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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
Xiaowei Xiang, Bing Shang, Xiaozheng Wang, Qinhua Chen
Yohimbine is a novel compounds for 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 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
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
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
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
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
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
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
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
Lidan Nong, Jue Ma, Guangyan Zhang, Chunyu Deng, Songsong Mao, Haifeng Li, Jianxiu Cui
Despite the complex vascular effects of dexmedetomidine (DEX), its actions on human pulmonary resistance arteries remain unknown. The present study tested the hypothesis that DEX inhibits vascular tension in human pulmonary arteries through the endothelial nitric oxide synthase (eNOS) mediated production of nitric oxide (NO). Pulmonary artery segments were obtained from 62 patients who underwent lung resection. The direct effects of DEX on human pulmonary artery tension and changes in vascular tension were determined by isometric force measurements recorded on a myograph...
September 2016: Korean Journal of Physiology & Pharmacology
Lucie Gerber, Frank B Jensen, Steffen S Madsen, William S Marshall
Nitric oxide (NO) modulates epithelial ion transport pathways in mammals, but this remains largely unexamined in fish. We explored the involvement of NO in controlling NaCl secretion by the opercular epithelium of seawater killifish using an Ussing chamber approach. Pharmacological agents were used to explore the mechanism(s) triggering NO action. A modified Biotin-switch technique was used to investigate S-nitrosation of proteins. Stimulation of endogenous NO production via the nitric oxide synthase (NOS) substrate L-arginine (2...
September 2, 2016: Journal of Experimental Biology
J R Smethells, N E Zlebnik, D K Miller, M J Will, F Booth, M E Carroll
BACKGROUND: Previous research has found that rats behaviorally screened for high (vs. low) wheel running were more vulnerable to cocaine abuse. To assess the extent to which a genetic component is involved in this drug-abuse vulnerability, rats selectively bred for high or low voluntary running (HVR or LVR, respectively) were examined for differences in cocaine seeking in the present study. METHODS: Female rats were trained to lever press for food and then were assessed for differences in acquisition of cocaine (0...
October 1, 2016: Drug and Alcohol Dependence
Brooke E Schmeichel, Melissa A Herman, Marisa Roberto, George F Koob
BACKGROUND: Cocaine addiction is characterized by patterns of compulsive drug-taking, including preoccupation with obtaining cocaine and loss of control over drug intake. The lateral hypothalamic hypocretin/orexin (HCRT) system has been implicated in drug-taking and the reinstatement of drug-seeking. Evidence suggests that HCRT may drive drug-seeking through activation of specific brain regions implicated in stress system dysfunction, including the central amygdala (CeA). The role of HCRT in the persistence of compulsive-like cocaine-taking has yet to be fully elucidated...
June 16, 2016: Biological Psychiatry
Majken B Thomsen, Thea P Lillethorup, Steen Jakobsen, Erik H Nielsen, Mette Simonsen, Gregers Wegener, Anne M Landau, R Andrew Tasker
RATIONALE: Epilepsy is a debilitating seizure disorder that affects approximately 50 million people. Noradrenaline reduces neuronal excitability, has anticonvulsant effects and is protective against seizure onset. OBJECTIVE: We investigated the role of α2-adrenoceptors in vivo in a neonatal domoic acid (DOM) rat model of epilepsy. METHODS: We injected male Sprague-Dawley rats daily from postnatal day 8-14 with saline or one of two sub-convulsive doses, 20 μg/kg (DOM20) or 60 μg/kg (DOM60) DOM, an AMPA/kainate receptor agonist...
October 2016: Psychopharmacology
Chandni Sheth, Teri M Furlong, Kristen A Keefe, Sharif A Taha
RATIONALE: Ethanol has rewarding and aversive properties, and the balance of these properties influences voluntary ethanol consumption. Preclinical and clinical evidence show that the aversive properties of ethanol limit intake. The neural circuits underlying ethanol-induced aversion learning are not fully understood. We have previously shown that the lateral habenula (LHb), a region critical for aversive conditioning, plays an important role in ethanol-directed behaviors. However, the neurocircuitry through which LHb exerts its actions is unknown...
October 2016: Psychopharmacology
Sumera Sajjad, Sadia Tobassum, Umer Farooq, Husna Malik, Musadiq İdris
BACKGROUND/AIM: To assess the therapeutic effects of naloxone and yohimbine on polycystic ovary syndrome (PCOS) in a rabbit model in terms of body weight and endocrinological parameters (luteinizing hormone, insulin, and estradiol). MATERIALS AND METHODS: A total of 50 adult, reproductively mature female rabbits (Oryctolagus cuniculus) were divided into five groups (n = 10/group). In the control group PCOS was not induced (negative control group), whereas in the remaining four groups (n = 40) PCOS was induced with a single i...
2016: Turkish Journal of Medical Sciences
Megan K Mahoney, John H Barnes, David Wiercigroch, Mary C Olmstead
Both impulsivity and stress are risk factors for substance abuse, but it is not clear how these two processes interact to alter susceptibility for the disorder. The aim of this project was to examine the pharmacology of a stress-impulsivity interaction in rats. To do so, we tested the effects of yohimbine on impulsive action and then assessed whether behavioural changes could be reduced by antagonists at different receptor subtypes. Male Long-Evans rats were injected with various doses of yohimbine (0-5.0 mg/kg) before testing in the response-inhibition task...
October 2016: Behavioural Pharmacology
Lechi Vo, Sean Hood, Peter D Drummond
: In healthy humans, high-frequency electrical stimulation (HFS) of the forearm not only evokes local signs of central sensitization but also triggers broader ipsilateral inhibitory influences on pain akin to a lateralized form of conditioned pain modulation. Paradoxically, some of these inhibitory influences are augmented by α2-adrenoceptor blockade. To determine whether opioid peptides mediate inhibitory effects after HFS, the opioid receptor antagonist naltrexone was co-administered orally with the α2-adrenoceptor antagonist yohimbine in 16 healthy women in a double-blind placebo-controlled crossover study...
August 4, 2016: Journal of Pain: Official Journal of the American Pain Society
Aliou B Gueye, Yaroslaw Pryslawsky, Jose M Trigo, Nafsika Poulia, Foteini Delis, Katerina Antoniou, Michael Loureiro, Steve R Laviolette, Kiran Vemuri, Alexandros Makriyannis, Bernard Le Foll
BACKGROUND: Multiple studies suggest a pivotal role of the endocannabinoid system in regulating the reinforcing effects of various substances of abuse. Rimonabant, a CB1 inverse agonist found to be effective for smoking cessation, was associated with an increased risk of anxiety and depression. Here we evaluated the effects of the CB1 neutral antagonist AM4113 on the abuse-related effects of nicotine and its effects on anxiety and depressive-like behavior in rats. METHODS: Rats were trained to self-administer nicotine under a fixed-ratio 5 or progressive-ratio schedules of reinforcement...
August 4, 2016: International Journal of Neuropsychopharmacology
Eun Jin Ahn, Geun Joo Choi, Hyun Kang, Chong Wha Baek, Yong Hun Jung, Young Cheol Woo, Si Ra Bang
BACKGROUND: Ginsenoside Rg3 is an extract of total ginseng saponins, which accounts for 4.7% of all saponins. This study aimed to identify the mechanisms of the antinociceptive effects of ginsenoside Rg3. METHODS: Rats were randomly divided into six groups, which were treated with vehicle or 0.5, 1, 1.5, 2, or 4 mg/kg of ginsenoside Rg3 intraperitoneally 2 h after a plantar incision was made. To evaluate the mechanisms of antinociceptive effects, the rats were intraperitoneally injected with naloxone 5 mg/kg, atropine 1 mg/kg, yohimbine 2 mg/kg, mecamylamine 1 mg/kg, prazosin 1 mg/kg, and dexmedetomidine 5 μg/kg...
July 22, 2016: European Surgical Research. Europäische Chirurgische Forschung. Recherches Chirurgicales Européennes
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