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Yohimbine

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https://www.readbyqxmd.com/read/27916366/rubus-occidentalis-analgesic-effect-in-a-rat-model-of-incisional-pain
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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...
October 30, 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
#11
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...
October 22, 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
#12
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
#13
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
https://www.readbyqxmd.com/read/27729248/new-2-aminothiazoline-derivatives-lower-blood-pressure-of-spontaneously-hypertensive-rats-shr-via-i1-imidazoline-and-alpha-2-adrenergic-receptors-activation
#14
Renan B Ferreira, Mariana G de Oliveira, Edson Antunes, Wanda P Almeida, Badr M Ibrahim, Abdel A Abdel-Rahman
2-Aminothiazolines share an isosteric relationship with imidazolines and oxazolines with antihypertensive activity mainly mediated by the imidazoline I1-receptor. In the present work, we have prepared five aminothiazolines, following a previously described synthetic pathway. Aminothiazolines derived from dicyclopropylmethylamine (ATZ1) and cyclohexylamine (3) are unprecedented in the literature. Competitive radioligand assay was carried out with all synthetic compounds, and the I1 receptor affinity in comparison to rilmenidine in PC12 cells was determined...
October 8, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27714428/pioglitazone-attenuates-the-opioid-withdrawal-and-vulnerability-to-relapse-to-heroin-seeking-in-rodents
#15
Giordano de Guglielmo, Marsida Kallupi, Giulia Scuppa, Gregory Demopulos, George Gaitanaris, Roberto Ciccocioppo
RATIONALE: Relapse to opioids is often driven by the avoidance of the aversive states of opioid withdrawal. We recently demonstrated that activation of peroxisome proliferator-activated receptor gamma (PPARγ) by pioglitazone reduces the motivation for heroin and attenuates its rewarding properties. However, the role of PPARγ in withdrawal and other forms of relapse to heroin is unknown. OBJECTIVES: To further address this issue, we investigated the role of PPARγ on the development and expression of morphine withdrawal in mice and the effect of pioglitazone on several forms of heroin relapse in rats...
October 6, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27677376/dexmedetomidine-protects-against-glucocorticoid-induced-progenitor-cell-apoptosis-in-neonatal-mouse-cerebellum
#16
Shawn David O'Connor, Omar Hoseá Cabrera, Joseph D Dougherty, Sukrit Singh, Brant Stephen Swiney, Patricia Salinas-Contreras, Nuri Bradford Farber, Kevin Kiyoshi Noguchi
OBJECTIVES: Glucocorticoids (GC) are used to improve respiratory mechanics in preterm infants despite clinical evidence linking neonatal GC therapy to cerebellar pathology. In developing mouse cerebellum, the GC dexamethasone (DEX) causes rapid GC-induced neural progenitor cell apoptosis (GINA). Focusing on pharmacological neuroprotection strategies, we investigated whether dexmedetomidine (DMT) protects against GINA. METHODS: Neonatal mice were pretreated with DMT prior to DEX challenge...
September 27, 2016: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/27664442/freeze-dried-extracts-of-bidens-biternata-lour-merr-and-sheriff-show-significant-antidiarrheal-activity-in-in-vivo-models-of-diarrhea
#17
Dennis Gacigi Kinuthia, Anne W Muriithi, Peter Waweru Mwangi
ETHNOPHARMACOLOGICAL RELEVANCE OF THE STUDY: Diarrhea remains one of the main killers of children aged below five years. Traditional antidiarrheal remedies form a potentially viable source of novel low cost efficacious treatments in low resource settings. There is therefore a pressing need to scientifically evaluate these remedies. AIM OF THE STUDY: This study aimed to investigate the in vivo and in vitro antidiarrheal activity of freeze dried Bidens biternata, a herb used in traditional Ayurvedic medicine in the management of diarrhea...
September 21, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27659409/sarcolemmal-%C3%AE-2-adrenoceptors-control-protective-cardiomyocyte-delimited-sympathoadrenal-response
#18
Yuri M Kokoz, Edward V Evdokimovskii, Alexander V Maltsev, Miroslav N Nenov, Olga V Nakipova, Alexey S Averin, Oleg Yu Pimenov, Ilia Y Teplov, Alexey V Berezhnov, Santiago Reyes, Alexey E Alekseev
Sustained cardiac adrenergic stimulation has been implicated in the development of heart failure and ventricular dysrhythmia. Conventionally, α2 adrenoceptors (α2-AR) have been assigned to a sympathetic short-loop feedback aimed at attenuating catecholamine release. We have recently revealed the expression of α2-AR in the sarcolemma of cardiomyocytes and identified the ability of α2-AR signaling to suppress spontaneous Ca(2+) transients through nitric oxide (NO) dependent pathways. Herein, patch-clamp measurements and serine/threonine phosphatase assay revealed that, in isolated rat cardiomyocytes, activation of α2-AR suppressed L-type Ca(2+) current (ICaL) via stimulation of NO synthesis and protein kinase G- (PKG) dependent activation of phosphatase reactions, counteracting isoproterenol-induced β-adrenergic activation...
September 19, 2016: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/27652229/the-drug-treatment-of-delayed-ejaculation
#19
REVIEW
Ibrahim A Abdel-Hamid, Moustafa A Elsaied, Taymour Mostafa
Delayed ejaculation (DE) is an uncommon and a challenging disorder to treat. It is often quite concerning to patients and it can affect psychosocial well-being. Here we reviewed how DE is treated pharmacologically .We also highlighted specific settings where drugs could be introduced to medical practice. Electronic databases were searched from 1966 to February 2016, including PubMed MEDLINE, EMBASE, EBCSO Academic Search Complete, Cochrane Systematic Reviews Database, and Google Scholar using key words; delayed ejaculation, retarded ejaculation, inhibited ejaculation, drugs, treatment, or pharmacology...
August 2016: Translational Andrology and Urology
https://www.readbyqxmd.com/read/27616615/onset-of-a-hypotensive-effect-following-ingestion-of-flavan-3-ols-involved-in-the-activation-of-adrenergic-receptors
#20
Akiko Saito, Kodai Inagawa, Rikihiko Ebe, Shinobu Fukase, Yukari Horikoshi, Masahiro Shibata, Naomi Osakabe
A lot of epidemiological and intervention studies support the hypotensive action resulting from ingestion of foods rich in flavan 3-ols. However, the mechanisms of this action remain unclear. We have reported previously on the alteration of the micro- and systemic circulations after administration of a flavan 3-ol fraction (FL) derived from cocoa in mammals. We also confirmed that blood catecholamine levels increase significantly after administration of FL. In the present study, we examined whether adrenaline receptors are involved in the hemodynamic changes using several adrenaline receptor (AR) blockers...
September 9, 2016: Free Radical Biology & Medicine
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