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https://www.readbyqxmd.com/read/29719628/novel-water-soluble-lignin-derivative-bp-cx-1-identification-of-components-and-screening-of-potential-targets-in-silico-and-in-vitro
#1
Elena I Fedoros, Alexey A Orlov, Alexander Zherebker, Ekaterina A Gubareva, Mikhail A Maydin, Andrey I Konstantinov, Konstantin A Krasnov, Ruben N Karapetian, Ekaterina I Izotova, Sergey E Pigarev, Andrey V Panchenko, Margarita L Tyndyk, Dmitry I Osolodkin, Evgeny N Nikolaev, Irina V Perminova, Vladimir N Anisimov
Identification of molecular targets and mechanism of action is always a challenge, in particular - for natural compounds due to inherent chemical complexity. BP-Cx-1 is a water-soluble modification of hydrolyzed lignin used as the platform for a portfolio of innovative pharmacological products aimed for therapy and supportive care of oncological patients. The present study describes a new approach, which combines in vitro screening of potential molecular targets for BP-Cx-1 using Diversity Profile - P9 panel by Eurofins Cerep (France) with a search of possible active components in silico in ChEMBL - manually curated chemical database of bioactive molecules with drug-like properties...
April 6, 2018: Oncotarget
https://www.readbyqxmd.com/read/29569251/prenatal-triptan-exposure-and-neurodevelopmental-outcomes-in-5-year-old-children-follow-up-from-the-norwegian-mother-and-child-cohort-study
#2
Gerd-Marie Eskerud Harris, Mollie Wood, Eivind Ystrom, Hedvig Nordeng
BACKGROUND: Triptans are commonly used to treat migraine headaches, but data on the long-term safety of these medications during pregnancy are sparse. Triptans have a biologically plausible mechanism for effects on the fetal brain through binding to 5-HT1 -receptors, and previous studies show increased risks of externalising behaviour problems in toddlers exposed to triptans during pregnancy. METHODS: We included 3784 children in the Norwegian Mother and Child Cohort Study, whose mothers returned the 5-year-questionnaire and reported a history of migraine or triptan use; 353 (9...
March 23, 2018: Paediatric and Perinatal Epidemiology
https://www.readbyqxmd.com/read/29555828/activation-of-5-ht1a-receptors-in-the-hypothalamic-paraventricular-nuclei-pvn-negatively-regulates-cytochrome-p450-expression-and-activity-in-rat-liver
#3
Ewa Bromek, Marta Rysz, Anna Haduch, Jacek Wojcikowski, Władysława Anna Daniel
Our recent work suggested a negative effect for the serotonergic innervation of the paraventricular nuclei (PVN) of the hypothalamus on growth hormone secretion and growth hormone-dependent expression of cytochrome P450 2C11 (CYP2C11). The aim of our present research was to determine the effect of the activation of the 5-HT1 or 5-HT2 receptors in the PVN on the expression and activity of cytochrome P450 in male rat liver. The serotonergic agonists 5-CT (5-carboxyamidotryptamine, a 5-HT1 receptor-type agonist), 8-OH-DPAT (8-hydroxy-2-(di-n-propyloamino)-tetralin, a 5-HT1A receptor agonist), sumatriptan (a 5-HT1B/D receptor agonist) and DOI (2,5-dimethoxy-4-iodoamphetamine, a 5-HT2A/C receptor agonist) were individually injected into the PVN...
March 19, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29524471/electroacupuncture-restores-hippocampal-synaptic-plasticity-via-modulation-of-5-ht-receptors-in-a-rat-model-of-depression
#4
Xuke Han, Huangan Wu, Ping Yin, Zeqin Chen, Xiaohua Cao, Yanhong Duan, Jian Xu, Lixing Lao, Shifen Xu
OBJECTIVE: The study aimed to determine the effect of electroacupuncture (EA) on Wistar Kyoto (WKY) depressive model rats and explore the possible mechanism of EA on hippocampal CA1 region neuronal synaptic plasticity. METHODS: The male WKY rats were randomized to three experimental groups (EA, Sham EA, and Model group, n = 8/group), and Wistar rats as the normal control group (n = 8). EA treatment was administered once daily for 3 weeks at acupuncture points Baihui (GV20) and Yintang (EX-HN3)...
May 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29495103/effects-of-sumatriptan-nasal-spray-imigran-on-human-nasal-mucosa
#5
L-H Cheng, P-C Wu, Y-Y Lin, Y-H Chu, H-W Wang
OBJECTIVES: Sumatriptan (Imigran) is a potent and highly selective 5-HT1 receptor agonist often used in treating acute migraine. Intranasal sumatriptan is well absorbed and is generally effective in relieving headache. However, the effects of Imigran on human nasal mucosa have rarely been well explored, to verify the effect of Imigran, which act on human nasal mucosa directly in vitro. DESIGN AND PARTICIPANTS: We examined the effectiveness of Imigran on human nasal mucosa by testing: (i) effect on human nasal mucosa resting tension; (ii) effect on contraction caused by 10-6  mol/L methoxamine as a sympathetic mimetic; and (iii) effect of the drugs on electrically induced on human nasal mucosa contractions...
March 1, 2018: Clinical Otolaryngology
https://www.readbyqxmd.com/read/29488143/targeted-5-ht-1f-therapies-for-migraine
#6
REVIEW
Marta Vila-Pueyo
Migraine is a common neurological disease characterised by the presence of attacks of unilateral, severe head pain accompanied by other symptoms. Although it has been classified as the sixth most disabling disorder, the available therapeutic options to treat this condition have not progressed accordingly. The advance in the development of 5-HT1 receptor agonists for migraine, including 5-HT1B/D and 5-HT1F receptor agonists, has meant a major step forward towards the progression of a better treatment for migraine...
April 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
https://www.readbyqxmd.com/read/29409499/mechanisms-of-multiple-neurotransmitters-in-the-effects-of-lycopene-on-brain-injury-induced-by-hyperlipidemia
#7
Weichun Yang, Ziyi Shen, Sixian Wen, Wei Wang, Minyu Hu
BACKGROUND: Lycopene is a kind of carotenoid, with a strong capacity of antioxidation and regulating the bloodlipid. There has been some evidence that lycopene has protective effects on the central nervous system, but few studies have rigorously explored the role of neurotransmitters in it. Therefore, the present study was designed to investigate the effects of several neurotransmitters as lycopene exerts anti-injury effects induced by hyperlipidemia. METHODS: Eighty adult SD rats, half male and half female, were randomly divided into eight groups on the basis of serum total cholesterol (TC) levels and body weight...
February 7, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29379077/immunomodulatory-capacity-of-the-serotonin-receptor-5-ht2b-in-a-subset-of-human-dendritic-cells
#8
Attila Szabo, Peter Gogolak, Gabor Koncz, Zsofia Foldvari, Kitti Pazmandi, Noemi Miltner, Szilard Poliska, Attila Bacsi, Srdjan Djurovic, Eva Rajnavolgyi
Serotonin is a monoamine neurotransmitter that signals through a wide array of receptors (5-HT1-7 ) many of which are also involved in immune processes. Dendritic cells (DCs) are crucial players in immune defense by bridging innate and adaptive immune responses via their vast repertoire of pattern recognition receptors and antigen-presenting capability. Although serotonin is known to influence immunity at many levels, cell type-specific expression and function of its receptors remains poorly understood. Here we aimed to study 5-HT1-7 expression and function in CD1a- and CD1a+ human monocyte-derived DCs (moDCs)...
January 29, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29305167/a-serotonin-receptor-cg5-htr-1-mediating-immune-response-in-oyster-crassostrea-gigas
#9
Yunke Jia, Bin Yang, Wenjing Dong, Zhaoqun Liu, Zhao Lv, Zhihao Jia, Limei Qiu, Lingling Wang, Linsheng Song
Serotonin receptors, including ligand-gated ion channel (LGICs) and G protein-coupled receptors (GPCR), play vital roles in modulating physiological processes and immunoreaction. In the present study, a homologue of serotonin (5-HT) receptor was identified from oyster Crassostrea gigas (designated Cg5-HTR-1). Its open reading frame (ORF) was of 1239 bp, encoding a polypeptide of 412 amino acids with a seven transmembrane region. Cg5-HTR-1 shared high similarity with the 5-HTRs from other animals. The cAMP contents in HEK293T cells decreased significantly after Cg5-HTR-1 transfection and 5-HT incubation (p < ...
May 2018: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/29290056/presynaptic-serotonin-5-ht-1b-d-receptor-mediated-inhibition-of-glycinergic-transmission-to-the-frog-spinal-motoneurons
#10
N I Kalinina, Aleksey V Zaitsev, N P Vesselkin
Endogenous monoamine 5-hydroxytryptamine (5-HT, serotonin) is a phylogenetically ancient neurotransmitter present in vertebrates. The functions of 5-HT in central nervous system are intensively studied; however, the presynaptic effects of 5-HT in frog spinal motoneurons are practically unexplored. We have previously shown that 5-HT decreases the frequency of glycinergic miniature inhibitory postsynaptic potentials (mIPSPs), but does not affect the frequency of GABAergic mIPSPs and increases the frequency of glutamatergic postsynaptic potentials...
March 2018: Journal of Comparative Physiology. A, Neuroethology, Sensory, Neural, and Behavioral Physiology
https://www.readbyqxmd.com/read/29022279/the-role-of-%C3%AE-1-and-%C3%AE-2-adrenoceptor-subtypes-in-the-vasopressor-responses-induced-by-dihydroergotamine-in-ritanserin-pretreated-pithed-rats
#11
Eduardo Rivera-Mancilla, Victor H Avilés-Rosas, Guadalupe Manrique-Maldonado, Alain H Altamirano-Espinoza, Belinda Villanueva-Castillo, Antoinette MaassenVanDenBrink, Carlos M Villalón
BACKGROUND: Dihydroergotamine (DHE) is an acute antimigraine agent that displays affinity for dopamine D2 -like receptors, serotonin 5-HT1/2 receptors and α1 /α2 -adrenoceptors. Since activation of vascular α1 /α2 -adrenoceptors results in systemic vasopressor responses, the purpose of this study was to investigate the specific role of α1 - and α2 -adrenoceptors mediating DHE-induced vasopressor responses using several antagonists for these receptors. METHODS: For this purpose, 135 male Wistar rats were pithed and divided into 35 control and 100 pretreated i...
October 11, 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28901281/review-5-ht1-5-ht2-5-ht3-and-5-ht7-receptors-and-their-role-in-the-modulation-of-pain-response-in-the-central-nervous-system
#12
Jose Luis Cortes-Altamirano, Adriana Olmos-Hernandez, Herlinda Bonilla Jaime, Paul Carrillo-Mora, Cindy Bandala, Samuel Reyes-Long, Alfonso Alfaro-Rodríguez
BACKGROUND: The aim of this review was to identify the mechanisms by which serotonin receptors involved at the central level are able to modulate the nociceptive response. Pain is a defense mechanism of the body that entails physiological, anatomical, neurochemical, and psychological changes, and is defined as an unpleasant sensory and emotional experience with potential risk of tissue damage, comprising the leading cause of appointments with Physicians worldwide. Treatment for this symptom has generated several neuropharmacological lines of research, due to the different types of pain and the various drugs employed to treat this condition...
January 30, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/28821451/5-ht7-receptor-antagonism-sb-269970-attenuates-bleomycin-induced-pulmonary-fibrosis-in-rats-via-downregulating-oxidative-burden-and-inflammatory-cascades-and-ameliorating-collagen-deposition-comparison-to-terguride
#13
Mona K Tawfik, Samy Makary
The neurotransmitter 5-hydroxytryptamine (5-HT) is involved in regulation of local tissue inflammation and repair through a set of receptors (5-HT1-7 receptors), which are expressed in the lung. Considering the protective importance of 5-HT receptor antagonists against development of pulmonary fibrosis, we evaluated whether 5-HT7 receptor antagonist (SB-269970) modulates lung inflammatory and fibrogenic processes in comparison with 5-HT2A/B receptor antagonist (terguride), in bleomycin (BLM)-induced idiopathic pulmonary fibrosis (IPF) model...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28771848/5-ht-modulates-the-rat-mesenteric-vasopressor-outflow-by-5-ht1d-sympatholytic-receptors
#14
José-Ángel García-Pedraza, Mónica García-Domingo, Miriam Gómez-Roso, Alicia Rodríguez-Barbero, María-Luisa Martín, Asunción Morán
5-hydroxytryptamine (5-HT) modulates noradrenergic activity in different cardiovascular territories, but its effect on the mesenteric vasopressor outflow has not yet been clarified. This study investigated the in vivo serotonergic influence, characterizing 5-HT receptors implicated, in sympathetic innervation of mesenteric vasculature. Wistar rats were anaesthetised and prepared for the in situ autoperfused rat mesentery, monitoring systemic blood pressure (SBP), heart rate (HR) and mesenteric perfusion pressure (MPP)...
August 3, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28626072/5-ht-causes-splanchnic-venodilation
#15
Bridget M Seitz, Hakan S Orer, Teresa Krieger-Burke, Emma S Darios, Janice M Thompson, Gregory D Fink, Stephanie W Watts
Serotonin [5-hydroxytryptamine (5-HT)] causes relaxation of the isolated superior mesenteric vein, 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 h) infusion of 5-HT lowers blood pressure, we tested the hypothesis that 5-HT causes in vitro and in vivo splanchnic venodilation that is 5-HT7 receptor dependent. In tissue baths for measurement of isometric contraction, the portal vein and abdominal inferior vena cava relaxed to 5-HT and the 5-HT1/7 receptor agonist 5-carboxamidotryptamine; relaxation was abolished by the 5-HT7 receptor antagonist SB-269970...
September 1, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28618340/fast-and-efficient-zirconia-based-reversed-phase-chromatography-for-selective-determination-of-triptans-in-rat-plasma
#16
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)...
September 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28590304/antinociceptive-effect-of-epicatechin-in-inflammatory-and-neuropathic-pain-in-rats
#17
Geovanna N Quiñonez-Bastidas, Jorge B Pineda-Farias, Francisco J Flores-Murrieta, Juan Rodríguez-Silverio, Juan G Reyes-García, Beatriz Godínez-Chaparro, Vinicio Granados-Soto, Héctor I Rocha-González
The aim of this study was to investigate the antinociceptive potential of (-)-epicatechin and the possible mechanisms of action involved in its antinociceptive effect. The carrageenan and formalin tests were used as inflammatory pain models. A plethysmometer was used to measure inflammation and L5/L6 spinal nerve ligation as a neuropathic pain model. Oral (-)-epicatechin reduced carrageenan-induced inflammation and nociception by about 59 and 73%, respectively, and reduced formalin- induced and nerve injury-induced nociception by about 86 and 43%, respectively...
April 2018: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28499152/development-of-assay-for-determination-of-eletriptan-hydrobromide-in-loaded-plga-nanoparticles
#18
Ozgur Esim, Ayhan Savaser, Sevinc Kurbanoglu, Cansel K Ozkan, Sibel A Ozkan, Yalcin Ozkan
Eletriptan Hydrobromide is a serotonin 5-HT1 receptor agonist and it used for the treatment of migraine headaches with or without aura. Even if the drug is well absorbed after oral administration, it has some drawbacks like first pass metabolism and decrease in bioavailability after migraine attacks. Encapsulation of drug into polymeric nanoparticles is one of the methods for protecting the drug against degradation. The present work described a preparation of Eletriptan Hydrobromide loaded poly (d,l-lactide-co-glycolide) nanoparticles prepared using o/w single emulsion solvent evaporation method...
August 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28486926/5-ht3-receptors-a-potential-therapeutic-target-for-epilepsy
#19
Hongyan Zhao, Yang Lin, Shurui Chen, Xin Li, Hongliang Huo
BACKGROUND: Epilepsy is a syndrome of brain dysfunction caused by spontaneous, abnormal discharge. Many anti-epileptic drugs have developed in past decades. 5-HT is an important neurotransmitter in the central and peripheral nervous system of the human body which is involved in a number of physiological activities, such as sensation, movement, and behavior. 5-HT subtype have been divided into seven sub-groups from 5-HT1 to 5HT7. However, the role of 5-HT3 receptor on epilepsy is unclear...
2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/28465374/regulation-of-%C3%AE-opioid-receptor-mediated-signaling-and-antinociception-in-peripheral-sensory-neurons-by-arachidonic-acid-dependent-12-15-lipoxygenase-metabolites
#20
Laura C Sullivan, Teresa A Chavera, Xiaoli Gao, Miryam M Pando, Kelly A Berg
The function of δ opioid receptors (DOR) expressed by peripheral pain-sensing neurons (nociceptors) is regulated by both cyclooxygenase- and lipoxygenase (LOX)-dependent arachidonic acid (AA) metabolites. Whereas cyclooxygenase metabolites enhance responsiveness, LOX metabolites elicit a refractory, nonsignaling state of the DOR receptor system for antinociceptive signaling. In this study, using high-performance liquid chromatography-tandem mass spectrometry analyses, we have found that the 12-/15-LOX metabolites, 12-hydroxyeicosatetraenoic acid (HETE) and 15-HETE, were elevated after treatment of adult rat primary sensory neuron cultures with AA...
July 2017: Journal of Pharmacology and Experimental Therapeutics
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