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Drug Development Research

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https://www.readbyqxmd.com/read/28195646/ns1209-spd-502-a-novel-selective-ampa-antagonist-for-stroke-neuropathic-pain-or-epilepsy-drug-development-lessons-learned
#1
Jan M Keppel Hesselink
Preclinical Research The selective AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor antagonist, NS1209 (also known as SPD 502) has been explored in several research and development campaigns since its selection as a lead drug candidate in the early 1990s by the Danish biotechnology company, NeuroSearch. The compound was successively tested in animal models of stroke, neuropathic pain and epilepsy. The preclinical data to support development for the treatment of stroke were incomplete, as the compound was administered after the stroke episode, and did not protect subcortical areas of the brain...
February 13, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28176369/morin-inhibits-proliferation-migration-and-invasion-of-bladder-cancer-ej-cells-via-modulation-of-signaling-pathways-cell-cycle-regulators-and-transcription-factor-mediated-mmp-9-expression
#2
Seung-Shick Shin, Se Yeon Won, Dae-Hwa Noh, Byungdoo Hwang, Wun-Jae Kim, Sung-Kwon Moon
Preclinical Research Previous studies have shown that morin exerts diverse pharmacological activities. In this study, we investigated the inhibitory activity of morin on bladder cancer EJ cells. Morin significantly inhibited EJ cell proliferation, which was related to the G1-phase cell cycle arrest together with the reduced expression of cyclin D1, cyclin E, CDK2, and CDK4 via increased expression of p21WAF1. Morin also increased ERK1/2 phosphorylation and decreased JNK and AKT phosphorylation without altering the p38MAPK phosphorylation levels...
February 8, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28176363/antinociceptive-and-antihyperalgesic-activity-of-a-traditional-maya-herbal-preparation-composed-of-pouteria-campechiana-chrysophyllum-cainito-citrus-limonum-and-annona-muricata
#3
Myrna Déciga-Campos, Rolffy Ortiz-Andrade, Amanda Sanchez-Recillas, José Salvador Flores-Guido, Mario A Ramírez Camacho
Preclinical Research The purpose of this work was to assess the antinociceptive and antihyperalgesic properties of an herbal preparation, composed of four vegetal species: Pouteria campechiana (P. campechiana), Chrysophyllum cainito (C. cainito), Citrus limonum (C. limonum), and Annona muricata (A. muricata), that is commonly used in combination (PCCA) in traditional Mayan medicine for the treatment of diabetes and pain. An ethanolic extract of PCCA was prepared at a ratio of 1:1:1:1 for each plant. The systemic antinociceptive effect of PCCA extract (50-600 mg/kg, p...
February 8, 2017: Drug Development Research
https://www.readbyqxmd.com/read/27987222/the-antinociceptive-effect-of-a-tapentadol-ketorolac-combination-in-a-mouse-model-of-trigeminal-pain-is-mediated-by-opioid-receptors-and-atp-sensitive-k-channels
#4
Israel Barreras-Espinoza, José Alberto Soto-Zambrano, Nicolás Serafín-Higuera, Ramón Zapata-Morales, Ángel Alonso-Castro, Ronell Bologna-Molina, Vinicio Granados-Soto, Mario A Isiordia-Espinoza
Preclinical Research The aim of the present study was to evaluate the antinoceptive interaction between the opioid analgesic, tapentadol, and the NSAID, ketorolac, in the mouse orofacial formalin test. Tapentadol or ketorolac were administered ip 15 min before orofacial formalin injection. The effect of the individual drugs was used to calculate their ED50 values and different proportions (tapentadol-ketorolac in 1:1, 3:1, and 1:3) were assayed in the orofacial test using isobolographic analysis and interaction index to evaluate the interaction between the drugs...
December 16, 2016: Drug Development Research
https://www.readbyqxmd.com/read/27859446/synthesis-of-five-and-six-membered-n-phenylacetamido-substituted-heterocycles-as-formyl-peptide-receptor-agonists
#5
Claudia Vergelli, Igor A Schepetkin, Giovanna Ciciani, Agostino Cilibrizzi, Letizia Crocetti, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Liliya N Kirpotina, Richard D Ye, Mark T Quinn
Preclinical Research Formyl peptide receptors (FPRs) are G-protein-coupled receptors that play an important role in the regulation of inflammatory process and cellular dysfunction. In humans, three different isoforms are expressed (FPR1, FPR2, and FPR3). FPR2 appears to be directly involved in the resolution of inflammation, an active process carried out by specific pro-resolving mediators that modulate specific receptors. Previously, we identified 2-arylacetamido pyridazin-3(2H)-ones as FPR1- or FPR2-selective agonists, as well as a large number of mixed-agonists for the three isoforms...
February 2017: Drug Development Research
https://www.readbyqxmd.com/read/27654302/fucoidan-induces-ros-dependent-apoptosis-in-5637-human-bladder-cancer-cells-by-downregulating-telomerase-activity-via-inactivation-of-the-pi3k-akt-signaling-pathway
#6
Min Ho Han, Dae-Sung Lee, Jin-Woo Jeong, Su-Hyun Hong, Il-Whan Choi, Hee-Jae Cha, Suhkmann Kim, Heui-Soo Kim, Cheol Park, Gi-Young Kim, Sung-Kwon Moon, Wun-Jae Kim, Yung Hyun Choi
Preclinical Research Fucoidan, a sulfated polysaccharide, is a compound found in various species of seaweed that has anti-viral, anti-bacterial, anti-oxidant, anti-inflammatory, and immunomodulatory activities; however, the underlying relationship between apoptosis and anti-telomerase activity has not been investigated. Here, we report that fucoidan-induced apoptosis in 5637 human bladder cancer cells was associated with an increase in the Bax/Bcl-2 ratio, the dissipation of the mitochondrial membrane potential (MMP, Δψm), and cytosolic release of cytochrome c from the mitochondria...
February 2017: Drug Development Research
https://www.readbyqxmd.com/read/27888525/breaking-sad-unleashing-the-breakthrough-potential-of-ketamine-s-rapid-antidepressant-effects
#7
David Feifel
Preclinical Research The surprising results of a small clinical trial on the effects of low dose ketamine, a 65-year old anesthetic drug that is also used off-label for chronic pain and recreationally as a club drug, in eight depressed subjects unleashed the most significant advance in antidepressant drug development in decades. That study and subsequent ones have demonstrated that low dose, infused ketamine is able to induce a remission of depression in patients who have failed conventional medications, within 24 h...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27813127/psychotropic-drug-development-strategies-that-target-neuropsychiatric-etiologies-in-alzheimer-s-and-parkinson-s-diseases
#8
REVIEW
Cornelis J Van der Schyf
Preclinical Research Neuropsychiatric symptoms are currently recognized as a common burden in patients suffering from Alzheimer's disease (AD), Parkinson's disease (PD), and many other neurodegenerative disorders. Earlier theories positing that these symptoms emerge predominantly in patients with late-stage disease have been largely dismissed. It is now generally accepted that many neuropsychiatric symptoms commonly manifest very early in neurodegenerative disease stages, and in many cases are even considered prodromal indicators...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27686062/do-circadian-rhythms-draw-the-patterns-of-sustained-mental-vigor-and-ailment
#9
Ashish Sharma, Rohit Goyal
Preclinical Research Circadian rhythms are fundamental processes in all cells that coordinate a variety of cellular functions related to a specific time of the day. Disruption of circadian rhythms markedly impacts homeostasis. In this Commentary, we present data that disruption of circadian rhythm may lead to the pathogenesis of neurodegenerative states. In this context, we further argue that there is an urgent need of developing new generations of compounds, chronobiotics, to modulate the molecular substrates of circadian timing system...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27633768/nanomedicine-in-psychiatry-new-therapeutic-opportunities-from-research-on-small-rnas
#10
Elena Milanesi, Carlo Maj, Luisella Bocchio-Chiavetto, Elisabetta Maffioletti
Preclinical Research Alterations in small non-coding RNAs have been observed in many human disease states including cancer, cardiovascular, developmental, neurological, and psychiatric disorders. These molecules have recently raised the interest of the scientific community for novel therapeutic approaches. Nanotechnologies, including the development of sophisticated nanoparticles, offer new ways for the delivery of small RNA-based therapies. The nanoparticle delivery method appears attractive, but so far most of the work in this area has been conducted in the context of cancer...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27633648/effects-of-intranasal-oxytocin-on-long-term-memory-in-healthy-humans-a-systematic-review
#11
Michela Brambilla, Rosa Manenti, Giovanni de Girolamo, Mauro Adenzato, Luisella Bocchio-Chiavetto, Maria Cotelli
Preclinical Research The neuropeptide oxytocin (Oxt) is implicated in complex emotional and social behaviors and appears to play an important role in learning and memory. Animal studies have shown that the effects of exogenous Oxt on memory vary according to the timing of administration, context, gender, and dose and may improve the memory of social, but not nonsocial stimuli. Oxt is intimately involved in a broad array of neuropsychiatric functions and may therefore be a pharmacological target for several psychiatric disorders...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27633258/new-horizons-in-pediatric-psychopharmacology
#12
Sarah Khan, Vijaylaxmi Rathore, Shahida Khan
Preclinical Research Recent advances in pediatric psychopharmacology have been rather uneven. Increased use of psychotropic drugs among the pediatric population has raised concerns regarding their inappropriate use and safety. While clinical trials have been conducted on various pediatric psychopharmacological drugs, there has been an insignificant amount of importance to innovation in holistic treatment. A rational approach toward elucidating the various challenges would be contingent on the convergence of the development of novel efficacious psychotropic drugs with concrete conceptual frameworks and guidelines fostering enhanced outcomes...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27594319/the-molecular-basis-of-insomnia-implication-for-therapeutic-approaches
#13
Zi-Jun Wang, Jian-Feng Liu
Preclinical Research Insomnia is one of the most common sleep disorders that is characterized by difficulty in sleep initiation, sleep maintenance, and/or poor sleep quality. Treatment for insomnia includes both pharmacological and non-pharmacological interventions. Recently, the development of pharmacological treatment for insomnia has been prompted by the understanding of the molecular neurobiology of sleep-wake regulation. For pharmacological treatment, benzodiazepines that target GABAergic system are the most widely used hypnotics...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27569987/benefits-of-cognitive-treatments-administered-to-patients-affected-by-mild-cognitive-impairment-mild-neurocognitive-disorder
#14
Marco Cavallo, Arianna Signorino, Maria Luisa Perucchini
Preclinical Research Mild Cognitive Impairment (MCI) now termed Mild Neurocognitive Disorder (MCD) in DSM-5, is widely used to define the disorder in individuals who have subjective cognitive deficits, objective memory impairments, or other cognitive deficits, without impairments in daily activities. Cognitive enhancers such as the acetylcholinesterase inhibitors, commonly used with some benefit in overt dementia, have recently started to be used in MCI/MCD. Treatment of disorders associated with cognitive dysfunction represents an expanding area of neurological rehabilitation and continues to be of paramount importance from political, social and ethical perspectives...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27539712/perspectives-in-designing-multifunctional-molecules-in-antipsychotic-drug-discovery
#15
REVIEW
Andrea Milelli, Eleonora Turrini, Elena Catanzaro, Francesca Maffei, Carmela Fimognari
Preclinical Research A novel and promising approach to overcome the limits of single-target therapy is represented by the multitarget approach. This strategy aims to simultaneously modulate several targets involved in the pathophysiology of a multifactorial disease, with the potential to enhance therapeutic effectiveness and improve drug safety. Although there has been a marked growth in the design of multitarget drugs (MTDs) in the last years in the context of anti-Alzheimer and anti-cancer drug discovery, a parallel expansion was not observed in antipsychotic drugs, even that for psychiatric disorders there is a cogent medical need for new treatments...
December 2016: Drug Development Research
https://www.readbyqxmd.com/read/27775155/recent-developments-of-hydrazide-hydrazone-derivatives-and-their-analogs-as-anticonvulsant-agents-in-animal-models
#16
Violina Angelova, Valentin Karabeliov, Pavlina A Andreeva-Gateva, Jana Tchekalarova
Preclinical Research Epilepsy is a chronic devastating neurological disorder characterized by synchronous interictal discharges. Treatment with antiepileptic drugs (AEDs) can alleviate spontaneous seizure activity without preventing the progression and development of epileptogenesis. Current design and development of new AEDs and strategies for the prevention of epilepsy is focused mainly on attenuating uncontrolled seizures, severe side effects and toxicity in chronic drug therapy. It has thus become necessary to discover new chemical pharmacophores with a broad spectrum of activity and less neurotoxicity...
November 2016: Drug Development Research
https://www.readbyqxmd.com/read/27654112/utilization-of-diurnal-rodents-in-the-research-of-depression
#17
Carmel Bilu, Haim Einat, Noga Kronfeld-Schor
Preclinical Research Most neuropsychiatric research, including that related to the circadian system, is performed using nocturnal animals, mainly laboratory mice and rats. Mood disorders are known to be associated with circadian rhythm abnormalities, but the mechanisms by which circadian rhythm disruptions interact with depression remain unclear. As the circadian system of diurnal and nocturnal mammals differs, we previously suggested that the utilization of diurnal animal models may be advantageous for understanding these relations...
November 2016: Drug Development Research
https://www.readbyqxmd.com/read/27633500/lithium-pharmacogenetics-where-do-we-stand
#18
REVIEW
Claudia Pisanu, Carla Melis, Alessio Squassina
Preclinical Research Bipolar disorder (BPD) is a chronic and disabling psychiatric disorder with a prevalence of 0.8-1.2% in the general population. Although lithium is considered the first-line treatment, a large percentage of patients do not respond sufficiently. Moreover, lithium can induce severe side effects and has poor tolerance and a narrow therapeutic index. The genetics of lithium response has been largely investigated, but findings have so far failed to identify reliable biomarkers to predict clinical response...
November 2016: Drug Development Research
https://www.readbyqxmd.com/read/27633376/improving-current-treatments-for-schizophrenia
#19
Nadja P Maric, Milica J Jovicic, Marina Mihaljevic, Cedo Miljevic
Preclinical Research After the identification of the schizophrenia as an illness over a century ago, treatment of affected individuals included unspecific, mostly very robust methods including deep insulin coma and lobectomy/leucotomy. The first relatively specific treatment of schizophrenia started about 60 years ago with the antipsychotic chlorpromazine. All currently approved antipsychotic drugs block dopamine receptors, indicating that manipulation of dopaminergic function is fundamental to a therapeutic response in psychosis...
November 2016: Drug Development Research
https://www.readbyqxmd.com/read/27594595/s-adenosyl-methionine-in-the-therapy-of-depression-and-other-psychiatric-disorders
#20
Nataša Karas Kuželički
Preclinical Research S-adenosyl methionine (SAM) is a major methyl donor and as such exerts its influence on CNS function through methylation reactions, such as methylation of several catecholamine moiety-containing neurotransmitters, epigenetic changes through methylation of DNA, RNA, RNA-binding proteins and histones, and phospholipid methylation. Based on available evidence, SAM is currently recommended as a next-step (second-line) treatment option following inadequate treatment response to a first-line antidepressant...
November 2016: Drug Development Research
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