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https://www.readbyqxmd.com/read/28499152/development-of-assay-for-determination-of-eletriptan-hydrobromide-in-loaded-plga-nanoparticles
#1
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...
May 2, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28486926/5-ht3-receptors-a-potential-therapeutic-target-for-epilepsy
#2
Hongyan Zhao, Pu Wang, Shurui Chen, Xin Li, Hongliang Huo
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. An increasing number of studies have shown that the activation of the 5-HT3 receptor can inhibit epileptic seizures, while inhibition of the 5HT3 receptor can promote spike waves...
May 8, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28465374/regulation-of-delta-opioid-receptor-mediated-signaling-and-antinociception-in-peripheral-sensory-neurons-by-arachidonic-acid-dependent-12-15-lipoxygenase-metabolites
#3
Laura C Sullivan, Teresa A Chavera, Xiaoli Gao, Miryam M Pando, Kelly A Berg
The function of delta opioid receptors (DOR) expressed by peripheral pain-sensing neurons (nociceptors) is regulated by both cyclooxygenase (COX)- and lipoxygenase (LOX)-dependent arachidonic acid (AA) metabolites (Sullivan et al., 2015). Whereas COX metabolites enhance responsiveness, LOX metabolites elicit a refractory, non-signaling 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 following treatment of adult rat primary sensory neuron cultures with AA...
May 2, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28459438/pericytes-impair-capillary-blood-flow-and-motor-function-after-chronic-spinal-cord-injury
#4
Yaqing Li, Ana M Lucas-Osma, Sophie Black, Mischa V Bandet, Marilee J Stephens, Romana Vavrek, Leo Sanelli, Keith K Fenrich, Antonio F Di Narzo, Stella Dracheva, Ian R Winship, Karim Fouad, David J Bennett
Blood vessels in the central nervous system (CNS) are controlled by neuronal activity. For example, widespread vessel constriction (vessel tone) is induced by brainstem neurons that release the monoamines serotonin and noradrenaline, and local vessel dilation is induced by glutamatergic neuron activity. Here we examined how vessel tone adapts to the loss of neuron-derived monoamines after spinal cord injury (SCI) in rats. We find that, months after the imposition of SCI, the spinal cord below the site of injury is in a chronic state of hypoxia owing to paradoxical excess activity of monoamine receptors (5-HT1) on pericytes, despite the absence of monoamines...
May 1, 2017: Nature Medicine
https://www.readbyqxmd.com/read/28409931/1-4-18-f-fluorobenzyl-4-tetrahydrofuran-2-yl-methyl-piperazine-a-novel-suitable-radioligand-with-low-lipophilicity-for-imaging-sigma-1-receptors-in-the-brain
#5
Yingfang He, Fang Xie, Jiajun Ye, Winnie Deuther-Conrad, Bixiao Cui, Liang Wang, Jie Lu, Jörg Steinbach, Peter Brust, Yiyun Huang, Jie Lu, Hongmei Jia
We have designed and synthesized novel piperazine compounds with low lipophilicity as σ1 receptor ligands. 1-(4-Fluorobenzyl)-4-((tetrahydrofuran-2-yl)methyl)piperazine (10) possessed low nanomolar σ1 receptor affinity and high selectivity toward the vesicular acetylcholine transporter (>2000-fold), σ2 receptors (52-fold), adenosine A2A, adrenergic α2, cannabinoid CB1, dopamine D1, D2L, γ-aminobutyric acid A (GABAA), NMDA, melatonin MT1, MT2 and serotonin 5-HT1 receptors. The corresponding radiotracer [(18)F]10 demonstrated high brain uptake and extremely high brain-to-blood ratios in biodistribution studies in mice...
April 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28287814/activation-and-deactivation-of-5-ht1-receptor-of-accumbens-shell-area-does-not-alter-acpa-induced-aversive-memory-deficit-in-male-rat
#6
Marzieh Keramati-Nojedehsadat, Shahrbanoo Oryan, Mohammad Reza Zarrindast, Vahab Babapour
BACKGROUND: Some studies have indicated a close relation between serotonergic and cannabinoidergic systems in several brain regions. Thus, the aim of current study is investigating the effect of 5-HT1 receptors of accumbens shell (Acb shell) on aversive memory deficit induced by ACPA (cannabinoid CB1 receptor agonist) using test-retest protocol of elevated plus-maze (EPM) in male Wistar rats. METHOD: Bilateral guide cannulae were implanted to allow microinjection of ACPA, CP94253 HCL (5-HT1 receptor agonist agonist) or GR127935 HCL (5-HT1 receptor antagonist)...
March 2017: Archives of Iranian Medicine
https://www.readbyqxmd.com/read/28229459/differential-serotonergic-modulation-across-the-main-and-accessory-olfactory-bulbs
#7
Zhenbo Huang, Nicolas Thiebaud, Debra Ann Fadool
KEY POINTS: There are serotonergic projections to both the main (MOB) and the accessory olfactory bulb (AOB). Current-clamp experiments demonstrate that serotonergic afferents are largely excitatory for mitral cells (MCs) in the MOB where 5-HT2A receptors mediate a direct excitatory action. Serotonergic afferents are predominately inhibitory for MCs in the AOB. There are two types of inhibition: indirect inhibition mediated through the 5-HT2 receptors on GABAergic interneurons and direct inhibition via the 5-HT1 receptors on MCs...
February 22, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28125053/interaction-of-new-developed-tio%C3%A2-based-photocatalytic-nanoparticles-with-pathogenic-microorganisms-and-human-dermal-and-pulmonary-fibroblasts
#8
Ionela Cristina Nica, Miruna Silvia Stan, Marcela Popa, Mariana Carmen Chifiriuc, Veronica Lazar, Gratiela G Pircalabioru, Iuliana Dumitrescu, Madalina Ignat, Marcel Feder, Liviu Cristian Tanase, Ionel Mercioniu, Lucian Diamandescu, Anca Dinischiotu
TiO₂-based photocatalysts were obtained during previous years in order to limit pollution and to ease human daily living conditions due to their special properties. However, obtaining biocompatible photocatalysts is still a key problem, and the mechanism of their toxicity recently received increased attention. Two types of TiO₂ nanoparticles co-doped with 1% of iron and nitrogen (TiO₂-1% Fe-N) atoms were synthesized in hydrothermal conditions at pH of 8.5 (HT1) and 5.5 (HT2), and their antimicrobial activity and cytotoxic effects exerted on human pulmonary and dermal fibroblasts were assessed...
January 25, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28107913/quantitative-structure-retention-relationship-model-for-the-determination-of-naratriptan-hydrochloride-and-its-impurities-based-on-artificial-neural-networks-coupled-with-genetic-algorithm
#9
Mikołaj Mizera, Anna Krause, Przemysław Zalewski, Robert Skibiński, Judyta Cielecka-Piontek
Mathematical modeling of Quantitative Structure - Property Relationships met great interest in fields of in silico drug design and more recently, pharmaceutical analysis. In our approach we proposed automated method of creation Quantitative Structure-Retention Relationship (QSRR) for analysis of triptans, selective serotonin 5-HT1 receptor agonists used for the treatment of acute headache. The method was created using hybrid machine learning approach, namely Genetic algorithm (GA) coupled with artificial neutral networks (ANN)...
March 1, 2017: Talanta
https://www.readbyqxmd.com/read/28040566/marked-sexual-dimorphism-in-5-ht1-receptors-mediating-pronociceptive-effects-of-sumatriptan
#10
Dioneia Araldi, Luiz F Ferrari, Paul Green, Jon D Levine
Amongst the side effects of triptans, a substantial percentage of patients experience injection site pain and tenderness, the underlying mechanism of which is unknown. We found that the dose range from 10fg to 1000ng (intradermal) of sumatriptan induced a complex dose-dependent mechanical hyperalgesia in male rats, with distinct peaks, at 1pg and 10ng, but no hyperalgesia at 1ng. In contrast, in females, there was 1 broad peak. The highest dose (1000ng) did not produce hyperalgesia in either sex. We evaluated the receptors mediating sumatriptan hyperalgesia (1pg, 1 and 10ng)...
March 6, 2017: Neuroscience
https://www.readbyqxmd.com/read/27926574/neural-activity-memory-and-dementias-serotonergic-markers
#11
Alfredo Meneses
Dysfunctional memory seems to be a key component of diverse dementias and other neuropsychiatric disorders; unfortunately, no effective treatment exists for this, probably because of the absence of neural biomarkers accompanying it. Diverse neurotransmission systems have been implicated in memory, including serotonin or 5-hydroxytryptamine (5-HT). There are multiple serotonergic pharmacological tools, well-characterized downstream signaling in mammals' species and neural markers providing new insights into memory functions and dysfunctions...
April 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27869315/aminoalkyl-derivatives-of-8-alkoxypurine-2-6-diones-multifunctional-5-ht1a-5-ht7-receptor-ligands-and-pde-inhibitors-with-antidepressant-activity
#12
Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Anna Partyka, Anna Wesołowska, Grzegorz Kazek, Monika Głuch-Lutwin, Agata Siwek, Gabriela Starowicz, Maciej Pawłowski
In the search for potential psychotropic agents, a new series of 3,7-dimethyl- and 1,3-dimethyl-8-alkoxypurine-2,6-dione derivatives of arylpiperazines, perhydroisoquinolines, or tetrahydroisoquinolines with flexible alkylene spacers (5-16 and 21-32) were synthesized and evaluated for 5-HT1A /5-HT7 receptor affinities as well as PDE4B1 and PDE10A inhibitory properties. The 1-(4-(4-(2-hydroxyphenyl)piperazin-1-yl)butyl)-3,7-dimethyl-8-propoxypurine-2,6-dione (16) and 7-(2-hydroxyphenyl)piperazinylalkyl-1,3-dimethyl-8-ethoxypurine-2,6-diones (31 and 32) as potent dual 5-HT1A /5-HT7 receptor ligands with antagonistic activity produced an antidepressant-like effect in the forced swim test in mice...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27777567/distribution-of-5-ht1f-receptors-in-monkey-vestibular-and-trigeminal-ganglion-cells
#13
Habiba O Usman, Carey D Balaban
BACKGROUND: Evidence of serotonergic involvement in vestibular pathway contributions to migraine and balance disorders is compelling. Serotonergic 5-HT1B and 5-HT1D receptors are expressed extensively in inner ear ganglia of monkeys and rats. The serotonergic 5-HT1F receptor is also a target of triptans. This study describes its distribution in vestibular and trigeminal ganglia of monkeys. METHODS: Using primary polyclonal antibodies raised against oligopeptides specific for the human 5-HT1F receptor, neuronal somatic area and intensity of immunoreactive vestibular and trigeminal ganglia were quantified...
2016: Frontiers in Neurology
https://www.readbyqxmd.com/read/27676327/chronic-sarpogrelate-treatment-reveals-5-ht7-receptor-in-the-serotonergic-inhibition-of-the-rat-vagal-bradycardia
#14
José Ángel García-Pedraza, Mónica García, María Luisa Martín, Nélida Eleno, Asunción Morán
5-Hydroxytryptamine (5-HT) modulates the cardiac parasympathetic neurotransmission, inhibiting the bradyarrhythmia by 5-HT2 receptor activation. We aimed to determine whether the chronic selective 5-HT2 blockade (sarpogrelate) could modify the serotonergic modulation on vagal cardiac outflow in pithed rat. Bradycardic responses in rats treated with sarpogrelate (30 mg·kg·d; orally) were obtained by electrical stimulation of the vagal fibers (3, 6, and 9 Hz) or intravenous (IV) injections of acetylcholine (1, 5, and 10 μg/kg)...
January 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/27570173/zerumbone-alleviates-chronic-constriction-injury-induced-allodynia-and-hyperalgesia-through-serotonin-5-ht-receptors
#15
Jasmine Siew Min Chia, Ahmad Akira Omar Farouk, Azam Shah Mohamad, Mohd Roslan Sulaiman, Enoch Kumar Perimal
Zerumbone, a bioactive sesquiterpene isolated from Zingiber zerumbet (Smith), has shown to exert antiallodynic and antihyperalgesic effects in neuropathic pain mice model in our recent study. The mechanism through which zerumbone alleviates neuropathic pain has yet to be elucidated. Thus, this study aimed to determine whether the serotonergic system, part of the descending pain modulation pathway, contributes to the antineuropathic effect of zerumbone. Participation of the serotonergic system in zerumbone-induced antiallodynia and antihyperalgesia was assessed using Dynamic Plantar Aesthesiometer von Frey test and Hargreaves plantar test respectively in chronic-constriction injury mice model...
October 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27544651/the-hallucinogen-d-lysergic-diethylamide-lsd-decreases-dopamine-firing-activity-through-5-ht1a-d2-and-taar1-receptors
#16
Danilo De Gregorio, Luca Posa, Rafael Ochoa-Sanchez, Ryan McLaughlin, Sabatino Maione, Stefano Comai, Gabriella Gobbi
d-lysergic diethylamide (LSD) is a hallucinogenic drug that interacts with the serotonin (5-HT) system binding to 5-HT1 and 5-HT2 receptors. Little is known about its potential interactions with the dopamine (DA) neurons of the ventral tegmental area (VTA). Using in-vivo electrophysiology in male adult rats, we evaluated the effects of cumulative doses of LSD on VTA DA neuronal activity, compared these effects to those produced on 5-HT neurons in the dorsal raphe nucleus (DRN), and attempted to identify the mechanism of action mediating the effects of LSD on VTA DA neurons...
August 17, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27531585/5-ht2a-receptor-enhancement-of-contractile-activity-of-the-porcine-urothelium-and-lamina-propria
#17
Christian Moro, Lily Edwards, Russ Chess-Williams
OBJECTIVES: To examine the effect of 5-hydroxytryptamine (5-HT; serotonin) on the contractile properties of the urothelium and lamina propria, as a better understanding of bladder physiology might aid the development of new treatments. METHODS: Strips of porcine urothelium and lamina propria were suspended in gassed Krebs-bicarbonate solution, and cumulative concentration-response curves for 5-HT were generated in the absence and presence of 5-HT antagonists, Nω-nitro-l-arginine and indomethacin...
August 16, 2016: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/27449278/the-potential-role-of-serotonergic-mechanisms-in-the-spinal-oxytocin-induced-antinociception
#18
Beatriz Godínez-Chaparro, Guadalupe Martínez-Lorenzana, Javier Rodríguez-Jiménez, Alfredo Manzano-García, Gerardo Rojas-Piloni, Miguel Condés-Lara, Abimael González-Hernández
The role of oxytocin (OXT) in pain modulation has been suggested. Indeed, hypothalamic paraventricular nuclei (PVN) electrical stimuli reduce the nociceptive neuronal activity (i.e., neuronal discharge associated with activation of Aδ- and C-fibers) of the spinal dorsal horn wide dynamic range (WDR) cells and nociceptive behavior. Furthermore, raphe magnus nuclei lesion reduces the PVN-induced antinociception, suggesting a functional interaction between the OXT and the serotoninergic system. The present study investigated in Wistar rats the potential role of spinal serotonergic mechanisms in the OXT- and PVN-induced antinociception...
December 2016: Neuropeptides
https://www.readbyqxmd.com/read/27411565/the-electroacupuncture-induced-analgesic-effect-mediated-by-5-ht1-5-ht3-receptor-and-muscarinic-cholinergic-receptors-in-rat-model-of-collagenase-induced-osteoarthritis
#19
Byung-Kwan Seo, Won-Suk Sung, Yeon-Cheol Park, Yong-Hyeon Baek
BACKGROUND: Osteoarthritis (OA) is an degenerative disease characterized by chronic joint pain. Complementary and alternative treatment such as acupuncture have been utilized to alleviate pain. The objective of this study was to investigate the analgesic mechanisms of electroacupuncture (EA) in the collagenase-induced osteoarthritis (CIOA) rat model. METHODS: Four weeks after inducing CIOA by injecting collagenase solution into the left knee of 5-week-old male Sprague-Dawley rats, 2 Hz and 100 Hz EA on Zusanli (ST 36) was performed...
July 13, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27317942/the-serotonergic-5-ht4-receptor-a-unique-modulator-of-hippocampal-synaptic-information-processing-and-cognition
#20
Hardy Hagena, Denise Manahan-Vaughan
Serotonin (5-hydroxytryptamine, 5-HT) contributes in multifarious ways to the regulation of brain function, spanning key aspects such as the sleep-wake cycle, appetite, mood and mental health. The 5-HT receptors comprise seven receptor families (5-HT1-7) that are further subdivided into 14 receptor subtypes. The role of the 5-HT receptor in the modulation of neuronal excitability has been well documented. Recently, however, it has become apparent that the 5-HT4 receptor may contribute significantly to cognition and regulates less ostensible aspects of brain function: it engages in metaplastic regulation of synaptic responsiveness in key brain structures such as the hippocampus, thereby specifically promoting persistent forms of synaptic plasticity, and influences the direction of change in synaptic strength in selected hippocampal subfields...
June 15, 2016: Neurobiology of Learning and Memory
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