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https://www.readbyqxmd.com/read/28094445/presynaptic-inhibition-of-transient-receptor-potential-vanilloid-type-1-trpv1-receptors-by-norepinephrine-in-nociceptive-neurons
#1
Saikat Chakraborty, Vincent Elvezio, Martin Kaczocha, Mario Rebecchi, Michelino Puopolo
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a well-known contributor to nociceptor excitability. To address whether norepinephrine can down-regulate TRPV1 channel activity in nociceptors and reduce their synaptic transmission, the effects of norepinephrine and clonidine were tested on the capsaicin-activated current recorded from acutely dissociated small diameter (<27 μm) dorsal root ganglia (DRG) neurons and on miniature excitatory postsynaptic currents (mEPSCs) recorded from large lamina I neurons in horizontal spinal cord slices...
January 17, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28028077/endogenous-%C3%AE-2a-adrenoceptor-operated-sympathoadrenergic-tones-attenuate-insulin-secretion-via-camp-trpm2-signaling
#2
Kiyonori Ito, Katsuya Dezaki, Masashi Yoshida, Hodaka Yamada, Rina Miura, Rauza Sukma Rita, Susumu Ookawara, Kaoru Tabei, Masanobu Kawakami, Kazuo Hara, Yoshiyuki Morishita, Toshihiko Yada, Masafumi Kakei
In pancreatic β-cells, pharmacological concentrations of catecholamines, including adrenaline, have been used to inhibit insulin release and explore the multiple mechanisms involved. However, the significance of these signaling pathways for physiological adrenergic functions in β-cells is largely unknown. In the process of glucose-induced insulin secretion, opening of background current through non-selective cation channels (NSCCs) might facilitate membrane depolarization by closure of the ATP-sensitive K(+) channels...
December 27, 2016: Diabetes
https://www.readbyqxmd.com/read/27998004/dexmedetomidine-preconditioning-for-myocardial-protection-in-ischemia-reperfusion-injury-in-rats-by-downregulation-of-the-hmgb1-tlr4-nf-%C3%AE%C2%BAb-signaling-pathway
#3
Yu-Fan Yang, Ke Peng, Hong Liu, Xiao-Wen Meng, Jing-Jing Zhang, Fu-Hai Ji
Pharmacological preconditioning reduces myocardial infarct size in ischemia-reperfusion (I-R) injury. Dexmedetomidine, a selective α2 -adrenoceptor agonist, has proven cardioprotective effect when administered prior to I-R, although underlying mechanisms for this effect are not fully understood. We evaluated whether dexmedetomidine preconditioning could induce a myocardio-protective effect against I-R injury by inhibiting associated inflammatory processes through downregulation of the high mobility group box 1 (HMGB1)-toll-like receptor 4 (TLR4)-nuclear factor κB (NF-κB) signaling pathway...
December 20, 2016: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/27975177/involvement-of-histaminergic-and-noradrenergic-receptors-in-the-oxytocin-induced-food-intake-in-neonatal-meat-type-chicks
#4
Seyed Vahid Mirnaghizadeh, Morteza Zendehdel, Vahab Babapour
Oxytocin neurons have a physiological role in food intake and energy balance. Several studies have shown that central histaminergic and adrenergic systems synapse on oxytocin neurons but there is no information for their interaction on food intake regulation in birds. The purpose of this study was to examine the effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptors antagonist), famotidine (histamine H2 receptors antagonist), thioperamide (histamine H3 receptors antagonist), prazosin (α1 receptor antagonist), yohimbine (α2 receptor antagonist), metoprolol (β1 adrenergic receptor antagonist), ICI 118,551 (β2 adrenergic receptor antagonist) and SR59230R (β3 adrenergic receptor antagonist) on oxytocin-induced hypophagia in 3-h food-deprived (FD3) neonatal broiler chicken...
December 14, 2016: Veterinary Research Communications
https://www.readbyqxmd.com/read/27939988/amtar2-functional-characterization-of-a-honeybee-tyramine-receptor-stimulating-adenylyl-cyclase-activity
#5
Tina Reim, Sabine Balfanz, Arnd Baumann, Wolfgang Blenau, Markus Thamm, Ricarda Scheiner
The biogenic monoamines norepinephrine and epinephrine regulate important physiological functions in vertebrates. Insects such as honeybees do not synthesize these neuroactive substances. Instead, they employ octopamine and tyramine for comparable physiological functions. These biogenic amines activate specific guanine nucleotide-binding (G) protein-coupled receptors (GPCRs). Based on pharmacological data obtained on heterologously expressed receptors, α- and β-adrenergic-like octopamine receptors are better activated by octopamine than by tyramine...
January 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/27939978/%C3%AE-1-adrenergic-receptor-downregulates-hepatic-fgf21-production-and-circulating-fgf21-levels-in-mice
#6
Katsunori Nonogaki, Takao Kaji
Fibroblast growth factor 21 (FGF21) is primarily secreted by the liver as an endocrine hormone and is suggested as a promising target for the treatment of metabolic diseases. FGF21 acts centrally to exert its effects on energy expenditure and body weight via the sympathetic nervous system in mice. Here we show that intraperitoneal injection of phentolamine (an α-adrenergic receptor antagonist, 5mg/kg) significantly increased plasma FGF21 levels compared with the saline controls in C57BL6J mice, whereas alprenolol (a β-adrenergic receptor antagonist, 6mg/kg) had no effect...
December 6, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27939824/pulmonary-platelet-accumulation-induced-by-catecholamines-its-involvement-in-lipopolysaccharide-induced-anaphylaxis-like-shock
#7
Zhiqian Yu, Hiroko Saito, Hirotada Otsuka, Yosuke Shikama, Hiromi Funayama, Mai Sakai, Shigeo Murai, Masanori Nakamura, Takashi Yokochi, Haruhiko Takada, Shunji Sugawara, Yasuo Endo
Intravenously injected lipopolysaccharides (LPS) rapidly induce pulmonary platelet accumulation (PPA) and anaphylaxis-like shock (ALS) in mice. Macrophages reportedly release catecholamines rapidly upon stimulation with LPS. Here, we examined the involvement of macrophage-derived catecholamines in LPS-induced PPA and ALS. A catecholamine or Klebsiella O3 (KO3) LPS was intravenously injected into mice, with 5-hydroxytryptamine in the lung being measured as a platelet marker. The tested catecholamines induced PPA, leading to shock...
February 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/27916366/rubus-occidentalis-analgesic-effect-in-a-rat-model-of-incisional-pain
#8
Geun Joo Choi, Hyun Kang, Won Joong Kim, Ji Wung Kwon, Beom Gyu Kim, Yoo Shin Choi, Young Joo Cha, Jin Soo Ko
BACKGROUND: The purpose of this study was to evaluate the analgesic effect of Rubus occidentalis extract (ROE) in a rat model of incisional pain. The involved mechanisms and proinflammatory cytokine response were also examined. MATERIALS AND METHODS: To investigate the analgesic effect, rats were intraperitoneally administered with normal saline or various doses of ROE before or after a plantar incision. To evaluate the involved mechanism, rats were intraperitoneally administered yohimbine, dexmedetomidine, prazosin, naloxone, atropine, or mecamylamine after a plantar incision; ROE was then administered intraperitoneally...
November 2016: Journal of Surgical Research
https://www.readbyqxmd.com/read/27912885/tetrandrine-an-alkaloid-from-s-tetrandra-exhibits-anti-hypertensive-and-sleep-enhancing-effects-in-shr-via-different-mechanisms
#9
Yuan-Li Huang, Su-Ying Cui, Xiang-Yu Cui, Qing Cao, Hui Ding, Jin-Zhi Song, Xiao Hu, Hui Ye, Bin Yu, Zhao-Fu Sheng, Zi-Jun Wang, Yong-He Zhang
BACKGROUND: Sleep disorders have been found to be associated with hypertension in both cross-sectional and longitudinal epidemiological studies. Tetrandrine, a major component of Stephania tetrandra, is well known as an antihypertensive agent. The anti-hypertension mechanism mainly relies on its L-type calcium channel blocking property. In the previous study, tetrandrine revealed both anti-hypertension and hypnotic effects in spontaneously hypertensive rats (SHRs). PURPOSE: This study aims to elucidate whether the antihypertensive mechanism of tetrandrine in SHRs is relevant to its hypnotic effect...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27900785/a-tryptoline-ring-distortion-strategy-leads-to-complex-and-diverse-biologically-active-molecules-from-the-indole-alkaloid-yohimbine
#10
Nicholas Paciaroni, Ranjala Ratnayake, James Matthews, Verrill Norwood, Austin Arnold, Long Dang, Hendrik Luesch, Robert William Huigens Iii
High-throughput screening (HTS) is the primary driver to current drug discovery efforts. New therapeutic agents that enter the market are a direct reflection of the structurally simple compounds that make up screening libraries. Unlike medically relevant natural products (e.g., morphine), small molecules currently being screened have low fraction sp3 character and few, if any, stereogenic centers. Although simple compounds have been useful in drugging certain biological targets (e.g., protein kinases), more sophisticated targets (e...
November 29, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27896229/effect-of-%C3%AE-2-adrenergic-agonists-and-antagonists-on-cytokine-release-from-human-lung-macrophages-cultured-in-vitro
#11
O Piazza, R I Staiano, E De Robertis, G Conti, V Di Crescenzo, S Loffredo, G Marone, G Zito Marinosci, M M Cataldi
The most trusted hypothesis to explain how α2-adrenergic agonists may preserve pulmonary functions in critically ill patients is that they directly act on macrophages by interfering with an autocrine/paracrine adrenergic system that controls cytokine release through locally synthetized noradrenaline and α1- and α2-adrenoreceptors. We tested this hypothesis in primary cultures of resident macrophages from human lung (HLMs). HLMs were isolated by centrifugation on percoll gradients from macroscopically healthy human lung tissue obtained from four different patients at the time of lung resection for cancer...
November 2016: Translational Medicine @ UniSa
https://www.readbyqxmd.com/read/27891620/modulation-of-formalin-induced-pain-related-behaviour-by-clonidine-and-yohimbine-in-the-speke-s-hinged-tortoise-kiniskys-spekii
#12
C M Makau, P K Towett, K S P Abelson, T I Kanui
The study was designed to investigate the involvement of noradrenergic and serotonergic receptor systems in the modulation of formalin-induced pain-related behaviour in the Speke's hinged tortoise. Intradermal injection of 100 μL of formalin at a dilution of 12.5% caused pain-related behaviour (hindlimb withdrawal) that lasted for a mean time of 19.28 min (monophasic response). Intrathecal administration of clonidine (α2 -adrenergic receptor agonist) and yohimbine (α2 -adrenergic receptor antagonist) at a dose of 40 μg/kg and 37...
November 27, 2016: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27891593/remote-chemical-immobilisation-method-for-free-ranging-australian-cattle
#13
J O Hampton, A Skroblin, A L Perry, T R De Ridder
BACKGROUND: Many situations are encountered in Australia where the capture and restraint of free-ranging cattle (Bos taurus/Bos indicus) is required. Chemical immobilisation via darting is a potentially useful tool for managing and researching large wild herbivores; however, there is no reliable method for its application to Australian cattle. The aim of this study was to develop an efficacious, humane, cost-effective ground darting method for free-ranging cattle. METHODS: The 30 female cattle were darted and captured on a pastoral station in north-west Australia from a vehicle...
December 2016: Australian Veterinary Journal
https://www.readbyqxmd.com/read/27847559/impaired-norepinephrine-regulation-of-monocyte-inflammatory-cytokine-balance-in-heart-failure
#14
Tien Mh Ng, Myron L Toews
AIM: To evaluate the effect of norepinephrine on inflammatory cytokine expression in ex vivo human monocytes and monocytic THP-1 cells. METHODS: For human monocyte studies, cells were isolated from 12 chronic heart failure (HF) (66 ± 12 years, New York Heart Association functional class III-IV, left ventricular ejection fraction 22% ± 9%) and 14 healthy subjects (66 ± 12 years). Monocytes (1 × 10(6)/mL) were incubated with lipopolysaccharide (LPS) 100 ng/mL, LPS + norepinephrine (NE) 10(-6) mol/L or neither (control) for 4 h...
October 26, 2016: World Journal of Cardiology
https://www.readbyqxmd.com/read/27845775/defining-the-role-of-corticotropin-releasing-factor-binding-protein-in-alcohol-consumption
#15
C L Haass-Koffler, A T Henry, G Melkus, J A Simms, M Naemmuddin, C K Nielsen, A W Lasek, M Magill, M L Schwandt, R Momenan, C A Hodgkinson, S E Bartlett, R M Swift, A Bonci, L Leggio
The corticotropin releasing factor (CRF) exerts its effects by acting on its receptors and on the binding protein (CRFBP), and has been implicated in alcohol use disorder (AUD). Therefore, identification of the exact contribution of each protein that mediates CRF effects is necessary to design effective therapeutic strategies for AUD. A series of in vitro/in vivo experiments across different species were performed to define the biological discrete role of CRFBP in AUD. First, to establish the CRFBP role in receptor signaling, we developed a novel chimeric cell-based assay and showed that CFRBP full length can stably be expressed on the plasma membrane...
November 15, 2016: Translational Psychiatry
https://www.readbyqxmd.com/read/27826897/interactions-between-%C3%AE-adrenergic-vasodilation-and-cervical-sympathetic-nerves-are-mediated-by-%C3%AE-2-adrenoceptors-in-the-rat-masseter-muscle
#16
Hisayoshi Ishii, Toshiya Sato
Neural and humoral autonomic mechanisms may be important in the maintenance of blood flow in the masseter muscle (MBF). However, their interactions remain unclear. In this study, we examined interactions between neural and humoral regulation of MBF and investigated the mechanisms mediating these interactions in urethane-anesthetized rats. Stimulation of the adrenal nerve (AN) projecting to the adrenal medulla increased MBF, and this increase was mediated by β-adrenoceptors. Sectioning of the superior cervical sympathetic trunk (CST) significantly inhibited increases in MBF induced by AN stimulation during high activity in the CST, but not during low activity...
November 8, 2016: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/27806917/clonidine-preconditioning-alleviated-focal-cerebral-ischemic-insult-in-rats-via-up-regulating-p-nmdar1-and-down-regulating-nmdar2a-p-nmdar2b
#17
Li Yanli, Zhang Xizhou, Wang Yan, Zhao Bo, Zha Yunhong, Li Zicheng, Yu Lingling, Yan Lingling, Chen Zhangao, Zheng Min, He Zhi
A brain ischemia rat model was established by middle cerebral artery occlusion (MCAO) for 2h and reperfusion for 4h to investigate the underlying mechanism of the neuroprotection action of clonidine, a classical alpha-2 adrenergic agonist, on cerebral ischemia. Clonidine and yohimbine were intraperitoneally given to the rats each day for a week before ischemia. Neurological deficits evaluations were carried out at 6h after operation. TTC staining method was used to measure the volume of brain infarction. Expression levels of NMDAR1, NMDAR2A, NMDAR2B were assayed by western blotting...
December 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27780710/the-effects-of-baicalein-on-gastric-mucosal-ulcerations-in-mice-protective-pathways-and-anti-secretory-mechanisms
#18
Ana Roseli S Ribeiro, José Diego do Nascimento Valença, Jeferson da Silva Santos, Thaise Boeing, Luisa Mota da Silva, Sérgio Faloni de Andrade, Ricardo L C Albuquerque-Júnior, Sara Maria Thomazzi
Many flavonoids have been shown to present good results for the treatment of gastric ulcers. Baicalein, a bioactive flavonoid derived from the Scutellaria baicalensis Georgi root, possesses several biological effects, such as anti-inflammatory and antioxidant. This study was conducted to assess the gastroprotective properties of baicalein. Anti-ulcerogenic assay was performed using the protocol of ulcer induced by ethanol/HCl in mice; then, the role of presynaptic α2-receptors, sulfhydryl (SH) compounds, nitric oxide (NO), prostaglandin (PG) and ATP-sensitive K(+) (KATP) channels in gastroprotection of baicalein was investigated...
December 25, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27770304/involvement-of-monoaminergic-systems-in-anxiolytic-and-antidepressive-activities-of-the-standardized-extract-of-cocos-nucifera-l
#19
Eliane Brito Cortez Lima, Caren Nádia Soares de Sousa, Lucas Nascimento Meneses, Yuri Freitas E Silva Pereira, Natália Castelo Branco Matos, Rayanne Brito de Freitas, Nycole Brito Cortez Lima, Manoel Cláudio Azevedo Patrocínio, Luzia Kalyne Almeida Moreira Leal, Glauce Socorro Barros Viana, Silvânia Maria Mendes Vasconcelos
Extracts from the husk fiber of Cocos nucifera are used in folk medicine, but their actions on the central nervous system have not been studied. Here, the anxiolytic and antidepressant effects of the standardized hydroalcoholic extract of C. nucifera husk fiber (HECN) were evaluated. Male Swiss mice were treated with HECN (50, 100, or 200 mg/kg) 60 min before experiments involving the plus maze test, hole-board test, tail suspension test, and forced swimming test (FST). HECN was administered orally (p.o.) in acute and repeated-dose treatments...
October 21, 2016: Journal of Natural Medicines
https://www.readbyqxmd.com/read/27739080/peek-tube-based-online-solid-phase-microextraction-high-performance-liquid-chromatography-for-the-determination-of-yohimbine-in-rat-plasma-and-its-application-in-pharmacokinetics-study
#20
Xiaowei Xiang, Bing Shang, Xiaozheng Wang, Qinhua Chen
Yohimbine is a novel compound for the treatment of erectile dysfunction derived from natural products, and pharmacokinetic study is important for its further development as a new medicine. In this work, we developed a novel PEEK tube-based solid-phase microextraction (SPME)-HPLC method for analysis of yohimbine in plasma and further for pharmacokinetic study. Poly (AA-EGDMA) was synthesized inside a PEEK tube as the sorbent for microextraction of yohimbine, and parameters that could influence extraction efficiency were systematically investigated...
October 14, 2016: Biomedical Chromatography: BMC
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