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Yohimbine

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https://www.readbyqxmd.com/read/28633926/synergic-stimulation-of-serotonin-5-ht1a-receptor-and-%C3%AE-2-adrenoceptors-for-neuropathic-pain-relief-preclinical-effects-of-2-substituted-imidazoline-derivatives
#1
Lorenzo Di Cesare Mannelli, Carla Ghelardini, Laura Micheli, Fabio Del Bello, Mario Giannella, Alessandro Piergentili, Wilma Quaglia
Neuropathic pain affects millions of people causing disability and impairing quality of life. Commonly used analgesics are generally characterized by limited therapeutic outcomes. The serotonin 5-HT1A receptor and the α2 adrenergic receptors are involved in central nociceptive mechanisms with a pivotal role in the inhibitory descending pain pathway. Since their stimulation may modulate the nervous signaling altered by neuropathies, the purpose of the present research is the study of the combined activation of 5-HT1A and α2 receptors by rationally designed imidazoline ligands ((S)-1 and 2-5) in a rat model of neuropathic pain (chronic constriction injury - CCI)...
June 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28627793/increased-sympathetic-outflow-induces-adaptation-to-acute-experimental-pain
#2
Lior Dayan, Uri Hochberg, Hadas Nahman-Averbuch, Silviu Brill, Jacob N Ablin, Giris Jacob
BACKGROUND: There are interrelationships between the autonomic nervous system and pain. This study aims to explore the effect of different autonomic manipulations on pain perception and modulation. METHODS: Twenty healthy subjects (10 men and 10 women, mean age 25±3) participate in this single-blinded, semi-randomized, controlled study, which included 2 study visits. Warm and heat pain thresholds, conditioned pain modulation and pain adaptation were tested before and after administration of phenylephrine, clonidine, yohimbine and saline...
June 19, 2017: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/28626198/the-therapeutic-effect-of-dexmedetomidine-on-rat-diabetic-neuropathy-pain-and-the-mechanism
#3
Yuecheng Lu, Baohua Lin, Junmin Zhong
Diabetic neuropathy pain (DNP) is a common chronic complication of diabetes characterized by spontaneous pain, hyperalgesia and allodynia. Dexmedetomidine is a selective α2 adrenergic agonist that relieves sympathetic nervous tension and reduces the release of glutamate. Thus, it is possible that dexmedetomidine may relieve DNP as well. In this study, we examined the effect of dexmedetomidine on DNP in the presence or absence of the α2 adrenergic antagonist yohimbine in rats utilizing a streptozotocin (STZ)-induced diabetes as a model of DNP...
June 14, 2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28623711/contribution-of-dopaminergic-and-noradrenergic-systems-in-the-antinociceptive-effect-of-%C3%AE-phenylalanyl-acetophenone
#4
Fernanda S S Sousa, Roberta G Anversa, Paloma T Birmann, Maurice N de Souza, Renata Balaguez, Diego Alves, Cristiane Luchese, Ethel A Wilhelm, Lucielli Savegnago
BACKGROUND: This study evaluated the antinociceptive action of α-(phenylalanyl) acetophenone (PSAP) in mice. METHODS: Evaluated whether the serotonergic, adrenergic and dopaminergic systems are involved in PSAP antinociceptive activity. PSAP was administered intragastrically (ig) 30min prior to formalin or glutamate test and compared with a standard drug, meloxicam (10mg/kg, ig). RESULTS: The treatment with PSAP (10-50mg/kg) caused inhibition in the neurogenic phase and reduced the paw oedema caused by intraplantar (ipl) injection of formalin...
March 27, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28603125/estimation-of-yohimbine-base-in-complex-mixtures-by-quantitative-hptlc-application
#5
Maged Saad Adel-Kader, Naif Wahebi Hamadan Alwahebi, Prawez Alam
The indole alkaloid Yohimbine has been used for over two centuries in the treatment of erectly dysfunction. Several formulations containing yohimbine salts, yohimbe bark power or extract are marketed worldwide. Determination of the amount of yohimbine in such formulation is a challenging task due to their complex nature. Extraction followed by acid-base purification resulted in a relatively pure alkaloids containing fractions. The exact amounts of yohimbine free base in different formulations were determined by densitometric HPTLC validated methods using silica gel TLC plates...
January 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28576724/interaction-of-gaba-and-norepinephrine-in-the-lateral-division-of-the-bed-nucleus-of-the-stria-terminals-in-anesthetized-rat-correlating-single-unit-and-cardiovascular-responses
#6
Fahimeh Yeganeh, Ali Nasimi, Masoumeh Hatam
The bed nucleus of the stria terminalis (BST) consists of multiple anatomically distinct nuclei. The lateral division, which receives dense noradrenergic innervation, has been implicated in cardiovascular regulation and modulation of responses to stress. This study is performed to identify the cardiovascular and single-unit responses of the lateral BST to norepinephrine (NE), involved adrenoceptors, and possible interaction with GABAergic system of the BST in urethane-anesthetized rats. NE, adrenoreceptor antagonists, and GABAA antagonist were microinjected into the lateral division of BST, while arterial pressure (AP), heart rate (HR), and single-unit responses were simultaneously recorded...
May 31, 2017: Neuroscience
https://www.readbyqxmd.com/read/28555511/mitigation-of-inflammation-using-the-intravenous-anesthetic-dexmedetomidine-in-the-mouse-air-pouch-model
#7
Takefumi Inada, Chisato Sumi, Kiichi Hirota, Koh Shingu, Akihisa Okamoto, Yoshiyuki Matsuo, Takahiko Kamibayashi
Dexmedetomidine, an α2-adrenergic/imidazoline receptor agonist, is a widely used intravenous anesthetic. Its primary current usage is for sedation of patients in the intensive care unit. The mouse air pouch model is versatile in studying the anti-inflammatory effect of a drug on a local inflammation, which is induced by a variety of substances. In the present study, using the carrageenan-induced air pouch inflammation model, we tested whether dexmedetomidine mitigates inflammation occurring locally in the mouse air pouch...
May 30, 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28507504/effects-of-%C3%AE-2a-adrenoceptors-on-norepinephrine-secretion-from-the-locus-coeruleus-during-chronic-stress-induced-depression
#8
Bin Wang, Ying Wang, Qiong Wu, Hong-Ping Huang, Shao Li
Chronic stressors can often lead to the development of psychological disorders, such as depression and anxiety. The locus coeruleus (LC) is a stress sensitive brain region located in the pons, with noradrenergic neurons that project to the hypothalamus, especially the paraventricular nucleus (PVN) of the hypothalamus. The purpose of this paper is to better understand how alpha 2A-adrenoceptors (α2A-ARs) and LC-hypothalamus noradrenergic system participate in the pathophysiological mechanism of depression. In vivo norepinephrine (NE) release in the PVN triggered by electrical stimulation in the LC was detected with carbon fiber electrodes in depression model of rats induced by chronic unpredictable mild stress (CUMS)...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28499312/evidence-for-the-involvement-of-monoaminergic-pathways-in-the-antidepressant-like-activity-of-cymbopogon-citratus-in-mice
#9
Solomon Umukoro, Somtochukwu I Ogboh, Osarume Omorogbe, Abdul-Lateef A Adekeye, Matthew O Olatunde
Objectives Depression is a complex neuropsychiatric disorder, which affects the quality of life of the sufferers and treatment approach is associated with serious adverse effects and sometimes therapeutic failures. Cymbopogon citratus leaf (CC) has been reported to exert anti-depressant effect but its mechanism of action is yet to be elucidated hence, the need for this study. Methods The anti-depressant-like effect of Cymbopogon citratus aqueous leaf was evaluated using forced swim test (FST), tail suspension test (TST) and yohimbine-induced lethality test (YLT) in aggregated mice...
May 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28491012/are-alpha-2d-adrenoceptor-subtypes-involved-in-rat-mydriasis-evoked-by-new-imidazoline-derivatives-marsanidine-and-7-methylmarsanidine
#10
Joanna Raczak-Gutknecht, Teresa Frąckowiak, Antoni Nasal, Anita Kornicka, Franciszek Sączewski, Roman Kaliszan
The imidazoline compounds may produce mydriasis after systemic administration to some species (rats, cats, and mice). In mydriatic activity of imidazolines, α2D-adrenoceptors subtype(s) seems to be involved. In this study, the pupil dilatory effect evoked by 2 newly synthesized imidazoline derivatives-α2-adrenoceptor agonists: marsanidine and 7-methylmarsanidine-was compared. The compounds were tested alone as well as in the presence of α2-adrenoceptor antagonists (nonselective, yohimbine, and selective toward the following α2-adrenoceptor subtypes-α2A-2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole maleate (BRL44408), α2B-2-[2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione dihydrochloride (ARC239), α2C-JP1302, α2D-2-(2,3-dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride [RX821002])...
April 2017: Dose-response: a Publication of International Hormesis Society
https://www.readbyqxmd.com/read/28454189/assessment-of-the-authenticity-of-herbal-dietary-supplements-comparison-of-chemical-and-dna-barcoding-methods
#11
Rahul S Pawar, Sara M Handy, Raymond Cheng, Nicole Shyong, Erich Grundel
About 7 % of the U. S. population reports using botanical dietary supplements. Increased use of such supplements has led to discussions related to their authenticity and quality. Reports of adulteration with substandard materials or pharmaceuticals are of concern because such substitutions, whether inadvertent or deliberate, may reduce the efficacy of specific botanicals or lead to adverse events. Methods for verifying the identity of botanicals include macroscopic and microscopic examinations, chemical analysis, and DNA-based methods including DNA barcoding...
April 28, 2017: Planta Medica
https://www.readbyqxmd.com/read/28441717/dexmedetomidine-relieves-formaldehyde-induced-pain-in-rats-through-both-%C3%AE-2-adrenoceptor-and-imidazoline-receptor
#12
Hong Zhang, Xiang Yan, De-Gui Wang, Yu-Fang Leng, Zhan-Hai Wan, Yong-Qiang Liu, Yan Zhang
Dexmedetomidine (DEX) is a highly selective α2 adrenergic receptor agonist. In this study, we investigated the analgesic effect and the underlying mechanisms of DEX on inflammatory visceral pain in rats. Twenty-five male Sprague Dawley (SD) rats were randomly divided into 5 groups, including control, sham, low dose DEX, medium dose DEX and high dose DEX group. Pain was induced with 10% formalin and scored every 15min till 2 h-post the induction. Hematoxylin-eosin (HE) staining was used to evaluate the toxicity of DEX on spinal cord neurons...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28432009/the-lateral-hypothalamus-to-lateral-habenula-projection-but-not-the-ventral-pallidum-to-lateral-habenula-projection-regulates-voluntary-ethanol-consumption
#13
Chandni Sheth, Teri M Furlong, Kristen A Keefe, Sharif A Taha
The lateral habenula (LHb) is an epithalamic brain region implicated in aversive processing via negative modulation of midbrain dopamine (DA) and serotonin (5-HT) systems. Given the role of the LHb in inhibiting DA and 5-HT systems, it is thought to be involved in various psychiatric pathologies, including drug addiction. In support, it has been shown that LHb plays a critical role in cocaine- and ethanol-related behaviors, most likely by mediating drug-induced aversive conditioning. In our previous work, we showed that LHb lesions increased voluntary ethanol consumption and operant ethanol self-administration and blocked yohimbine-induced reinstatement of ethanol self-administration...
April 19, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28427990/neuropeptide-y-not-involved-in-cutaneous-vascular-control-in-young-human-females-taking-oral-contraceptive-hormones
#14
Gary J Hodges, Zachary T Martin, Andrew T Del Pozzi
We previously reported that the cutaneous vasodilator response to local warming in males required noradrenaline (NA) and neuropeptide-Y (NPY). Animal work has shown no role for NPY in female vascular control. We investigated the contribution of NA and NPY in human female cutaneous vascular control. Nine female and nine male participants volunteered. To elucidate whether synthetic oestrogen and progesterone altered cutaneous vascular responses, females were tested in high-hormone (HH) and low-hormone (LH) phases of oral contraceptive pill (OCP)...
April 18, 2017: Microvascular Research
https://www.readbyqxmd.com/read/28409566/combined-effects-of-glucocorticoid-and-noradrenergic-activity-on-loss-aversion
#15
Zsofia Margittai, Gideon Nave, Marijn Van Wingerden, Alfons Schnitzler, Lars Schwabe, Tobias Kalenscher
Loss aversion is a well-known behavioral regularity in financial decision-making, describing humans' tendency to overweigh losses compared to gains of the same amount. Recent research indicates that stress and associated hormonal changes affect loss aversion, yet the underlying neuroendocrine mechanisms are still poorly understood. Here, we investigated the causal influence of two major stress neuromodulators, cortisol and noradrenaline, on loss aversion during financial decision-making. In a double-blind, placebo-controlled between subject design, we orally administered either the α2-adrenergic antagonist yohimbine (increasing noradrenergic stimulation), hydrocortisone, both substances, or a placebo to healthy young men...
April 14, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28385635/effect-of-diazepam-and-yohimbine-on-neuronal-activity-in-sham-and-hemiparkinsonian-rats
#16
Katherine A O'Connor, Emily Mahoney, Adolfo Ramirez-Zamora, Eric S Molho, Julie G Pilitsis, Damian S Shin
The prefrontal cortex and the amygdala are critical for the emotional guidance of behavior and are believed to be a site of action for many anxiolytics and anxiogenics. Despite extensive studies examining how these drugs affect behavior, there is little information regarding their effects on neuronal activity. Additionally, with recent recognition of anxiety as a non-motor symptom of Parkinson's disease, it is unknown if activity in the cortex and the amygdala is altered. Previously, we reported that hemiparkinsonian rats had higher baseline anxiety-like behavior and diminished responsiveness to the acute anxiolytic, diazepam...
April 4, 2017: Neuroscience
https://www.readbyqxmd.com/read/28379112/comparison-of-two-sedation-protocols-for-short-electroretinography-in-cats
#17
María J Del Sole, Pablo Nejamkin, Verónica Cavilla, Paula Schaiquevich, Laura Moreno
Objectives The objectives were to compare two different sedative combinations, xylazine-ketamine and dexmedetomidine-ketamine, on the short electroretinography (ERG) protocol and their impact on sedative effect, reversal times and physiological variables in cats. Methods Six healthy spayed female domestic cats were sedated using one of two ketamine-containing protocols: intramuscular xylazine hydrochloride (1 mg/kg) plus ketamine hydrochloride (3 mg/kg) (XK), and dexmedetomidine hydrochloride (5 µg/kg) plus ketamine hydrochloride (3 mg/kg) (DK)...
April 1, 2017: Journal of Feline Medicine and Surgery
https://www.readbyqxmd.com/read/28369032/bidirectional-regulatory-effects-of-dexmedetomidine-on-porcine-coronary-tone-in-vitro
#18
Shu-Zhi Zhou, Zhi-Ming Li, Xue-Ru Liu, Jun Zhou, Xiao-Qiu Tan, Yan Yang, Ji-Cheng Wei
BACKGROUND Studies in vivo have shown that dexmedetomidine (DEX) could protect the myocardium and modulate the coronary blood flow. This study aimed to investigate the direct and concentration-dependent effects of DEX on the tone of porcine coronary artery in vitro and the underlying mechanisms. MATERIAL AND METHODS Distal branches of the porcine anterior descending coronary arteries were dissected and cut into 3-5 mm rings. The tones of coronary rings in response to cumulative DEX were measured using the PowerLab system...
April 3, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28362179/serotonin-induced-hypophagia-is-mediated-via-%C3%AE-2-and-%C3%AE-2-adrenergic-receptors-in-neonatal-layer-type-chickens
#19
M Zendehdel, F Sardari, S Hassanpour, M Rahnema, A Adeli, E Ghashghayi
1. Serotoninergic and adrenergic systems play crucial roles in feed intake regulation in avians but there is no report on possible interactions among them. So, in this study, 5 experiments were designed to evaluate the interaction of central serotonergic and adrenergic systems on food intake regulation in 3 h food deprived (FD3) neonatal layer-type chickens. 2. In Experiment 1, chickens received intracerebroventricular (ICV) injection of control solution, serotonin (56.74 nmol), prazosin (α1 receptor antagonist, 10 nmol) and co-injection of serotonin plus prazosin...
March 31, 2017: British Poultry Science
https://www.readbyqxmd.com/read/28344096/dissociable-effects-of-systemic-and-orbitofrontal-administration-of-adrenoceptor-antagonists-on-yohimbine-induced-motor-impulsivity
#20
Wendy K Adams, Michael M Barrus, Fiona D Zeeb, Paul J Cocker, James Benoit, Catharine A Winstanley
The α2-adrenoceptor antagonist, yohimbine, is commonly used as a pharmacological stressor. Its behavioural effects are typically attributed to elevated noradrenaline release via blockade of central, inhibitory autoreceptors. We have previously reported that yohimbine increases motor impulsivity in rats on the five-choice serial reaction time task (5CSRTT), a cognitive behavioural assessment which measures motor impulsivity and visuospatial attention. Furthermore, this effect depended on cyclic adenomonophosphate (cAMP) signalling via cAMP response element binding (CREB) protein in the orbitofrontal cortex (OFC)...
March 23, 2017: Behavioural Brain Research
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