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https://www.readbyqxmd.com/read/29767995/structure-activity-relationships-and-therapeutic-potentials-of-5-ht7-receptor-ligands-an-update
#1
Maria N Modica, Enza Lacivita, Sebastiano Intagliata, Loredana Salerno, Giuseppe Romeo, Valeria Pittala, Marcello Leopoldo
Serotonin 5-HT7 receptor (5-HT7R) has been the subject of intense research efforts because of its presence in brain areas such as hippocampus, hypothalamus, and cortex. Preclinical data link the 5-HT7R to a variety of central nervous system processes such as regulation of circadian rhythms, mood, cognitions, pain processing, and mechanisms of addiction. 5-HT7R blockade has antidepressant effects and may ameliorate cognitive deficits associated with schizophrenia. 5-HT7R has been recently shown to modulate neuronal morphology, excitability, and plasticity, thus contributing to shape brain networks during development and to remodel neuronal wiring in the mature brain...
May 16, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29765245/the-epidemiology-of-outpatient-pain-treatment-in-pediatrics
#2
Stacy Baldridge, Laura Wallace, Aditi Kadakia
Background: There is limited real-world, population-level data on the prevalence and treatment of pain in children. An understanding of pediatric pain conditions and its management can help inform provider education, treatment guidelines, and design of pediatric pain studies. Therefore, in this study, we aimed to describe the prevalence of conditions associated with acute and chronic pain in pediatric patients and to characterize pediatric pain treatment with nonsteroidal anti-inflammatory drugs, cyclooxygenase-2 (COX-2) inhibitors, opioids (immediate release or extended release), antidepressants, topical analgesics, anticonvulsants, and other therapies based on a large, real-world sample...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29763654/obturator-neuromodulation-with-laparoscopic-placement-of-an-obturator-lead-for-the-treatment-of-intractable-opioid-dependent-chronic-pelvic-pain-due-to-obturator-neuralgia
#3
Richard P Marvel
Chronic pelvic pain(CPP) is a common condition in women that can have a devastating effect on quality of life. Some of the most severe forms of CPP are related to peripheral nerve injuries causing persistent neuropathic pain. This is a case of a young woman with severe opioid dependent chronic pelvic and right groin pain due to obturator neuralgia. She had failed a multitude of treatments including multiple medications, manual physical therapy, nerve blocks, surgical neurolysis and spinal cord stimulation without significant benefit...
May 12, 2018: Journal of Minimally Invasive Gynecology
https://www.readbyqxmd.com/read/29760410/motivational-changes-that-develop-in-a-mouse-model-of-inflammation-induced-depression-are-independent-of-indoleamine-2-3-dioxygenase
#4
Elisabeth G Vichaya, Geoffroy Laumet, Diana L Christian, Aaron J Grossberg, Darlene J Estrada, Cobi J Heijnen, Annemieke Kavelaars, Robert Dantzer
Despite years of research, our understanding of the mechanisms by which inflammation induces depression is still limited. As clinical data points to a strong association between depression and motivational alterations, we sought to (1) characterize the motivational changes that are associated with inflammation in mice, and (2) determine if they depend on inflammation-induced activation of indoleamine 2,3 dioxygenase-1 (IDO1). Lipopolysaccharide (LPS)-treated or spared nerve injured (SNI) wild type (WT) and Ido1 -/- mice underwent behavioral tests of antidepressant activity (e...
April 27, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29752984/antinociceptive-effects-of-the-antidepressant-phenelzine-are-mediated-by-context-dependent-inhibition-of-neuronal-responses-in-the-dorsal-horn
#5
Liam E Potter, Suzanne Doolen, Katherine Mifflin, Gustavo Tenorio, Glen Baker, Bradley K Taylor, Bradley J Kerr
The putative strong anti-nociceptive properties of the antidepressant phenelzine (PLZ) have not been widely explored as a treatment for pain. Antinociceptive effects of PLZ were identified in the formalin model of tonic pain (Mifflin et al. 2016) and in allodynia associated with experimental autoimmune encephalomyelitis, (EAE) a mouse model of multiple sclerosis (Potter et al. 2016). Here, we further clarify the specific types of stimuli and contexts in which PLZ modulates nociceptive sensitivity. Our findings indicate that PLZ selectively inhibits ongoing inflammatory pain while sparing transient reflexive and acute nociception...
May 9, 2018: Neuroscience
https://www.readbyqxmd.com/read/29752818/fluoxetine-uses-in-nociceptive-pain-management-a-promising-adjuvant-to-opioid-analgesics
#6
Mostafa M Hamdy, Mohamed M Elbadr, Ahmed Barakat
Fluoxetine, a commonly prescribed antidepressant, use in nociceptive pain management represent one of the unsettled issues of fluoxetine therapeutics. By reviewing the literature about fluoxetine's possible roles in this setting; those could be solitary antinociceptive effect, enhancement of acute morphine analgesia, blocking morphine tolerance development, and blocking dependence development and associated abstinence syndrome. In this study, we examined those four alleged roles of fluoxetine. Moreover, since effective alleviation of morphine tolerance, dependence, and abstinence syndrome represents one of the most challenging medical needs, we biochemically analyzed fluoxetine effect on these phenomena...
May 12, 2018: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29751080/prenylated-%C3%AE-diketones-two-new-additions-to-the-family-of-biologically-active-hypericum-perforatum-l-hypericaceae-secondary-metabolites
#7
Niko S Radulović, Marija S Genčić, Nikola M Stojanović, Pavle J Randjelović, Nicolas Baldovini, Vanya Kurteva
Two novel β-diketones, 2,6,9-trimethyl-8-decene-3,5-dione (A) and 3,7,10-trimethyl-9-undecene-4,6-dione (B), were identified from the renowned medicinal plant Hypericum perforatum L. The structures of β-diketones A and B were corroborated by syntheses (4 steps starting from methyl acetoacetate, overall yields 30% and 23%, respectively). In solution, these β-diketones predominantly exist as two rapidly interconverting β-keto-enol tautomers. The structures of A and B show some common fragments with the molecules of hyperforin and adhyperforin, respectively, the acknowledged multi-target secondary metabolites from St...
May 8, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29742620/ketamine-differentially-restores-diverse-alterations-of-neuroligins-in-brain-regions-in-a-rat-model-of-neuropathic-pain-induced-depression
#8
Wei Pan, Guang-Fen Zhang, Hui-Hui Li, Mu-Huo Ji, Zhi-Qiang Zhou, Kuan-Yu Li, Jian-Jun Yang
Depression is present in a large proportion of patients suffering from chronic pain, and yet the underlying mechanisms remain to be elucidated. Neuroligins (NLs), as a family of cell-adhesion proteins, are involved in synaptic formation and have been linked to various neuropsychiatric disorders. Here, we studied the alterations in NL1 and NL2 in the medial prefrontal cortex (mPFC), the anterior cingulate cortex (ACC), and the hippocampus in a rat model of neuropathic pain-induced depression, and whether ketamine, a rapid and robust antidepressant, could restore these abnormalities...
May 8, 2018: Neuroreport
https://www.readbyqxmd.com/read/29742109/effect-of-single-dose-imipramine-on-chronic-low-back-and-experimental-pain-a-randomized-controlled-trial
#9
Jürg Schliessbach, Andreas Siegenthaler, Lukas Bütikofer, Andreas Limacher, Peter Juni, Pascal H Vuilleumier, Ulrike Stamer, Lars Arendt-Nielsen, Michele Curatolo
Antidepressants are frequently prescribed as co-analgesics in chronic pain. While their efficacy is well documented for neuropathic pain, the evidence is less clear in musculoskeletal pain conditions. The present study therefore evaluated the effect of the tricyclic antidepressant imipramine on chronic low-back pain in a randomized, double-blinded placebo-controlled design. To explore the mechanisms of action and the influence of drug metabolism, multimodal quantitative sensory tests (QST) and genotyping for cytochrome P450 2D6 (CYP2D6) were additionally performed...
2018: PloS One
https://www.readbyqxmd.com/read/29732584/giving-priority-to-preclinical-pain-measures-resistant-to-existing-drugs-for-developing-innovative-analgesics
#10
Yukinori Nagakura
Preclinical Research & Development Chronic pain is a major health and socioeconomic burden because of its high prevalence, negative influence on patients' physical and/or emotional conditions, and huge costs to society. The responses of chronic pain patients to analgesic therapies vary substantially from individual to individual, and no more than a minority of chronic pain patients with various etiologies such as neuropathy and inflammation are, in fact, successfully relieved by existing drugs including opioid analgesics, nonopioid analgesics, antiepileptics, and antidepressants...
May 6, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29730170/the-antidepressant-effects-of-rosiglitazone-on-rats-with-depression-induced-by-neuropathic-pain
#11
Jian Zong, Xingzhi Liao, Bingxu Ren, Zhiping Wang
A growing number of studies reported that rosiglitazone (a PPARgamma agonist) could ameliorate the painful state and prevent stress-induced depression. However, whether rosiglitazone can prevent pain-induced depression is unclear. This study aimed to explore the antidepressant effects of rosiglitazone in L5 spinal nerve transection (SNT) induced neuropathic pain rats. In addition, AMPK inhibitor (Compound C) and autophagic antagonist (3-methyladenine, 3-MA) were applied to investigate the underlying therapeutic mechanisms...
May 3, 2018: Life Sciences
https://www.readbyqxmd.com/read/29730027/synthesis-and-activity-of-di-or-trisubstituted-n-phenoxyalkyl-or-n-2-2-phenoxy-ethoxy-ethyl-piperazine-derivatives-on-the-central-nervous-system
#12
Katarzyna Pańczyk, Karolina Pytka, Magdalena Jakubczyk, Anna Rapacz, Kinga Sałat, Anna Furgała, Agata Siwek, Monika Głuch-Lutwin, Anna Gryboś, Karolina Słoczyńska, Elżbieta Pękala, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Dorota Żelaszczyk, Henryk Marona, Anna M Waszkielewicz
Aim of the study was evaluation of anxiolytic, antidepressant, anticonvulsant and analgesic activity in a series of a consistent group of compounds. A series of eleven new N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives has been obtained. Their affinity towards 5-HT1A , 5-HT2A , 5-HT6 , 5-HT7 , D2 and α1 receptors has been assessed, and then functional assays were performed. The compounds were evaluated in mice, i.p. for their antidepressant-like (forced swim test), locomotor, anxiolytic-like (four-plate test) activities as well as - at higher doses - for anticonvulsant potential (MES) and neurotoxicity (rotarod)...
April 25, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29726344/effectiveness-of-theta-burst-versus-high-frequency-repetitive-transcranial-magnetic-stimulation-in-patients-with-depression-three-d-a-randomised-non-inferiority-trial
#13
Daniel M Blumberger, Fidel Vila-Rodriguez, Kevin E Thorpe, Kfir Feffer, Yoshihiro Noda, Peter Giacobbe, Yuliya Knyahnytska, Sidney H Kennedy, Raymond W Lam, Zafiris J Daskalakis, Jonathan Downar
BACKGROUND: Treatment-resistant major depressive disorder is common; repetitive transcranial magnetic stimulation (rTMS) by use of high-frequency (10 Hz) left-side dorsolateral prefrontal cortex stimulation is an evidence-based treatment for this disorder. Intermittent theta burst stimulation (iTBS) is a newer form of rTMS that can be delivered in 3 min, versus 37·5 min for a standard 10 Hz treatment session. We aimed to establish the clinical effectiveness, safety, and tolerability of iTBS compared with standard 10 Hz rTMS in adults with treatment-resistant depression...
April 28, 2018: Lancet
https://www.readbyqxmd.com/read/29724663/effect-of-problem-solving-therapy-versus-supportive-management-in-older-adults-with-low-back-pain-and-depression-while-on-antidepressant-pharmacotherapy
#14
Jordan F Karp, Xiaotian Gao, Abdus S Wahed, Jennifer Q Morse, Bruce L Rollman, Debra K Weiner, Charles F Reynolds
OBJECTIVE: Testing stepped-care approaches that address both depression and low back pain are needed to optimize outcomes in older adults. METHODS: This university-based late-life depression research center assessed 227 adults aged ≥ 60 years with chronic low back pain and depression. In Phase 1 participants received 6 weeks of low-dose venlafaxine (≤150 mg/day). Nonresponders were randomized to 10 weeks of high-dose venlafaxine (up to 300 mg/day) plus problem-solving therapy (PST) or high-dose venlafaxine with supportive management...
March 30, 2018: American Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29715490/an-antidepressant-related-pharmacological-signature-for-positive-allosteric-modulators-of-%C3%AE-2-3-containing-gaba-a-receptors
#15
K R Methuku, X Li, R Cerne, S D Gleason, J M Schkeryantz, V V N P B Tiruveedhula, L K Golani, G Li, M M Poe, Md T Rahman, J M Cook, J L Fisher, J M Witkin
Data from transgenic animals and novel pharmacological agents has realigned scientific scrutiny on the therapeutic potential of positive allosteric modulators (PAMs) of α2/3-containing GABAA receptors. Evidence for analgesic, anticonvulsant, and anxiolytic activity of α2/3-selective PAMs has been presented along with the clinical potential for a milder motor-impacting profile compared to non-selective GABAA receptor PAMs. A new series of α2/3-selective PAMs was recently introduced which has anxiolytic and anticonvulsant activity in rodent models...
April 28, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29714124/clinical-application-of-pharmacogenetics-in-pain-management
#16
D Max Smith, Kristin W Weitzel, Larisa H Cavallari, Amanda R Elsey, Siegfried Of Schmidt
There is growing experience translating genomic data into clinical practice, as seen with the Implementing GeNomics In pracTicE (IGNITE) network. A primary example is the influence of CYP2D6 genotype on the beneficial and adverse effects of some opioids. Clinical recommendations exist to guide drug therapy based on CYP2D6 genotype for codeine, tramadol, oxycodone and hydrocodone, although the level of supporting evidence differs by drug. Limited evidence also supports the use of genetic data to guide other medications in chronic pain therapy, including tricyclic antidepressants and celecoxib...
March 2018: Personalized Medicine
https://www.readbyqxmd.com/read/29708207/ssri-associated-bruxism-a-systematic-review-of-published-case-reports
#17
REVIEW
Andrew R Garrett, Jason S Hawley
Purpose of review: Antidepressant-associated movement disorders are a well-described phenomenon. However, antidepressant-associated bruxism, jaw pain, or jaw spasm, while reported in dental literature, is less commonly recognized among neurologists. We summarize the clinical features and treatment of antidepressant-associated bruxism and associated jaw pain through a systematic review of case reports. Recent findings: Antidepressant-associated bruxism may occur in pediatric and adult patients, most commonly among female patients...
April 2018: Neurology. Clinical Practice
https://www.readbyqxmd.com/read/29686645/phantom-limb-pain-in-pediatric-oncology
#18
REVIEW
Patrick DeMoss, Logan H Ramsey, Cynthia Windham Karlson
Phantom limb pain (PLP) is a prevalent problem for children and adolescents undergoing amputation due to cancer treatment. The symptoms are wide ranging from sharp to tingling. PLP in children typically lasts for a few minutes but can be almost constant and can be highly distressing. This focused review describes the characteristics, epidemiology, mechanisms, and evidence-based treatment of PLP in pediatric populations, focusing on pediatric cancer. In pediatric oncology, the administration of chemotherapy is a risk factor that potentially sensitizes the nervous system and predisposes pediatric cancer patients to develop PLP after amputation...
2018: Frontiers in Neurology
https://www.readbyqxmd.com/read/29678770/self-reported-pain-in-patients-with-schizophrenia-results-from-the-national-first-step-face-sz-cohort
#19
Guillaume Fond, Laurent Boyer, Meja Andrianarisoa, Ophelia Godin, Ewa Bulzacka, Fabrice Berna, Lore Brunel, Nathalie Coulon, Bruno Aouizerate, Delphine Capdevielle, Isabelle Chereau, Thierry D'amato, Hélène Denizot, Caroline Dubertret, Julien Dubreucq, Catherine Faget, Sylvain Leignier, Jasmina Mallet, David Misdrahi, Romain Rey, Christophe Lancon, Christine Passerieux, Aurélie Schandrin, Mathieu Urbach, Pierre Vidailhet, Marion Leboyer, Franck Schurhoff, Pierre-Michel Llorca, M Andrianarisoa, B Aouizerate, F Berna, O Blanc, L Brunel, E Bulzacka, D Capdevielle, I Chereau-Boudet, G Chesnoy-Servanin, Danion Jm, T D'Amato, A Deloge, C Delorme, H Denizot, J M Dorey, C Dubertret, J Dubreucq, C Faget, C Fluttaz, G Fond, S Fonteneau, F Gabayet, E Giraud-Baro, R M Honciuc, D Lacelle, C Lançon, H Laouamri, M Leboyer, T Le Gloahec, Y Le Strat, Llorca, J Mallet, E Metairie, D Misdrahi, I Offerlin-Meyer, C Passerieux, P Peri, S Pires, C Portalier, R Rey, C Roman, M Sebilleau, A Schandrin, F Schurhoff, A Tessier, Tronche Am, M Urbach, F Vaillant, A Vehier, P Vidailhet, E Vilà, H Yazbek, A Zinetti-Bertschy
INTRODUCTION: Little is known about perception of physical pain in schizophrenia (SZ). Some studies have suggested that patients with SZ may have an increased pain threshold, while others have suggested that patients with SZ may suffer from undetected and untreated high physical pain levels. The objectives of this study were (i) to investigate the prevalence of self-reported physical pain in stabilized SZ subjects, and (ii) to determine whether physical pain was associated with psychiatric characteristics and somatic comorbidities (iii) to determine whether antidepressants and benzodiazepine administration were associated with lower self-reported pain...
April 17, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29678564/prescription-medication-use-among-community-based-us-adults-with-chronic-low-back-pain-a-cross-sectional-population-based-study
#20
Anna Shmagel, Linh Ngo, Kristine Ensrud, Robert Foley
Many classes of medications have been evaluated in chronic low back pain (cLBP), however their utilization in the community remains unclear. We examine patterns of prescription medication use among Americans with cLBP in a nationally representative, community-based sample. The Back Pain Survey was administered to a representative sample of US adults aged 20-69 (N = 5103) during the 2009-2010 cycle of the National Health and Nutrition Examination Survey (NHANES). cLBP was defined as self-reported pain in the area between the lower posterior margin of the ribcage and the horizontal gluteal fold on most days for at least 3 months (N = 700)...
April 17, 2018: Journal of Pain: Official Journal of the American Pain Society
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