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Neuropharmacology

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https://www.readbyqxmd.com/read/28327374/discovery-and-molecular-interaction-studies-of-a-highly-stable-tarantula-peptide-modulator-of-acid-sensing-ion-channel-1
#1
REVIEW
Sing Yan Er, Ben Cristofori-Armstrong, Pierre Escoubas, Lachlan D Rash
Acute pharmacological inhibition of acid-sensing ion channel 1a (ASIC1a) is efficacious in rodent models in alleviating symptoms of neurological diseases such as stroke and multiple sclerosis. Thus, ASIC1a is a promising therapeutic target and selective ligands that modulate it are invaluable research tools and potential therapeutic leads. Spider venoms have provided an abundance of voltage-gated ion channel modulators, however, only one ASIC modulator (PcTx1) has so far been isolated from this source. Here we report the discovery, characterization, and chemical stability of a second spider venom peptide that potently modulates ASIC1a and ASIC1b, and investigate the molecular basis for its subtype selectivity...
March 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28322978/delta-opioid-receptor-antagonism-leads-to-excessive-ethanol-consumption-in-mice-with-enhanced-activity-of-the-endogenous-opioid-system
#2
Piotr Poznanski, Anna Lesniak, Michal Korostynski, Klaudia Szklarczyk, Marzena Lazarczyk, Piotr Religa, Magdalena Bujalska-Zadrozny, Bogdan Sadowski, Mariusz Sacharczuk
The opioid system modulates the central reinforcing effects of ethanol and participates in the etiology of addiction. However, the pharmacotherapy of ethanol dependence targeted on the opioid system is little effective and varies due to individual patients' sensitivity. In the present study, we used two mouse lines with high (HA) and low (LA) activity of the endogenous opioid system to analyze the effect of opioid receptor blockade on ethanol drinking behavior. We found that LA and HA lines characterized by divergent magnitudes of swim stress-induced analgesia also differ in ethanol intake and preference...
March 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28322980/role-of-perineuronal-nets-in-the-anterior-dorsal-lateral-hypothalamic-area-in-the-acquisition-of-cocaine-induced-conditioned-place-preference-and-self-administration
#3
Jordan M Blacktop, Ryan P Todd, Barbara A Sorg
Addiction involves drug-induced neuroplasticity in the circuitry of motivated behavior, which includes the medial forebrain bundle and the lateral hypothalamic area. Emerging at the forefront of neuroplasticity regulation are specialized extracellular matrix (ECM) structures that form perineuronal nets (PNNs) around certain neurons, mainly parvalbumin positive (PV(+)), fast-spiking interneurons (FSINs), making them a promising target for the regulation of drug-induced neuroplasticity. Despite the emerging significance of PNNs in drug-induced neuroplasticity and the well-established role of the lateral hypothalamic area (LHA) in reward, reinforcement, and motivation, very little is known about how PNN-expressing neurons control drug-seeking behavior...
March 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28322979/3-4-methylenedioxymethamphetamine-mdma-ecstasy-produces-edema-due-to-bbb-disruption-induced-by-mmp-9-activation-in-rat-hippocampus
#4
Mercedes Pérez-Hernández, María Encarnación Fernández-Valle, Ana Rubio-Araiz, Rebeca Vidal, María Dolores Gutiérrez-López, Esther O'Shea, María Isabel Colado
The recreational drug of abuse, 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) disrupts blood-brain barrier (BBB) integrity in rats through an early P2X7 receptor-mediated event which induces MMP-9 activity. Increased BBB permeability often causes plasma proteins and water to access cerebral tissue leading to vasogenic edema formation. The current study was performed to examine the effect of a single neurotoxic dose of MDMA (12.5 mg/kg, i.p.) on in vivo edema development associated with changes in the expression of the perivascular astrocytic water channel, AQP4, as well as in the expression of the tight-junction (TJ) protein, claudin-5 and Evans Blue dye extravasation in the hippocampus of adult male Dark Agouti rats...
March 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28315352/bilirubin-and-brain-a-pharmacological-approach
#5
REVIEW
Cesare Mancuso
For many decades, the world scientific literature has accounted for a number of works on the biological effects of bilirubin-IXalpha (BR). The first studies focused on the neurotoxic effects of the excessive production of BR, in particular regarding both physiological neonatal jaundice and the more severe ones, typically as consequences of severe hemolysis or other underlying diseases. Only since 1987, has significant evidence, however, underlined the neuroprotective role of BR linked to the scavenging effect of free radicals as reactive oxygen species and nitric oxide and its congeners...
March 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28315351/-3-h-bmt-046091-a-potent-and-selective-radioligand-to-determine-aak1-distribution-and-target-engagement
#6
Justin V Louis, Yifeng Lu, Rick Pieschl, Yung Tian, Yang Hong, Kumaran Dandapani, Sreenivasulu Naidu, Reeba K Vikramadithyan, Carolyn Dzierba, Sarat Kumar Sarvasiddhi, Susheel J Nara, Joanne Bronson, John E Macor, Charlie Albright, Walter Kostich, Yu-Wen Li
Adaptor-associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of serine/threonine kinases, plays a role in modulating clatherin coated endocytosis of specific surface receptors. We have demonstrated that AAK1 inhibitors are efficacious in rodent models of neuropathic pain (Kostich et al., 2016). Here we have characterized the binding properties and distribution pattern of the tritiated AAK1 radioligand, [(3)H]BMT-046091, in rodents and cynomolgus monkeys, and used the radioligand to measure the brain target occupancy following systemic administration of AAK1 inhibitors...
March 14, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28302570/hippocampal-endothelin-1-decreases-excitability-of-pyramidal-neurons-and-produces-anxiolytic-effects
#7
Ming Chen, Shu Shu, Huan-Huan Yan, Lei Pei, Ze-Fen Wang, Qi Wan, Lin-Lin Bi
Anxiety disorders contribute to the pathophysiology of psychiatric diseases, including major depression, substance abuse, and schizophrenia. The hippocampus is important for anxiety modulation. However, the mechanisms that control the neuronal activity of the hippocampus in anxiety are still not clear. We found that Endothelin-1 (ET1) mRNA in the hippocampus was down-regulated in high-anxiety mice. Neutralizing endogenous ET1 in the hippocampal CA1 enhanced anxiety-like behaviors. We next revealed that most expression of ET1 and its receptors in the CA1 takes place in pyramidal neurons, and the ET1 signaling pathway directly regulated the excitability of CA1 pyramidal neurons and glutamatergic synaptic neurotransmission...
March 13, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28300552/monoaminergic-modulation-of-gabaergic-transmission-onto-cerebellar-globular-cells
#8
Moritoshi Hirono, Soichi Nagao, Yuchio Yanagawa, Shiro Konishi
Cerebellar Purkinje cells (PCs) project their axon collaterals to underneath of the PC layer and make GABAergic synaptic contacts with globular cells, a subgroup of Lugaro cells. GABAergic transmission derived from the PC axon collaterals is so powerful that it could inhibit globular cells and regulate their firing patterns. However, the physiological properties and implications of the GABAergic synapses on globular cells remain unknown. Using whole-cell patch-clamp recordings from globular cells in the mouse cerebellum, we examined the monoaminergic modulation of GABAergic inputs to these cells...
March 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28288815/rf313-an-orally-bioavailable-neuropeptide-ff-receptor-antagonist-opposes-effects-of-rf-amide-related-peptide-3-and-opioid-induced-hyperalgesia-in-rodents
#9
Khadija Elhabazi, Jean-Paul Humbert, Isabelle Bertin, Raphaelle Quillet, Valérie Utard, Martine Schmitt, Jean-Jacques Bourguignon, Emilie Laboureyras, Meric Ben Boujema, Guy Simonnet, Caroline Ancel, Valérie Simonneaux, Massimiliano Beltramo, Bernard Bucher, Tania Sorg, Hamid Meziane, Elodie Schneider, Benoit Petit-Demoulière, Brigitte Ilien, Frédéric Bihel, Frédéric Simonin
Although opiates represent the most effective analgesics, their use in chronic treatments is associated with numerous side effects including the development of pain hypersensitivity and analgesic tolerance. We recently identified a novel orally active neuropeptide FF (NPFF) receptor antagonist, RF313, which efficiently prevents the development of fentanyl-induced hyperalgesia in rats. In this study, we investigated the properties of this compound into more details. We show that RF313 exhibited a pronounced selectivity for NPFF receptors, antagonist activity at NPFF1 receptor (NPFF1R) subtype both in vitro and in vivo and no major side effects when administered in mice up to 30 mg/kg...
March 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28288814/galanin-1-15-enhancement-of-the-behavioral-effects-of-fluoxetine-in-the-forced-swimming-test-gives-a-new-therapeutic-strategy-against-depression
#10
Antonio Flores-Burgess, Carmelo Millón, Belen Gago, Manuel Narváez, Dasiel O Borroto-Escuela, Guadalupe Mengod, José Angel Narváez, Kjell Fuxe, Luis Santín, Zaida Díaz-Cabiale
The pharmacological treatment of major depression is mainly based on drugs elevating serotonergic (5-HT) activity. Specifically, selective 5-HT reuptake inhibitors, including Fluoxetine (FLX), are the most commonly used for treatment of major depression. However, the understanding of the mechanism of action of FLX beyond its effect of elevating 5-HT is limited. The interaction between serotoninergic system and neuropeptides signalling could be a key aspect. We examined the ability of the neuropeptide Galanin(1-15) [GAL(1-15)] to modulate the behavioral effects of FLX in the forced swimming test (FST) and studied feasible molecular mechanisms...
March 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28286213/carbonic-anhydrase-activation-enhances-object-recognition-memory-in-mice-through-phosphorylation-of-the-extracellular-signal-regulated-kinase-in-the-cortex-and-the-hippocampus
#11
Lucas Canto de Souza, Gustavo Provensi, Daniela Vullo, Fabrizio Carta, Andrea Scozzafava, Alessia Costa, Scheila Daiane Schmidt, Maria Beatrice Passani, Claudiu T Supuran, Patrizio Blandina
Rats injected with by d-phenylalanine, a carbonic anhydrase (CA) activator, enhanced spatial learning, whereas rats given acetazolamide, a CA inhibitor, exhibited impairments of fear memory consolidation. However, the related mechanisms are unclear. We investigated if CAs are involved in a non-spatial recognition memory task assessed using the object recognition test (ORT). Systemic administration of acetazolamide to male CD1 mice caused amnesia in the ORT and reduced CA activity in brain homogenates, while treatment with d-phenylalanine enhanced memory and increased CA activity...
March 9, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28284823/activation-of-the-nmda-receptor-neuronal-nitric-oxide-synthase-pathway-within-the-ventral-bed-nucleus-of-the-stria-terminalis-mediates-the-negative-affective-component-of-pain
#12
Satoshi Deyama, Yaya Sugano, Sakura Mori, Taiju Amano, Mitsuhiro Yoshioka, Katsuyuki Kaneda, Masabumi Minami
Pain consists of sensory and affective components. Although the neuronal mechanisms underlying the sensory component of pain have been studied extensively, those underlying its affective component are only beginning to be elucidated. Previously, we showed the pivotal role of the ventral part of the bed nucleus of the stria terminalis (vBNST) in the negative affective component of pain. Here, we examined the role of glutamate-nitric oxide (NO) signaling in the affective component of pain in rats using a conditioned place aversion (CPA) test...
March 9, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28283392/addictions-neuroclinical-assessment-a-reverse-translational-approach
#13
REVIEW
Laura E Kwako, Reza Momenan, Erica N Grodin, Raye Z Litten, David Goldman
Incentive salience, negative emotionality, and executive function are functional domains that are etiologic in the initiation and progression of addictive disorders, having been implicated in humans with addictive disorders and in animal models of addictions. Measures of these three neuroscience-based functional domains can capture much of the effects of inheritance and early exposures that lead to trait vulnerability shared across different addictive disorders. For specific addictive disorders, these measures can be supplemented by agent specific measures such as those that access pharmacodynamic and pharmacokinetic variation attributable to agent-specific gatekeeper molecules including receptors and drug-metabolizing enzymes...
March 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28283391/residues-w320-and-y328-within-the-binding-site-of-the-%C3%AE-opioid-receptor-influence-opiate-ligand-bias
#14
J Daniel Hothersall, Rubben Torella, Sian Humphreys, Monique Hooley, Alastair Brown, Gordon McMurray, Sarah A Nickolls
The development of G protein-biased agonists for the μ-opioid receptor (MOR) offers a clear drug discovery rationale for improved analgesia and reduced side-effects of opiate pharmacotherapy. However, our understanding of the molecular mechanisms governing ligand bias is limited, which hinders our ability to rationally design biased compounds. We have investigated the role of MOR binding site residues W320 and Y328 in controlling bias, by receptor mutagenesis. The pharmacology of a panel of ligands in a cAMP and a β-arrestin2 assay were compared between the wildtype and mutated receptors, with bias factors calculated by operational analysis using ΔΔlog(τ/KA) values...
March 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28279662/in%C3%A2-vivo-interactions-between-%C3%AE-7-nicotinic-acetylcholine-receptor-and-nuclear-peroxisome-proliferator-activated-receptor-%C3%AE-implication-for-nicotine-dependence
#15
Asti Jackson, Deniz Bagdas, Pretal P Muldoon, Aron H Lichtman, F Ivy Carroll, Mark Greenwald, Michael F Miles, M Imad Damaj
Chronic tobacco use dramatically increases health burdens and financial costs. Limitations of current smoking cessation therapies indicate the need for improved molecular targets. The main addictive component of tobacco, nicotine, exerts its dependency effects via nicotinic acetylcholine receptors (nAChRs). Activation of the homomeric α7 nAChR reduces nicotine's rewarding properties in conditioned place preference (CPP) test and i.v. self-administration models, but the mechanism underlying these effects is unknown...
March 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28274821/the-galanin-3-receptor-antagonist-snap-37889-suppresses-alcohol-drinking-and-morphine-self-administration-in-mice
#16
Karlene J Scheller, Spencer J Williams, Andrew J Lawrence, Elvan Djouma
The neuropeptide, galanin, is widely expressed in the central and peripheral nervous systems and is involved in a range of different functions including nociception, neurogenesis, hormone release, reproduction, cognitive function and appetite. Given the overlap between galanin expression and reward circuitry in the brain, galanin has been targeted for alcohol use disorder (AUD) and opioid dependency. Furthermore, the galanin-3 receptor (GAL3) specifically regulates emotional states and plays a role in motivation, reward and drug-seeking behaviour...
March 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28274820/histamine-induces-kcnq-channel-dependent-gamma-oscillations-in-rat-hippocampus-via-activation-of-the-h1-receptor
#17
Richard Andersson, Dagmar Galter, Daniela Papadia, André Fisahn
Histamine is an aminergic neurotransmitter, which regulates wakefulness, arousal and attention in the central nervous system. Histamine receptors have been the target of efforts to develop pro-cognitive drugs to treat disorders such as Alzheimer's disease and schizophrenia. Cognitive functions including attention are closely associated with gamma oscillations, a rhythmical electrical activity pattern in the 30-80 Hz range, which depends on the synchronized activity of excitatory pyramidal cells and inhibitory fast-spiking interneurons...
March 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28267583/identification-of-the-first-biased-nps-receptor-agonist-that-retains-anxiolytic-and-memory-promoting-effects-with-reduced-levels-of-locomotor-stimulation
#18
Stewart D Clark, Terrence P Kenakin, Steven Gertz, Carla Hassler, Elaine A Gay, Tiffany L Langston, Rainer K Reinscheid, Scott P Runyon
The neuropeptide S system has been implicated in a number of centrally mediated behaviors including memory consolidation, anxiolysis, and increased locomotor activity. Characterization of these behaviors has been primarily accomplished using the endogenous 20AA peptide (NPS) that demonstrates relatively equal potency for the calcium mobilization and cAMP second messenger pathways at human and rodent NPS receptors. This study is the first to demonstrate that truncations of the NPS peptide provides small fragments that retain significant potency only at one of two single polymorphism variants known to alter NPSR function (NPSR-107I), yet demonstrate a strong level of bias for the calcium mobilization pathway over the cAMP pathway...
March 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28267582/melanocortin-4-receptor-ligands-modulate-energy-homeostasis-through-urocortin-1-neurons-of-the-centrally-projecting-edinger-westphal-nucleus
#19
Nóra Füredi, Ákos Nagy, Alexandra Mikó, Gergely Berta, Tamás Kozicz, Erika Pétervári, Márta Balaskó, Balázs Gaszner
The role of the urocortin 1 (Ucn1) expressing centrally projecting Edinger-Westphal (EWcp) nucleus in energy homeostasis and stress adaptation response has previously been investigated. Morphological and functional studies have proven that orexigenic and anorexigenic peptidergic afferents and receptors for endocrine messengers involved in the energy homeostasis are found in the EWcp. The central role of the hypothalamic melanocortin system in energy homeostasis is well known, however, no data have been published so far on possible crosstalk between melanocortins and EWcp-Ucn1...
March 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28259598/tropisetron-sensitizes-%C3%AE-7-containing-nicotinic-receptors-to-low-levels-of-acetylcholine-in%C3%A2-vitro-and-improves-memory-related-task-performance-in-young-and-aged-animals
#20
Patrick M Callahan, Daniel Bertrand, Sonia Bertrand, Marc R Plagenhoef, Alvin V Terry
Tropisetron, a 5-HT3 receptor antagonist commonly prescribed for chemotherapy-induced nausea and vomiting also exhibits high affinity, partial agonist activity at α7 nicotinic acetylcholine receptors (α7 nAChRs). α7 nAChRs are considered viable therapeutic targets for neuropsychiatric disorders such as Alzheimer's disease (AD). Here we further explored the nAChR pharmacology of tropisetron to include the homomeric α7 nAChR and recently characterized heteromeric α7β2 nAChR (1:10 ratio) and we evaluated its cognitive effects in young and aged animals...
March 1, 2017: Neuropharmacology
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