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https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#1
Thomas Pokorny, Katrin H Preller, Michael Kometer, Isabel Dziobek, Franz X Vollenweider
Background: Impaired empathic abilities lead to severe negative social consequences and influence the development and treatment of several psychiatric disorders. Furthermore, empathy has been shown to play a crucial role in moral and prosocial behaviour. Although the serotonin (5-HT) system has been implicated in modulating empathy and moral behaviour, the relative contribution of the various 5-HT receptor subtypes is still unknown. Methods: We investigated the acute effect of psilocybin (0...
June 16, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28636828/pharmacokinetic-drug-evaluation-of-extended-release-lorcaserin-for-the-treatment-of-obesity
#2
Kathryn Hurren, Marissa W Dunham
Lorcaserin is a serotonin 2C receptor antagonist that was FDA approved in 2012. Lorcaserin is recently available as an extended-release (ER) formulation for the treatment of obesity as an adjunct to lifestyle modification. Areas covered: The pharmacokinetics, pharmacodynamics, efficacy, and safety of lorcaserin ER will be reviewed. Expert opinion: Lorcaserin ER 20mg daily provides drug exposure bioequivalent to lorcaserin immediate release (IR) 10mg twice daily. Lorcaserin IR is associated with 3.3% and 3.0% placebo-subtracted weight loss in patients without and with diabetes, respectively...
June 21, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28633926/synergic-stimulation-of-serotonin-5-ht1a-receptor-and-%C3%AE-2-adrenoceptors-for-neuropathic-pain-relief-preclinical-effects-of-2-substituted-imidazoline-derivatives
#3
Lorenzo Di Cesare Mannelli, Carla Ghelardini, Laura Micheli, Fabio Del Bello, Mario Giannella, Alessandro Piergentili, Wilma Quaglia
Neuropathic pain affects millions of people causing disability and impairing quality of life. Commonly used analgesics are generally characterized by limited therapeutic outcomes. The serotonin 5-HT1A receptor and the α2 adrenergic receptors are involved in central nociceptive mechanisms with a pivotal role in the inhibitory descending pain pathway. Since their stimulation may modulate the nervous signaling altered by neuropathies, the purpose of the present research is the study of the combined activation of 5-HT1A and α2 receptors by rationally designed imidazoline ligands ((S)-1 and 2-5) in a rat model of neuropathic pain (chronic constriction injury - CCI)...
June 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28633671/preliminary-safety-and-efficacy-profile-of-prucalopride-in-the-treatment-of-systemic-sclerosis-ssc-related-intestinal-involvement-results-from-the-open-label-cross-over-progass-study
#4
Barbara Vigone, Monica Caronni, Adriana Severino, Chiara Bellocchi, Anna Rita Baldassarri, Mirella Fraquelli, Gaia Montanelli, Alessandro Santaniello, Lorenzo Beretta
BACKGROUND: Prokinetics are used to treat enteric dismotility symptoms in systemic sclerosis (SSc) patients, but they often lack adequate efficacy. The most effective prokinetics belonging to the serotonin (5-HT4) receptor agonists class were withdrawn due to cardiac toxicity in relation to modest 5-HT4 receptor affinity. Prucalopride is a high-affinity 5-HT4 receptor agonist with no major cardiac issues, for which the efficacy in SSc has not yet been assessed. METHODS: Forty patients with self-reported mild to moderately severe enteric symptoms were enrolled in a cross-over 2 × 2 study...
June 20, 2017: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/28631100/co-modulation-of-an-allosteric-modulator-of-nicotinic-receptor-cholinesterase-inhibitor-galantamine-and-a-5-ht4-receptor-agonist-rs-67333-effect-on-scopolamine-induced-memory-deficit-in-the-mouse
#5
Thomas Freret, Véronique Lelong-Boulouard, Pierre Lecouflet, Katia Hamidouche, François Dauphin, Michel Boulouard
AIM: It is widely assumed that the upcoming therapeutics for Alzheimer's disease will require to act on more than one target to be effective. We investigated here whether a combination of the nicotinic receptor allosteric modulator/cholinesterase inhibitor galantamine can act synergistically with the type 4 serotonin receptor (5-HT4R) partial agonist, RS-67333, to counterbalance deficits in short- and long-term memory. To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task...
June 19, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28629964/a-novel-heterocyclic-compound-improves-working-memory-in-the-radial-arm-maze-and-modulates-the-dopamine-receptor-d1r-in-frontal-cortex-of-the-sprague-dawley-rat
#6
Ahmed M Hussein, Yogesh D Aher, Predrag Kalaba, Nilima Y Aher, Vladimir Dragačević, Bojana Radoman, Marija Ilic, Johann Leban, Tetyana Beryozkina, Abdel Baset M A Ahmed, Ernst Urban, Thierry Langer, Gert Lubec
A series of compounds have been shown to enhance cognitive function via the dopaminergic system and indeed the search for more active and less toxic compounds is continuing. It was therefore the aim of the study to synthetise and test a novel heterocyclic compound for cognitive enhancement in a paradigm for working memory. Specific and effective dopamine re-uptake inhibition (DAT (IC50=4,1 ± 0,8μM) made us test this compound in a radial arm maze (RAM) in the rat. CE-125 (4-((benzhydrylsulfinyl)methyl)-2-cyclopropylthiazole), was tested for dopamine (DAT), serotonin and norepinephrine re-uptake inhibition by a well-established system...
June 16, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28628885/use-of-antidepressants-and-risk-of-hospitalization-for-acute-myocardial-infarction-a-nationwide-case-crossover-study
#7
Chi-Shin Wu, Hsiao-Ting Wu, Yu-Ting Tsai, Ya-Wen Huang, Hui-Ju Tsai
BACKGROUND: We aimed to investigate the association between antidepressant use and the risk of hospitalization for acute myocardial infarction (AMI). METHODS: A case-crossover study was conducted using a nationwide population-based sample from Taiwan's National Health Insurance Research Database. A total of 18,631 patients with incident AMI were included in this study. The effects of antidepressant use as well as that of various classes (including tricyclic or tetracyclic antidepressants; selective serotonin reuptake inhibitors; or serotonin norepinephrine reuptake inhibitors), doses, and receptor-binding profiles of the antidepressants on AMI were assessed...
June 3, 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28628756/atypical-sympathomimetic-drug-lerimazoline-mediates-contractile-effects-in-rat-aorta-predominantly-by-5-ht2a-receptors
#8
Eldina Rizvić, Goran Janković, Slađana Kostić-Rajačić, Miroslav M Savić
Lerimazoline is a sympathomimetic drug that belongs to the imidazoline class of compounds, and is used as a nasal decongestant. Studies on lerimazoline are rare, and its pharmacological profile is not completely understood. Here, we analyzed the affinity of lerimazoline for dopamine receptor D2, serotonin 5-HT1A and 5-HT2A receptors and α1-adrenoceptor, and investigated lerimazoline contractile effects in isolated rat thoracic aorta. We also determined the effect of several antagonists on the contractile response to lerimazoline, including prazosin (α1-adrenoceptor antagonist), RX 821002 and rauwolscine (α2-adrenoceptor antagonists), JP 1302 (α2C-adrenoceptor antagonist), methiothepin (non-selective 5-HT receptor antagonist), SB 224289 (5-HT1B receptor antagonist), BRL 15572 (5-HT1D receptor antagonist), and ketanserin (5-HT2A receptor antagonist)...
June 19, 2017: Bosnian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28626786/interaction-between-estradiol-and-5-ht1a-receptors-in-the-median-raphe-nucleus-on-acquisition-of-aversive-information-and-association-to-the-context-in-ovariectomized-rats
#9
Telma Gonçalves Carneiro Spera de Andrade, João Victor Dos Santos Silva, Matheus Fitipaldi Batistela, Fernando Frei, Ana Beatriz Sant'Ana
The median raphe nucleus (MRN) is related to stress resistance and defensive responses, a crucial source of serotonergic neurons that project to prosencephalic structures related to stress and anxiety. Estrogen receptors were identified in this mesencephalic structure. It is possible that the estrogen action is related to serotonin effect on somatodendritic 5-HT1A receptors, inhibiting the function of serotonergic neurons and thus preventing of the stress effect and inducing anxiolysis. So, in order to evaluate these aspects, female Wistar rats were ovariectomized and 21 days later were given a direct microinjection of estradiol benzoate (EB) (1200 ng) into the MRN, preceded by microinjections of saline or WAY100...
December 2017: Neurobiology of Stress
https://www.readbyqxmd.com/read/28626482/the-possible-mechanisms-of-analgesia-produced-by-microinjection-of-morphine-into-the-lateral-habenula-in-the-acute-model-of-trigeminal-pain-in-rats
#10
Emad Khalilzadeh, Gholamreza Vafaei Saiah
This study aimed to assess the effect of intra-habenular injection of morphine on acute trigeminal pain in rats. Also here, we examined the involvement of raphe nucleus opioid and 5HT3 receptors on the antinociceptive activity of intra habenular morphine to explore the possibility of existence of descending antinociceptive relay between the habenula and raphe nucleus. The numbers of eye wiping response elicited by applying a drop (40 μL) of NaCl (5 M) solution on the corneal surface were taken as an index of acute trigeminal nociception...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28626072/5-ht-causes-splanchnic-venodilation
#11
Bridget Mahon Seitz, Hakan Orer, Teresa Krieger-Burke, Emma S Darios, Janice M Thompson, Gregory D Fink, Stephanie W Watts
Serotonin (5-HT, 5-hydroxytrypamine) causes relaxation of the isolated superior mesenteric vein (SMV), a splanchnic blood vessel, through activation of the 5-HT7 receptor. As part of studies designed to identify the mechanism(s) through which chronic (>24 hours) infusion of 5-HT lowers blood pressure, we test the hypothesis that 5-HT causes an in vitro and in vivo splanchnic venodilation that is 5-HT7 receptor-dependent. In tissue baths for measurement of isometric contraction, the portal vein (PV) and abdominal inferior vena cava (Ab IVC) relaxed to 5-HT and the 5-HT1/7 receptor agonist 5-carboxamidotryptamine (5-CT); relaxation was abolished by the 5-HT7 receptor antagonist SB269970...
June 16, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28625456/the-effect-of-ondansetron-on-analgesic-efficacy-of-acetaminophen-after-hysterectomy-a-randomized-double-blinded-placebo-controlled-trial
#12
Onur Koyuncu, Steve Leung, Jing You, Menekse Oksar, Selim Turhanoglu, Cagla Akkurt, Kenan Dolapcioglu, Hanifi Sahin, Daniel I Sessler, Alparslan Turan
OBJECTIVES: To determine that perioperative ondansetron reduces the analgesic efficacy of acetaminophen. DESIGN: Randomized, double-blinded study. PATIENTS: 120 patients ASA I-II who underwent abdominal hysterectomy. INTERVENTIONS: All the patients were given 1g acetaminophen at skin closure. Patients were divided into two groups; ondansetron HCl (8mg, 2ml IV) (Group I, N=60) and saline (2ml IV) (Group II, N=60) at the skin closure...
August 2017: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/28623179/modulation-of-tgf-%C3%AE-smad-and-erk-signaling-pathways-mediates-the-anti-fibrotic-effect-of-mirtazapine-in-mice
#13
Dalia M El-Tanbouly, Walaa Wadie, Rabab H Sayed
Serotonin (5-HT) has been implicated as a key driver of liver fibrosis, acting via 5-HT2 receptor activation in the hepatic stellate cells. The current study was conducted to investigate the effects of mirtazapine, a 5-HT2A antagonist, in a mouse model of liver fibrosis. Mice received thioacetamide (TAA, 150mg/kg/biweekly, ip) for nine successive weeks for induction of liver fibrosis. Administration of mirtazapine significantly improved the plasma aminotransferases, reduced hepatic 5-HT concentration and ameliorated TAA-induced liver fibrosis, as demonstrated by reduced portal blood pressure, liver procollagen I content and α alpha smooth muscle actin expression...
June 13, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28621702/short-duration-physical-activity-prevents-the-development-of-activity-induced-hyperalgesia-through-opioid-and-serotoninergic-mechanisms
#14
Lucas V Lima, Josimari M DeSantana, Lynn A Rasmussen, Kathleen A Sluka, Lucas Vasconcelos Lima
Regular physical activity prevents development of chronic muscle pain through modulation of central mechanisms that involve rostral ventromedial medulla (RVM). We tested if pharmacological blockade or genetic deletion of mu-opioid receptors in physically active mice modulates excitatory and inhibitory systems in the RVM in an activity-induced hyperalgesia model. We examined response frequency to mechanical stimulation of the paw, muscle withdrawal thresholds, and expression of phosphorylation of the NR1 subunit of the NMDA receptor (p-NR1) and serotonin transporter (SERT) in the RVM...
June 8, 2017: Pain
https://www.readbyqxmd.com/read/28618340/fast-and-efficient-zirconia-based-reversed-phase-chromatography-for-selective-determination-of-triptans-in-rat-plasma
#15
Sameh Ahmed, Noha N Atia
Selective and fast chromatographic method was essential for the determination of triptans, selective serotonin receptor (5-HT1) agonists, in biological specimens. However, selective chromatographic separation of these highly basic drugs is a challenging problem on silica-based stationary phases. Zirconia-based stationary phases have been introduced as an efficient alternative for silica-based columns offering unique stability, selectivity, and retention ability for various classes of drugs. Herein, a new selective, fast and reproducible high performance liquid chromatographic method (HPLC) was developed and validated for the determination of four triptans in plasma samples namely; Sumatriptan (SMT), Zolmitriptan (ZLT), Eletriptan (ELT) and Rizatriptan (RZT)...
June 7, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28615487/cognitive-specialization-for-learning-faces-is-associated-with-shifts-in-the-brain-transcriptome-of-a-social-wasp
#16
Ali J Berens, Elizabeth A Tibbetts, Amy L Toth
The specialized ability to learn and recall individuals based on distinct facial features is known in only a few, large-brained social taxa. Social paper wasps in the genus Polistes are the only insects known to possess this form of cognitive specialization. We analyzed genome-wide brain gene expression during facial and pattern training for two species of paper wasps (P. fuscatus, which has face recognition, and P. metricus, which does not) using RNA sequencing. We identified 237 transcripts associated with face specialization in P...
June 15, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28612503/distinctive-in-vitro-signal-transduction-profile-of-nlx-112-a-potent-and-efficacious-serotonin-5-ht1a-receptor-agonist
#17
Adrian Newman-Tancredi, Jean-Claude Martel, Cristina Cosi, Peter Heusler, Fabrice Lestienne, Mark A Varney, Didier Cussac
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT1A receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. METHODS: NLX-112 was tested on G-protein activation, inhibition of adenylyl cyclase, ERK1/2 phosphorylation (pERK) and receptor internalization in recombinant cell lines. NLX-112 was also tested on G-protein activation in rat hippocampal membranes. Gα subunit mRNA expression in cell lines and rat brain tissue was quantified by quantitative PCR...
June 14, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28611585/role-of-n-arachidonoyl-serotonin-aa-5-ht-in-sleep-wake-cycle-architecture-sleep-homeostasis-and-neurotransmitters-regulation
#18
Eric Murillo-Rodríguez, Vincenzo Di Marzo, Sergio Machado, Nuno B Rocha, André B Veras, Geraldo A M Neto, Henning Budde, Oscar Arias-Carrión, Gloria Arankowsky-Sandoval
The endocannabinoid system comprises several molecular entities such as endogenous ligands [anandamide (AEA) and 2-arachidonoylglycerol (2-AG)], receptors (CB1 and CB2), enzymes such as [fatty acid amide hydrolase (FAHH) and monoacylglycerol lipase (MAGL)], as well as the anandamide membrane transporter. Although the role of this complex neurobiological system in the sleep-wake cycle modulation has been studied, the contribution of the blocker of FAAH/transient receptor potential cation channel subfamily V member 1 (TRPV1), N-arachidonoyl-serotonin (AA-5-HT) in sleep has not been investigated...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28608854/the-influence-of-the-rs6295-gene-polymorphism-on-serotonin-1a-receptor-distribution-investigated-with-pet-in-patients-with-major-depression-applying-machine-learning
#19
A Kautzky, G M James, C Philippe, P Baldinger-Melich, C Kraus, G S Kranz, T Vanicek, G Gryglewski, W Wadsak, M Mitterhauser, D Rujescu, S Kasper, R Lanzenberger
Major depressive disorder (MDD) is the most common neuropsychiatric disease and despite extensive research, its genetic substrate is still not sufficiently understood. The common polymorphism rs6295 of the serotonin-1A receptor gene (HTR1A) is affecting the transcriptional regulation of the 5-HT1A receptor and has been closely linked to MDD. Here, we used positron emission tomography (PET) exploiting advances in data mining and statistics by using machine learning in 62 healthy subjects and 19 patients with MDD, which were scanned with PET using the radioligand [carbonyl-(11)C]WAY-100635...
June 13, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28607752/enhanced-disease-reduction-using-clozapine-an-atypical-antipsychotic-agent-and-glatiramer-acetate-combination-therapy-in-experimental-autoimmune-encephalomyelitis
#20
Laura K Green, Pirooz Zareie, Nikki Templeton, Robert A Keyzers, Bronwen Connor, Anne Camille La Flamme
BACKGROUND: Atypical antipsychotic agents (AAP) alleviate the symptoms of severe mental health disorders, such as schizophrenia, by antagonizing dopamine and serotonin receptors. Recently, AAP have also been shown to exhibit immunomodulatory properties in the central nervous system (CNS). OBJECTIVE: Building on research which demonstrated the ability of the AAP risperidone and clozapine to modify the disease course of experimental autoimmune encephalomyelitis (EAE), an animal model of multiple sclerosis (MS), we aimed to more fully investigate the potential of clozapine as a possible treatment for MS...
January 2017: Multiple Sclerosis Journal—Experimental, Translational and Clinical
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