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https://www.readbyqxmd.com/read/28214685/role-of-laxative-and-antioxidant-properties-of-malva-sylvestris-leaves-in-constipation-treatment
#1
Mohamed-Amine Jabri, Dalanda Wannes, Najla Hajji, Mohsen Sakly, Lamjed Marzouki, Hichem Sebai
INTRODUCTION: Mallaw (Malva sylvestris L.) is a medicinal plant who is traditionally being used as an antiulcer, laxative and anti-hemorrhoid, besides of its culinary use as a food in Tunisian cuisine. The present study was carried out to evaluate the protective effect of Malva sylvestris aqueous extract (MSAE) on constipation- induced by loperamide in male Wistar rats. METHODS: Rats were divided into six groups of six animals each: Control, Loperamide (LOP), LOP+ yohimbine (2mg/kg b...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28207596/a-role-for-adrenergic-receptors-in-the-uterotonic-effects-of-ergometrine-in-isolated-human-term-nonlaboring-myometrium
#2
Rebecca A Fanning, Florike Sheehan, Claire Leyden, Niamh Duffy, Luis F Iglesias-Martinez, Michael F Carey, Deirdre P Campion, John J O'Connor
BACKGROUND: Ergometrine is a uterotonic agent that is recommended in the prevention and management of postpartum hemorrhage. Despite its long-standing use, the mechanism by which it acts in humans has never been elucidated fully. The objective of this study was to investigate the role of adrenoreceptors in ergometrine's mechanism of action in human myometrium. The study examined the hypothesis that α-adrenoreceptor antagonism would result in the reversal of the uterotonic effects of ergometrine...
February 15, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28190472/gastroprotective-and-anti-secretory-mechanisms-of-2-phenylquinoline-an-alkaloid-isolated-from-galipea-longiflora
#3
Eduardo Breviglieri, Luisa Mota da Silva, Thaise Boeing, Lincon Bordignon Somensi, Benhur Judah Cury, Alberto Gimenez, Valdir Cechinel Filho, Sérgio Faloni de Andrade
BACKGROUND: We previously described the gastroprotective effect of 2-phenylquinoline (2-PQ), the main alkaloid isolated from the bark of Galipea longiflora (Rutaceae). However, despite the significant and promising results, the pharmacological mechanisms of the gastroprotection induced by 2-PQ have not been investigated. PURPOSE: To evaluate the mechanisms underlying the gastroprotective effects of 2-PQ. STUDY DESIGN: We used an in vivo mouse ulcer model and in vitro methodologies involving H⁺/K⁺-ATPase and L929 murine fibroblasts...
February 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28188706/comparison-of-atipamezole-with-yohimbine-for-antagonism-of-xylazine-in-mice-anesthetized-with-ketamine-and-xylazine
#4
Christopher F Janssen Pauline Maiello M Jerry Wright Jr Kara B Kracinovsky And Joseph T Newsome
The α2 adrenergic agonist xylazine produces a sedative effect and is typically combined with ketamine and used for anesthesia or chemical restraint of laboratory mice. Xylazine's sedative effect-and its undesirable side effects of bradycardia, hypotension, and poor tissue perfusion-can be reversed by administration of α2 antagonists, such as atipamezole or yohimbine. Although atipamezole and yohimbine dosing guidelines are available for mice, no controlled comparison has been performed to guide the lab animal community in the selection of one over the other...
February 10, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28168894/effect-of-combined-opioid-receptor-and-%C3%AE-2-adrenoceptor-blockade-on-anxiety-and-electrically-evoked-startle-responses
#5
Lechi Vo, Peter D Drummond
The R3 component of the electrically evoked blink reflex may form part of a startle reaction. Acoustic startle responses are augmented by yohimbine, an α2-adrenoceptor antagonist that blocks α2-autoreceptors, and are potentiated by opioid receptor blockade. To investigate these influences on electrically evoked startle responses, 16 mg yohimbine, with (16 participants) or without 50 mg naltrexone (23 participants), was administered in separate double-blind placebo-controlled cross-over experiments. In each experiment, R3 (a probable component of the startle response) was examined before and after high-frequency electrical stimulation of the forearm, a procedure that initiates inhibitory pain controls...
January 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28167291/elucidation-of-the-possible-mechanism-of-analgesic-actions-of-butanol-leaf-fraction-of-olax-subscorpioidea-oliv
#6
Saidi Odoma, Abdulkadir Umar Zezi, Nuhu Mohammed Danjuma, Abubakar Ahmed, Muhammed Garba Magaji
ETHNOPHARMACOLOGICAL RELEVANCE: Preparations of Olax subscorpioidea have been used traditionally for the management of pains, inflammatory diseases, yellow fever, cancer and rheumatism. Previously, the analgesic activity of its leaf extract have been reported. Furthermore, an analgesic assay guided fractionation showed that the butanol soluble fraction is the most active. However, the mechanism of this activity remains to be elucidated. This present study investigated the possible pharmacological mechanisms involved in the analgesic activity of the butanol leaf fraction of Olax subscorpioidea (BFOS) using the acetic acid induced writhing test in mice...
February 3, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28149034/acute-pesticide-ingestion-managed-with-yohimbine-as-a-rescue-therapy
#7
Prashant Nasa, Deven Juneja
Amitraz is used as a pesticide in agricultural and veterinary medicine. It is primarily a central α2 adrenergic agonist and known to cause central nervous system depression, convulsions, respiratory depression, and bradycardia on severe intoxication. We report a case of a 3-year-old child who presented with accidental ingestion of amitraz solution with signs of severe poisoning. There is no specific antidote of amitraz poisoning in humans, however, animal experiments with α2 adrenergic antagonists such as yohimbine and atimepazole have been successful...
December 2016: Indian Journal of Critical Care Medicine
https://www.readbyqxmd.com/read/28110639/amitraz-poisoning-a-case-report-of-an-unusual-pesticide-poisoning-in-sri-lanka-and-literature-review
#8
H M M T B Herath, S P Pahalagamage, Nilukshana Yogendranathan, M D M S Wijayabandara, Aruna Kulatunga
BACKGROUND: Amitraz is a pesticide used worldwide on animals and in agriculture. It contains triazapentadiene, which is a centrally acting alpha-2 adrenergic agonist. Amitraz poisoning is fairly uncommon in humans and occurs via oral, dermal or inhalational routes. Only a limited number of case reports of human intoxication have been published and most of them are of accidental ingestion by children. CASE PRESENTATION: A twenty-year-old Sri Lankan female presented following self-ingestion of 20 ml of amitraz resulting in 37...
January 23, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28094445/presynaptic-inhibition-of-transient-receptor-potential-vanilloid-type-1-trpv1-receptors-by-norepinephrine-in-nociceptive-neurons
#9
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
#10
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
#11
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
#12
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...
March 2017: Veterinary Research Communications
https://www.readbyqxmd.com/read/27939988/amtar2-functional-characterization-of-a-honeybee-tyramine-receptor-stimulating-adenylyl-cyclase-activity
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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