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https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#1
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28211304/granisetron-and-carvedilol-can-protect-experimental-rats-againstadjuvant-induced-arthritis
#2
Yasmin Moustafa Ahmed, Basim Anwar Shehata Messiha, Ali Ahmed Abo-Saif
CONTEXT: Rheumatoid arthritis (RA), a disabling autoimmune disorder of the joints as well as other organs, affects about 1% of population. Unfortunately, all current treatments of RA cause severe gastrointestinal, renal and other complications. OBJECTIVE: We aimed to evaluate the possible antiarthritic effects of a serotonin 5-HT3 receptor blocker, granisetron, and a nonselective adrenergic receptor blocker, carvedilol, on complete Freund's adjuvant-induced RA in adult female albino rats...
April 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28209485/effects-of-clozapine-on-adipokine-secretions-productions-and-lipid-droplets-in-3t3-l1-adipocytes
#3
Tomomi Tsubai, Akira Yoshimi, Yoji Hamada, Makoto Nakao, Hiroshi Arima, Yutaka Oiso, Yukihiro Noda
Clozapine, a second-generation antipsychotic (SGA), is a cause of side effects related to metabolic syndrome. The participation of serotonin 5-HT2C and histamine H1 receptors in the central nervous system has been reported as a mechanism of the weight gain caused by clozapine. In the present study, we investigated the direct pharmacological action of clozapine on the 3T3-L1 adipocytes and compared it to that of blonanserin, an SGA with low affinity for both receptors. Short-term exposure to clozapine decreased secretion and mRNA expression of leptin...
January 28, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28208011/glucosylsphingosine-activates-serotonin-receptor-2a-and-2b-implication-of-a-novel-itch-signaling-pathway
#4
Ramsha Afzal, Won-Sik Shim
Recent reports claimed that glucosylsphingosine (GS) is highly accumulated and specifically evoking itch-scratch responses in the skins of atopic dermatitis (AD) patients. However, it was unclear how GS can trigger itch-scratch responses, since there were no known molecular singling pathways revealed yet. In the present study, it was verified for the first time that GS can activate mouse serotonin receptor 2a (mHtr2a) and 2b (mHtr2b), but not 2c (mHtr2c) that are expressed in HEK293T cells. Specifically, effects of GS on all mouse serotonin receptor 2 subfamily were evaluated by calcium imaging techniques...
February 17, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28205278/optimal-dose-of-ramosetron-in-female-patients-with-irritable%C3%A2-bowel-syndrome-with-diarrhea-a-randomized-placebo-controlled-phase-ii-study
#5
S Fukudo, K Matsueda, K Haruma, M Ida, H Hayase, H Akiho, Y Nakashima, M Hongo
BACKGROUND: Previous studies showed that 5 μg of ramosetron, a serotonin (5-hydroxytryptamine: 5-HT)-3 receptor antagonist, is only effective in male patients with irritable bowel syndrome (IBS) with diarrhea (IBS-D). We hypothesized that either dose 1.25, 2.5, or 5 μg of ramosetron would be effective in female patients with IBS-D. METHODS: This randomized, double-blind, placebo-controlled, phase II dose-finding exploratory trial included 409 female outpatients with IBS-D treated in Japan...
February 16, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28203201/modulation-of-synaptic-plasticity-in-the-cortex-needs-to-understand-all-the-players
#6
REVIEW
Claire N J Meunier, Pascal Chameau, Philippe M Fossier
The prefrontal cortex (PFC) is involved in cognitive tasks such as working memory, decision making, risk assessment and regulation of attention. These functions performed by the PFC are supposed to rely on rhythmic electrical activity generated by neuronal network oscillations determined by a precise balance between excitation and inhibition balance (E/I balance) resulting from the coordinated activities of recurrent excitation and feedback and feedforward inhibition. Functional alterations in PFC functions have been associated with cognitive deficits in several pathologies such as major depression, anxiety and schizophrenia...
2017: Frontiers in Synaptic Neuroscience
https://www.readbyqxmd.com/read/28202410/atypical-antipsychotic-clozapine-reversed-deficit-on-prepulse-inhibition-of-the-acoustic-startle-reflex-produced-by-microinjection-of-doi-into-the-inferior-colliculus-in-rats
#7
Rodolpho Pereira de Oliveira, Karen Yuriko Nagaishi, Regina Cláudia Barbosa Silva
Dysfunctions of the serotonergic system have been suggested to be important in the neurobiology of schizophrenia. Patients with schizophrenia exhibit deficits in an operational measure of sensorimotor gating: prepulse inhibition (PPI) of startle. PPI is the normal reduction in the startle response caused by a low intensity non-startling stimulus (prepulse) which is presented shortly before the startle stimulus (pulse). The hallucinogen 2,5-dimethoxy-4-iodoamphetamine (DOI), a 5-hydroxytryptamine(HT)2 receptor agonist disrupted PPI in rats...
February 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28196617/the-neuropeptides-galanin-and-galanin-1-15-in-depression-like-behaviours
#8
REVIEW
Carmelo Millón, Antonio Flores-Burgess, Manuel Narváez, Dasiel O Borroto-Escuela, Belén Gago, Luis Santín, Estela Castilla-Ortega, José Ángel Narváez, Kjell Fuxe, Zaida Díaz-Cabiale
Galanin is a 29 amino acid neuropeptide widely distributed in neurons within the central nervous system. Galanin exerts its biological activities through three different G protein-receptors and participates in a number of functions, including mood regulation. Not only Galanin but also Galanin N-terminal fragments like Galanin(1-15) are active at the central level. In this work, we review the latest findings in studies on Galanin and Galanin(1-15) in depression-related behaviours. Our focus is on animal models for depression, and we pay some attention to research data obtained in human studies...
January 31, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28195088/serotonin-receptor-4-5-hydroxytryptamine-receptor-type-4-regulates-expression-of-estrogen-receptor-beta-and-cell-migration-in-hormone-naive-prostate-cancer
#9
Yasuhiro Nakamura, Kazue Ise, Yuto Yamazaki, Fumiyoshi Fujishima, Keely M McNamara, Hironobu Sasano
BACKGROUND: Estrogens are considered to potentially play some roles in the development and progression of prostate cancer through estrogen receptor beta (ERβ). However, additional factors which could influence the clinical outcome of the patients through modulating these steroid signalings have also been proposed. Among these, increased expression of serotonin receptor especially that of 5-hydroxytryptamine receptor Type 4 (5-HTR4) has been recently proposed to be involved in autocrine/paracrine mechanisms of castration-resistant prostate cancer, but the presence and clinical significance of 5-HTR4 in hormone-naive prostate cancer (HNPC) and its interaction with hormonal signaling pathways have remained virtually unknown...
January 2017: Indian Journal of Pathology & Microbiology
https://www.readbyqxmd.com/read/28194935/a-potential-pet-radiotracer-for-the-5-ht2c-receptor-synthesis-and-in-vivo-evaluation-of-4-3-18-f-fluorophenethoxy-pyrimidine
#10
Juhyeon Kim, Byung Seok Moon, Byung Chul Lee, Ho-Young Lee, Hak Joong Kim, Hyunah Choo, Ae Nim Pae, Yong Seo Cho, Sun-Joon Min
The serotonin 2C receptor subtype (5-HT2C) is an excitatory 5-HT receptor widely distributed throughout the central nerve system. As the 5-HT2C receptor displays multiple actions on various neurotransmitter systems including glutamate, dopamine, epinephrine and -aminobutyric acid (GABA), abnormalities of the 5-HT2C receptor are associated with psychiatric diseases such as depression, schizophrenia, drug abuse, and anxiety. Up to date, three kinds of 5-HT2C PET radiotracers such as [11C]N-methylated arylazepine (1), [11C]WAY-163909 (2), [18F]fluorophenylcyclopropane (3) have been developed, but they may not be suitable for in vivo 5-HT2C imaging study due to their modest specific binding...
February 14, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28194646/nanoemulsion-thermoreversible-pluronic-f127-based-hydrogel-containing-hyptis-pectinata-lamiaceae-leaf-essential-oil-produced-a-lasting-anti-hyperalgesic-effect-in-chronic-noninflammatory-widespread-pain-in-mice
#11
Lucindo J Quintans-Júnior, Renan G Brito, Jullyana S S Quintans, Priscila L Santos, Zaine T Camargo, Péricles A Barreto, Maria F Arrigoni-Blank, Waldecy Lucca-Júnior, Luciana Scotti, Marcus T Scotti, Sandra J Kolker, Kathleen A Sluka
We evaluated if a nanostructured thermoreversible Pluronic F127-based hydrogel incorporated with Hyptis pectinata leaf essential oil (NE-EOH) produces a long-lasting anti-hyperalgesic effect on chronic muscle pain in an animal model. We induced chronic muscle pain by injecting the gastrocnemius with saline injections. Paw and muscle withdrawal thresholds and motor performance were evaluated after treatment and compared with morphine, diazepam, or vehicle. Naloxone and methysergide administration tested the involvement of opioid and serotonin receptors, respectively...
February 13, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28194570/genetic-and-biochemical-changes-of-the-serotonergic-system-in-migraine-pathobiology
#12
REVIEW
Claudia Francesca Gasparini, Robert Anthony Smith, Lyn Robyn Griffiths
Migraine is a brain disorder characterized by a piercing headache which affects one side of the head, located mainly at the temples and in the area around the eye. Migraine imparts substantial suffering to the family in addition to the sufferer, particularly as it affects three times more women than men and is most prevalent between the ages of 25 and 45, the years of child rearing. Migraine typically occurs in individuals with a genetic predisposition and is aggravated by specific environmental triggers. Attempts to study the biochemistry of migraine began as early as the 1960s and were primarily directed at serotonin metabolism after an increase of 5-hydroxyindoleacetic acid (5-HIAA), the main metabolite of serotonin was observed in urine of migraineurs...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28194132/molecular-imaging-markers-to-track-huntington-s-disease-pathology
#13
REVIEW
Heather Wilson, Rosa De Micco, Flavia Niccolini, Marios Politis
Huntington's disease (HD) is a progressive, monogenic dominant neurodegenerative disorder caused by repeat expansion mutation in the huntingtin gene. The accumulation of mutant huntingtin protein, forming intranuclear inclusions, subsequently leads to degeneration of medium spiny neurons in the striatum and cortical areas. Genetic testing can identify HD gene carriers before individuals develop overt cognitive, psychiatric, and chorea symptoms. Thus, HD gene carriers can be studied in premanifest stages to understand and track the evolution of HD pathology...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28193998/inhibition-of-serotonin-receptor-type-1-in-acute-myeloid-leukemia-impairs-leukemia-stem-cell-functionality-a-promising-novel-therapeutic-target
#14
A Etxabe, M C Lara-Castillo, J M Cornet-Masana, A Banús-Mulet, M Nomdedeu, M A Torrente, M Pratcorona, M Díaz-Beyá, J Esteve, R M Risueño
Acute myeloid leukemia (AML) is a clinically and molecularly heterogeneous neoplasia with poor outcome, organized as a hierarchy initiated and maintained by a subpopulation with differentiation and self-renewal capacities called leukemia stem cells (LSCs). Although currently used chemotherapy is capable of initially reducing the tumor burden producing a complete remission, most patients will ultimately relapse and will succumb to their disease. As such, new therapeutic strategies are needed. AML cells differentially expressed serotonin receptors type 1 (HTR1) compared to healthy blood cells and the most primitive hematopoietic fraction; in fact, HTR1B expression on AML patient samples correlated with clinical outcome...
February 14, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28193834/genome-wide-analysis-of-the-circulating-mirnome-after-cerebral-ischemia-reveals-a-reperfusion-induced-microrna-cluster
#15
Stefan Uhlmann, Eva Mracsko, Ehsan Javidi, Sarah Lamble, Ana Teixeira, Agnes Hotz-Wagenblatt, Karl-Heinz Glatting, Roland Veltkamp
BACKGROUND AND PURPOSE: Circulating microRNAs (miRNAs) are emerging biomarkers for stroke because of their high stability in the bloodstream and association with pathophysiologic conditions. However, the circulating whole-genome miRNAs (miRNome) has not been characterized comprehensively in the acute phase of stroke. METHODS: We profiled the circulating miRNome in mouse models of acute ischemic and hemorrhagic stroke by next-generation sequencing. Stroke models were compared with sham-operated and naive mice to identify deregulated circulating miRNAs...
February 13, 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/28192174/does-genetic-bdnf-deficiency-in-rats-interact-with-neurotransmitter-control-of-prepulse-inhibition-implications-for-schizophrenia
#16
Maarten van den Buuse, Davina Biel, Kathrin Radscheit
Several studies have suggested a role of BDNF in the development of schizophrenia. For example, post-mortem studies have shown significantly reduced levels of BDNF protein expression in the brain of schizophrenia patients. We investigated the relationship between reduced levels of BDNF in the brain and the regulation of prepulse inhibition (PPI), a behavioral endophenotype of schizophrenia. We used BDNF heterozygous mutant rats which display a 50% decrease of mature BDNF protein levels. Previously, we observed normal baseline PPI and responses to the dopamine D1/D2 receptor agonist, apomorphine, in these rats...
February 9, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28188762/effects-of-the-5-ht6-receptor-antagonist-idalopirdine-on-extracellular-levels-of-monoamines-glutamate-and-acetylcholine-in-the-rat-medial-prefrontal-cortex
#17
Arne Mørk, Rasmus Vinther Russell, Inge E M de Jong, Gennady Smagin
Idalopirdine (Lu AE58054) is a high affinity and selective antagonist for the human serotonin 5-HT6 receptor (Ki 0.83nM) in phase III development for mild-to-moderate Alzheimer's disease as an adjunct therapy to acetylcholinesterase inhibitors (AChEIs). We have studied the effects of idalopirdine on extracellular levels of monoamines, glutamate and acetylcholine in the medial prefrontal cortex (mPFC) of freely-moving rats using microdialysis. Idalopirdine (10mg/kg p.o.) increased extracellular levels of dopamine, noradrenaline and glutamate in the mPFC and showed a trend to increase serotonin levels...
February 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28188677/5-hydroxytryptamine1a-receptor-density-in-the-hippocampus-of-patients-with-temporal-lobe-epilepsy-is-associated-with-disease-duration
#18
N C Fonseca, H P G Joaquim, L L Talib, S Vincentiis, W F Gattaz, K D Valente
BACKGROUND AND PURPOSE: To date, no study has evaluated the association between serotonin receptor density and clinical variables in patients with temporal lobe epilepsy caused by hippocampal sclerosis (TLE-HS) using hippocampal tissue. We evaluated 5-hydroxytryptamine1A receptor (5-HT1AR) density in hippocampal tissue from patients with TLE-HS. METHODS: We analyzed the hippocampal tissue of 34 patients with pharmacoresistant unilateral TLE-HS. 5-HT1AR density was measured using semiquantitative western blotting...
February 11, 2017: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
https://www.readbyqxmd.com/read/28185872/neuronal-and-molecular-effects-of-cannabidiol-on-the-mesolimbic-dopamine-system-implications-for-novel-schizophrenia-treatments
#19
REVIEW
Justine Renard, Christopher Norris, Walter Rushlow, Steven R Laviolette
Growing clinical and pre-clinical evidence points to a critical role for cannabidiol (CBD), the largest phytochemical component of cannabis, as a potential pharmacotherapy for various neuropsychiatric disorders. In contrast to delta-9-tetrahydrocannabinol (THC), which is associated with acute and neurodevelopmental pro-psychotic side-effects, CBD possesses no known psychoactive or dependence-producing properties. However, evidence has demonstrated that CBD strongly modulates the mesolimbic dopamine (DA) system and may possess promising anti-psychotic properties...
February 7, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28185036/practical-application-of-the-average-information-content-maximization-aic-max-algorithm-selection-of-the-most-important-structural-features-for-serotonin-receptor-ligands
#20
Dawid Warszycki, Marek Śmieja, Rafał Kafel
The Average Information Content Maximization algorithm (AIC-MAX) based on mutual information maximization was recently introduced to select the most discriminatory features. Here, this methodology was applied to select the most significant bits from the Klekota-Roth fingerprint for serotonin receptors ligands as well as to select the most important features for distinguishing ligands with activity for one receptor versus another. The interpretation of selected bits and machine-learning experiments performed using the reduced interpretations outperformed the raw fingerprints and indicated the most important structural features of the analyzed ligands in terms of activity and selectivity...
February 9, 2017: Molecular Diversity
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