purposes, 2) promote paralysis for prey capture, or 3) facilitate delivery of venom components into the circulation...
July 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28712684/cerebellar-perineuronal-nets-in-cocaine-induced-pavlovian-memory-site-matters
#10
Maria Carbo-Gas, Josep Moreno-Rius, Julian Guarque-Chabrera, Dolores Vazquez-Sanroman, Isis Gil-Miravet, Daniela Carulli, Freek Hoebeek, Chris De Zeeuw, Carla Sanchis-Segura, Marta Miquel
One of the key mechanisms for the stabilization of synaptic changes near the end of critical periods for experience-dependent plasticity is the formation of specific lattice extracellular matrix structures called perineuronal nets (PNNs). The formation of drug memories depends on local circuits in the cerebellum, but it is unclear to what extent it may also relate to changes in their PNN. Here, we investigated changes in the PNNs of the cerebellum following cocaine-induced preference conditioning. The formation of cocaine-related preference memories increased expression of PNN-related proteins surrounding Golgi inhibitory interneurons as well as that of cFos in granule cells at the apex of the cerebellar cortex...
July 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28711518/antagonism-of-the-5-ht6-receptor-preclinical-rationale-for-the-treatment-of-alzheimer-s-disease
#11
REVIEW
Inge E M de Jong, Arne Mørk
Antagonism of the 5-HT6 receptor is a promising approach for the symptomatic treatment of Alzheimer's disease (AD). There is compelling preclinical evidence for the procognitive potential of 5-HT6 receptor antagonists and several compounds are in clinical development, as adjunct therapy to acetylcholinesterase inhibitors (AChEIs). This manuscript summarizes the scientific rationale for the use of 5-HT6 receptor antagonists as AD treatment, with some focus on the selective and high-affinity 5-HT6 receptor antagonist idalopirdine (Lu AE58054)...
July 12, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28709671/mechanism-and-properties-of-positive-allosteric-modulation-of-n-methyl-d-aspartate-receptors-by-6-alkyl-2-naphthoic-acid-derivatives
#12
Kiran Sapkota, Mark W Irvine, Guangyu Fang, Erica S Burnell, Neil Bannister, Arturas Volianskis, Georgia R Culley, Shashank M Dravid, Graham L Collingridge, David E Jane, Daniel T Monaghan
The theory that N-methyl-d-aspartate receptor (NMDAR) hypofunction is responsible for the symptoms of schizophrenia is well supported by many pharmacological and genetic studies. Accordingly, positive allosteric modulators (PAMs) that augment NMDAR signaling may be useful for treating schizophrenia. Previously we have identified several NMDAR PAMs containing a carboxylic acid attached to naphthalene, phenanthrene, or coumarin ring systems. In this study, we describe several functional and mechanistic properties of UBP684, a 2-naphthoic acid derivative, which robustly potentiates agonist responses at each of the four GluN1a/GluN2 receptors and at neuronal NMDARs...
July 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28705440/inhibition-of-trkb-at-the-nucleus-accumbens-using-ana-12-regulates-basal-and-stress-induced-orexin-a-expression-within-the-mesolimbic-system-and-affects-anxiety-sociability-and-motivation
#13
Idu Azogu, Helene Plamondon
Repeated stress exposure can lead to the development of anxiety and mood disorders. An emerging biological substrate of depression and associated pathology is the nucleus accumbens (NAc), which through interactions with limbic, cognitive and motor circuits can regulate a variety of stress responses. Within these circuits, orexin neurons are involved in arousal and stress adaptability, effects proposed mediated via brain-derived neurotrophic factor signaling. This study tested the hypotheses that 1) repeated exposure to heterotypic stress alters social ability and preference and passive avoidant behaviors, 2) TrkB receptors at the NAc shell regulates stress-induced behavioral responses and orexin expression within the mesocorticolimbic system...
July 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28705439/activation-of-nociceptin-orphanin-fq-receptors-inhibits-contextual-fear-memory-reconsolidation
#14
Khaoula Rekik, Raquel Faria Da Silva, Morgane Colom, Salvatore Pacifico, Nurulain T Zaveri, Girolamo Calo', Claire Rampon, Bernard Frances, Lionel Mouledous
Several neuropeptidergic systems act as modulators of cognitive performances. Among them, nociceptin, an opioid-like peptide also known as orphanin FQ (N/OFQ), has recently gained attention. Stimulation of its receptor, the N/OFQ opioid receptor (NOP), which is expressed in brain regions involved in emotion, memory and stress response, has inhibitory effects on the acquisition and/or consolidation of spatial and emotional memory in rodents. Recently, N/OFQ was also proposed to be linked to the pathogenesis of Post-Traumatic Stress Disorder in humans...
July 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28694098/sleep-promoting-potential-of-low-dose-%C3%AE-asarone-in-rat-model
#15
Arathi Radhakrishnan, N Jayakumari, Velayudhan Mohan Kumar, Kamalesh K Gulia
Commonly used hypnotics have undesirable side-effects, especially during continuous usage. On the other hand, some herbal products, which are used for prolonged periods, are suggested to have a sleep inducing property, though the claims have not been validated scientifically. The hypnotic potential of α-Asarone, an active principle of Acorus species, was tested in the present study by first identifying the optimal dose of α-Asarone for improving sleep, followed by studies that evaluated the effect of repeated administration of this optimal dose for five days on sleep deprived rats...
July 8, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28694097/behavioural-pharmacology-of-the-%C3%AE-5-gabaa-receptor-antagonist-s44819-enhancement-and-remediation-of-cognitive-performance-in-preclinical-models
#16
István Gacsályi, Krisztina Móricz, Gábor Gigler, János Wellmann, Katalin Nagy, István Ling, József Barkóczy, József Haller, Jeremy J Lambert, Gábor Szénási, Michael Spedding, Ferenc A Antoni
Previous work has shown that S44819 is a novel GABAA receptor (GABAAR) antagonist, which is selective for extrasynaptic GABAARs incorporating the α5 subunit (α5-GABAARs). The present study reports on the preclinical neuropsychopharmacological profile of S44819. Significantly, no sedative or pro-convulsive side effects of S44819 were found at doses up to 30 mg/kg i.p. Object recognition (OR) memory in intact mice was enhanced by S44819 (0.3 mg/kg p.o.) given before the acquisition trial. Mice treated with phencyclidine for two weeks and tested six days after the cessation of treatment failed to show OR memory...
July 8, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28694099/a-new-dawn-in-cannabinoid-neurobiology-the-road-from-molecules-to-therapeutic-discoveries
#17
EDITORIAL
Joseph Cheer, Yasmin Hurd
No abstract text is available yet for this article.
July 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28689026/venom-peptides-as-pharmacological-tools-and-therapeutics-for-diabetes
#18
REVIEW
Samuel D Robinson, Helena Safavi-Hemami
Diabetes mellitus is a chronic disease caused by a deficiency in production of insulin by the beta cells of the pancreas (type 1 diabetes, T1D), or by partial deficiency of insulin production and the ineffectiveness of the insulin produced (type 2 diabetes, T2D). Animal venoms are a unique source of compounds targeting ion channels and receptors in the nervous and cardiovascular systems. In recent years, several venom peptides have also emerged as pharmacological tools and therapeutics for T1D and T2D. Some of these peptides act directly as mimics of endogenous metabolic hormones while others act on ion channels expressed in pancreatic beta cells...
July 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28689025/venom-derived-peptide-inhibitors-of-voltage-gated-potassium-channels
#19
REVIEW
Raymond S Norton, K George Chandy
Voltage-gated potassium channels play a key role in human physiology and pathology. Reflecting their importance, numerous channelopathies have been characterised that arise from mutations in these channels or from autoimmune attack on the channels. Voltage-gated potassium channels are also the target of a broad range of peptide toxins from venomous organisms, including sea anemones, scorpions, spiders, snakes and cone snails; many of these peptides bind to the channels with high potency and selectivity. In this review we describe the various classes of peptide toxins that block these channels and illustrate the broad range of three-dimensional structures that support channel blockade...
July 5, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28687201/corrigendum-to-a-selective-cb2r-agonist-jwh133-restores-neuronal-circuit-after-germinal-matrix-hemorrhage-in-the-preterm-via-cx3cr1-microglia-neuropharm-119-2017-157-169
#20
Jun Tang, Hongping Miao, Bing Jiang, Qianwei Chen, Liang Tan, Yihao Tao, Jianbo Zhang, Fabao Gao, Hua Feng, Gang Zhu, Zhi Chen
No abstract text is available yet for this article.
July 4, 2017: Neuropharmacology
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