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https://www.readbyqxmd.com/read/29677541/tert-butyl-4-1-phenyl-1h-pyrazol-4-yl-methyl-piperazine-1-carboxylate-lqfm104-new-piperazine-derivative-with-antianxiety-and-antidepressant-like-effects-putative-role-of-serotonergic-system
#1
Dayane Moreira da Silva, Germán Sanz, Boniek Gontijo Vaz, Flávio Silva de Carvalho, Luciano Morais Lião, Danillo Ramos de Oliveira, Lorrane Kelle da Silva Moreira, Carina Sofia Cardoso, Adriane Ferreira de Brito, Daiany Priscilla Bueno da Silva, Fabio Fagundes da Rocha, Ianca Gontijo Cavalcante Santana, Pablinny Moreira Galdino, Elson Alves Costa, Ricardo Menegatti
The piperazine derivatives correspond to an extensive chemical class of compounds with numerous neuropharmacological activities, including antidepressant (e.g., nefazodone, trazodone) and anxiolytic (e.g., buspirone) properties. Therefore, aiming to identify a new antidepressant and antianxiety lead-compound, our group designed, synthesized, and investigated the effects of a new piperazine compound, namely, LQFM104, on the behavior of mice. Male albino Swiss mice were treated with LQFM104 prior to predictive behavioral tests as open field (OFT), elevated plus maze (EPM), forced swimming (FST), and tail suspension tests (TST)...
April 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29676327/fluvoxamine-induced-intracranial-hypertension-in-a-10-year-old-boy
#2
Hemalini Samant, Preetam Samant
Drug-induced intracranial hypertension is a well-established entity. We report a rare case of intracranial hypertension with papilledema in a 10-year-old boy following use of fluvoxamine, a selective serotonin reuptake inhibitor. On discontinuing the drug, the papilledema resolved over 4 months without any residual visual anomalies. To the best of our knowledge, this is the first report of fluvoxamine-induced intracranial hypertension with papilledema.
May 2018: Indian Journal of Ophthalmology
https://www.readbyqxmd.com/read/29675596/post-finasteride-syndrome-and-post-ssri-sexual-dysfunction-two-sides-of-the-same-coin
#3
REVIEW
Silvia Giatti, Silvia Diviccaro, Giancarlo Panzica, Roberto Cosimo Melcangi
Sexual dysfunction is a clinical condition due to different causes including the iatrogenic origin. For instance, it is well known that sexual dysfunction may occur in patients treated with antidepressants like selective serotonin reuptake inhibitors (SSRI). A similar side effect has been also reported during treatment with finasteride, an inhibitor of the enzyme 5alpha-reductase, for androgenetic alopecia. Interestingly, sexual dysfunction persists in both cases after drug discontinuation. These conditions have been named post-SSRI sexual dysfunction (PSSD) and post-finasteride syndrome (PFS)...
April 19, 2018: Endocrine
https://www.readbyqxmd.com/read/29674967/no-acute-effects-of-cannabidiol-on-the-sleep-wake-cycle-of-healthy-subjects-a-randomized-double-blind-placebo-controlled-crossover-study
#4
Ila M P Linares, Francisco S Guimaraes, Alan Eckeli, Ana C S Crippa, Antonio W Zuardi, Jose D S Souza, Jaime E Hallak, José A S Crippa
Cannabidiol (CBD) is a component of Cannabis sativa that has a broad spectrum of potential therapeutic effects in neuropsychiatric and other disorders. However, few studies have investigated the possible interference of CBD on the sleep-wake cycle. The aim of the present study was to evaluate the effect of a clinically anxiolytic dose of CBD on the sleep-wake cycle of healthy subjects in a crossover, double-blind design. Twenty-seven healthy volunteers that fulfilled the eligibility criteria were selected and allocated to receive either CBD (300 mg) or placebo in the first night in a double-blind randomized design (one volunteer withdrew from the study)...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29674777/-la-diagnostic-clinical-interview-for-drug-withdrawal-1-did-w1-new-symptoms-of-selective-serotonin-reuptake-inhibitors-ssri-or-serotonin-norepinephrine-reuptake-inhibitors-snri-affidabilit%C3%A3-fra-valutatori
#5
Fiammetta Cosci, Guy Chouinard, Virginie-Anne Chouinard, Giovanni Andrea Fava
RIASSUNTO. Scopo. Dopo la riduzione della dose o la sospensione di Selective Serotonin Reuptake Inhibitors (SSRI) o di Serotonin Norepinephrine Reuptake Inhibitors (SNRI) si possono verificare molti fenomeni clinici. Nel 2015, è stata delineata una nuova classificazione delle sindromi d'astinenza da SSRI/SNRI (cioè, nuovi sintomi, rimbalzo, disturbi persistenti post-astinenza) sulla base della letteratura e delle osservazioni cliniche. Un'intervista clinica semistrutturata, la Diagnostic clinical Interview for Drug Withdrawal 1 - New Symptoms of SSRI and SNRI (DID-W1), è stata sviluppata allo scopo di identificare e differenziare queste sindromi...
March 2018: Rivista di Psichiatria
https://www.readbyqxmd.com/read/29674241/protective-effect-of-betulinic-acid-against-intracerebroventricular-streptozotocin-induced-cognitive-impairment-and-neuronal-damage-in-rats-possible-neurotransmitters-and-neuroinflammatory-mechanism
#6
Madhu Kaundal, Rahul Deshmukh, Mohd Akhtar
BACKGROUND: The purpose of the study was to explore the therapeutic potential of Betulinic acid (BA) in streptozotocin (STZ) induced memory damage in experimental rats. METHODS: STZ (3 mg/kg bilaterally) as intracerebroventrical (icv) route was administered on day 1 and 3 in rats. Donepezil (5 mg/kg/day po), used as standard, and BA (5, 10 and 15 mg/kg/day po) were administered after 1 h of 1st STZ infusion up to 21 days. Object recognition task (ORT) for non-spatial, Morris water maze (MWM) for spatial and locomotor activity were performed to evaluate behavioral changes in rats...
December 6, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29673739/association-of-serotonin-and-gaba-pathway-gene-polymorphisms-with-alcohol-dependence-a-preliminary-study
#7
Shweta Sahni, Mayanka Tickoo, Ranjan Gupta, Meera Vaswani, Atul Ambekar, Tripti Grover, Arundhati Sharma
BACKGROUND: Alcohol dependence (AD), characterized by profound disruptions in specific circuits of the brain is influenced by both environmental, which play a significant role in developing addiction and genetic factors, which make some individuals more susceptible to disruptions. Various polymorphisms in the neurotransmitter genes are reported to increase the risk of developing dependence. The present study aimed to identify association of serotonin and GABA polymorphisms with AD in Indian subjects...
April 9, 2018: Asian Journal of Psychiatry
https://www.readbyqxmd.com/read/29673128/synthesis-analytical-characterization-and-monoamine-transporter-activity-of-the-new-psychoactive-substance-4-methylphenmetrazine-4-mpm-with-differentiation-from-its-ortho-and-meta-positional-isomers
#8
Gavin McLaughlin, Michael H Baumann, Pierce V Kavanagh, Noreen Morris, John D Power, Geraldine Dowling, Brendan Twamley, John O'Brien, Gary Hessman, Folker Westphal, Donna Walther, Simon D Brandt
The availability of new psychoactive substances on the recreational drug market continues to create challenges for scientists in the forensic, clinical and toxicology fields. Phenmetrazine (3-methyl-2-phenylmorpholine) and an array of its analogs form a class of psychostimulants that are well documented in the patent and scientific literature. The present study reports on two phenmetrazine analogs that have been encountered on the NPS drug market following the introduction of 3-fluorophenmetrazine (3-FPM), namely 4-methylphenmetrazine (4-MPM) and 3-methylphenmetrazine (3-MPM)...
April 19, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29671235/evaluation-of-neurotransmitter-alterations-in-four-distinct-brain-regions-after-rapid-eye-movement-sleep-deprivation-remsd-induced-mania-like-behaviour-in-swiss-albino-mice
#9
Saiful Alom Siddique, Thangavel Tamilselvan, Manikkannan Vishnupriya, Elumalai Balamurugan
A number of neurotransmitter systems have been implicated in contributing to the pathology of mood disorders, including those of dopamine (DA), serotonin (5-HT), norepinephrine (NE) and γ-aminobutyric acid (GABA). Rapid eye movement sleep deprivation (REMSD) alters most of the neurotransmitters, which may have adverse behavioural changes and other health consequences like mania and other psychiatric disorders. The exact role of REMSD altered neurotransmitter levels and the manner in which emerging consequences lead to mania-like behaviour is poorly understood...
April 18, 2018: Neurochemical Research
https://www.readbyqxmd.com/read/29668991/the-onset-and-progression-of-chronic-colitis-parallels-increased-mucosal-serotonin-release-via-enterochromaffin-cell-hyperplasia-and-downregulation-of-the-serotonin-reuptake-transporter
#10
Rhian Stavely, Sarah Fraser, Shilpa Sharma, Ahmed A Rahman, Vanesa Stojanovska, Samy Sakkal, Vasso Apostolopoulos, Paul Bertrand, Kulmira Nurgali
Background: Serotonin (5-hydroxytryptamine, 5-HT) has been linked with several inflammation-associated intestinal diseases, including ulcerative colitis (UC). The largest pool of 5-HT in the body is in enterochromaffin (EC) cells located throughout the intestinal tract. EC cells are mechanosensitive and detect noxious stimuli, inducing secretion of 5-HT, which plays an important role in enteric reflexes and immunomodulation. In this study, we evaluated intestinal 5-HT levels in the Winnie mouse model of spontaneous chronic colitis, which closely replicates UC...
April 13, 2018: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/29668649/examining-parental-medication-adherence-as-a-predictor-of-child-medication-adherence-in-pediatric-anxiety-disorders
#11
Greta A Bushnell, M Alan Brookhart, Bradley N Gaynes, Scott N Compton, Stacie B Dusetzina, Til Stürmer
BACKGROUND: Selective serotonin reuptake inhibitors (SSRIs) are the recommended first-line pharmacotherapy for pediatric anxiety disorders but adherence remains difficult to predict. OBJECTIVES: To estimate SSRI adherence in children with anxiety disorders and determine if prior parental medication adherence is predictive of child high SSRI adherence. METHODS: We identified children (3-17 y) initiating SSRI treatment after an anxiety disorder diagnosis in a commercial claims database (2005-2014)...
April 17, 2018: Medical Care
https://www.readbyqxmd.com/read/29667458/sudden-unexpected-death-in-epilepsy-ongoing-challenges-in-finding-mechanisms-and-prevention
#12
Doungporn Ruthirago, Parunyou Julayanont, Amputch Karukote, Mohamed Shehabeldin, Kenneth Nugent
Patients with epilepsy have a significantly higher risk of death than the general population. Sudden unexpected death in epilepsy (SUDEP) is the leading cause of sudden death among patients with epilepsy. Despite on-going research, there are still deficits in our knowledge about the mechanisms, genetic factors, and prevention of SUDEP. Current evidence suggests that cardiac arrhythmias, respiratory dysfunction, and brainstem arousal system dysfunction are the major mechanisms of SUDEP, and animal models support the role of neurotransmitters, especially serotonin and adenosine, in pathophysiology of SUDEP...
April 18, 2018: International Journal of Neuroscience
https://www.readbyqxmd.com/read/29667320/flotillin-1-interacts-with-the-serotonin-transporter-and-modulates-chronic-corticosterone-response
#13
Sonali N Reisinger, Eryan Kong, Barbara Molz, Thomas Humberg, Spyros Sideromenos, Ana Cicvaric, Thomas Steinkellner, Jae-Won Yang, Maureen Cabatic, Francisco J Monje, Harald H Sitte, Benjamin J Nichols, Daniela D Pollak
Aberrant serotonergic neurotransmission in the brain is considered at the core of the pathophysiological mechanisms involved in neuropsychiatric disorders. Gene by environment interactions contribute to the development of depression and involve modulation of the availability and functional activity of the serotonin transporter (SERT). Using behavioral and in vivo electrophysiological approaches together with biochemical, molecular-biological and molecular imaging tools we establish Flotillin-1 (Flot1) as a novel protein interacting with SERT and demonstrate its involvement in the response to chronic corticosterone (CORT) treatment...
April 18, 2018: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29667177/adverse-placental-effects-of-valproic-acid-studies-in-perfused-human-placentas
#14
Miriam Rubinchik-Stern, Miriam Shmuel, Jacob Bar, Michal Kovo, Sara Eyal
OBJECTIVE: In utero exposure to valproic acid (VPA) has been associated with worse pregnancy outcomes compared to all other antiepileptic drugs. We have previously shown that VPA alters the expression of placental transporters for hormones and nutrients in vitro and in pregnant mice. Here, our aim was to characterize the effects of short exposure to VPA on the expression of carriers for compounds essential for fetal development in human placentas ex vivo, under controlled conditions...
April 17, 2018: Epilepsia
https://www.readbyqxmd.com/read/29666456/serotonin-is-an-endogenous-regulator-of-intestinal-cyp1a1-via-ahr
#15
Christopher Manzella, Megha Singhal, Waddah A Alrefai, Seema Saksena, Pradeep K Dudeja, Ravinder K Gill
Aryl hydrocarbon receptor (AhR) is a nuclear receptor that controls xenobiotic detoxification via induction of cytochrome P450 1A1 (CYP1A1) and regulates immune responses in the intestine. Metabolites of L-tryptophan activate AhR, which confers protection against intestinal inflammation. We tested the hypothesis that serotonin (5-HT) is an endogenous activator of AhR in intestinal epithelial cells. Treatment of Caco-2 monolayers with 5-HT induced CYP1A1 mRNA in a time- and concentration-dependent manner and also stimulated CYP1A1 activity...
April 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29666372/brain-serotonin-synthesis-capacity-in-obsessive-compulsive-disorder-effects-of-cognitive-behavioral-therapy-and-sertraline
#16
Jennifer I Lissemore, Debbie Sookman, Paul Gravel, Alexandre Berney, Amir Barsoum, Mirko Diksic, Thomas E Nordahl, Gilbert Pinard, Igor Sibon, Jean Cottraux, Marco Leyton, Chawki Benkelfat
Cognitive behavioral therapy (CBT) and selective serotonin reuptake inhibitors (SSRIs) are both effective treatments for some patients with obsessive-compulsive disorder (OCD), yet little is known about the neurochemical changes related to these treatment modalities. Here, we used positron emission tomography and the α-[11 C]methyl-L-tryptophan tracer to examine the changes in brain regional serotonin synthesis capacity in OCD patients following treatment with CBT or SSRI treatment. Sixteen medication-free OCD patients were randomly assigned to 12 weeks of either CBT or sertraline treatment...
April 18, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29666360/signaling-pathways-responsible-for-the-rapid-antidepressant-like-effects-of-a-glun2a-preferring-nmda-receptor-antagonist
#17
Marta Gordillo-Salas, Fuencisla Pilar-Cuéllar, Yves P Auberson, Albert Adell
In a previous study we found that the preferring GluN2A receptor antagonist, NVP-AAM077, elicited rapid antidepressant-like effects in the forced swim test that was related to the release of glutamate and serotonin in the medial prefrontal cortex. In the present work we sought to examine the duration of this behavioral effect as well as the molecular readouts involved. Our results showed that NVP-AAM077 reduced the immobility in the forced swim test 30 min and 24 h after its administration. However, this effect waned 7 days later...
April 18, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29666153/the-ins-and-outs-of-vesicular-monoamine-transporters
#18
REVIEW
Dana Yaffe, Lucy R Forrest, Shimon Schuldiner
The H+ -coupled vesicular monoamine transporter (VMAT) is a transporter essential for life. VMAT mediates packaging of the monoamines serotonin, dopamine, norepinephrine, and histamine from the neuronal cytoplasm into presynaptic vesicles, which is a key step in the regulated release of neurotransmitters. However, a detailed understanding of the mechanism of VMAT function has been limited by the lack of availability of high-resolution structural data. In recent years, a series of studies guided by homology models has revealed significant insights into VMAT function, identifying residues that contribute to the binding site and to specific steps in the transport cycle...
April 17, 2018: Journal of General Physiology
https://www.readbyqxmd.com/read/29665098/patterns-of-antidepressant-use-during-pregnancy-a-nationwide-population-based-cohort-study
#19
Anne Bénard-Laribière, Elodie Pambrun, Anne-Laure Sutter-Dallay, Sophie Gautier, Caroline Hurault-Delarue, Christine Damase-Michel, Isabelle Lacroix, Bernard Bégaud, Antoine Pariente
AIMS: We explored the patterns of antidepressant use during pregnancy. METHODS: A cohort of women who started a pregnancy in 2014 was identified using data from the French reimbursement healthcare system (covering approximately 99% of the population). Antidepressant uses (initiated before or during pregnancy) were assessed. Explored changes in antidepressant treatment were: associations, switches, discontinuation, and resumption of antidepressants during pregnancy...
April 17, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29665066/serotonin-beta-amyloid-and-cognition-in-parkinson-disease
#20
Vikas Kotagal, Cathie Spino, Nicolaas I Bohnen, Robert A Koeppe, Roger L Albin
OBJECTIVE: Serotoninergic neurotransmission may modulate beta-amyloid peptide (Aβ) metabolism through up-regulation of alpha-secretase. Early Parkinson disease (PD) shows variable serotoninergic denervation, which may impact Aβ deposition. METHODS: We conducted three analyses to explore associations between serotoninergic neurotransmission and cerebral Aβ burden in PD. The first was a cross-sectional imaging study of PD subjects (n=23) using the serotoninergic transporter positron emission tomography (PET) ligand [11 C]DASB and amyloid PET Pittsburgh compound B ([11 C]PiB)...
April 17, 2018: Annals of Neurology
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