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ketamine pharmacology

Andresa H Betti, Camila B Antonio, Thais E T Pompeu, Thaise S Martins, Vivian Herzfeldt, Eveline D Stolz, Carlos A M Fraga, Eliezer Barreiro, François Noël, Stela M K Rates
Aiming to identify new antipsychotic lead-compounds, our group has been working on the design and synthesis of new N-phenylpiperazine derivatives. Here, we characterized LASSBio-1422 as a pharmacological prototype of this chemical series. Adult male Wistar rats and CF1 mice were used for in-vitro and in-vivo assays, respectively. LASSBio-1422 [1 and 5 mg/kg, postoperatively (p.o.)] inhibited apomorphine-induced climbing as well as ketamine-induced hyperlocomotion (1 and 5 mg/kg, p.o.), animal models predictive of efficacy on positive symptoms...
October 13, 2016: Behavioural Pharmacology
Mark Galizio, Brooke April, Melissa Deal, Andrew Hawkey, Danielle Panoz-Brown, Ashley Prichard, Katherine Bruce
The Odor Span Task is an incrementing non-matching-to-sample procedure that permits the study of behavior under the control of multiple stimuli. Rats are exposed to a series of odor stimuli and selection of new stimuli is reinforced. Successful performance thus requires remembering which stimuli have previously been presented during a given session. This procedure has been frequently used in neurobiological studies as a rodent model of working memory; however, only a few studies have examined the effects of drugs on performance in this task...
October 17, 2016: Journal of the Experimental Analysis of Behavior
Maria Jenelyn M Alviar, Tom Hale, Monalisa Dungca
BACKGROUND: This is an updated version of the original Cochrane review published in Issue 12, 2011. Phantom limb pain (PLP) is pain that arises in the missing limb after amputation and can be severe, intractable, and disabling. Various medications have been studied in the treatment of phantom pain. There is currently uncertainty in the optimal pharmacologic management of PLP. OBJECTIVES: This review aimed to summarise the evidence of effectiveness of pharmacologic interventions in treating PLP...
October 14, 2016: Cochrane Database of Systematic Reviews
Yoshiro Tomimatsu, Diana Cash, Motohisa Suzuki, Kazunori Suzuki, Michel Bernanos, Camilla Simmons, Steven C R Williams, Haruhide Kimura
TAK-063 is a selective phosphodiesterase 10A (PDE10A) inhibitor that produces potent antipsychotic-like and pro-cognitive effects at 0.3mg/kg (26% PDE10A occupancy in rats) or higher in rodents through the balanced activation of the direct and indirect pathways of striatal medium spiny neurons (MSNs). In this study, we evaluated the specific binding of TAK-063 using in vitro autoradiography (ARG) and the modulation of brain activity using pharmacological magnetic resonance imaging (phMRI) and electroencephalography (EEG)...
October 8, 2016: Neuroscience
Tony Chung Tung Lo, Stephen Tung Yeung, Sujin Lee, Kira Skavinski, Solomon Liao
OBJECTIVE: Ehlers-Danlos syndrome frequently causes acute and chronic pain because of joint subluxations and dislocations secondary to hypermobility. Current treatments for pain related to Ehlers-Danlos syndrome and central pain syndrome are inadequate. This case report discusses the therapeutic use of ketamine intravenous infusion as an alternative. CASE REPORT: A 27-year-old Caucasian female with a history of Ehlers-Danlos syndrome and spinal cord ischemic myelopathy resulting in central pain syndrome, presented with severe generalized body pain refractory to multiple pharmacological interventions...
2016: Journal of Pain Research
Isabelle Karine da Costa Nunes, Everton Tenório de Souza, Suzana Vanessa S Cardozo, Vinicius de Frias Carvalho, Nelilma Correia Romeiro, Patrícia Machado Rodrigues E Silva, Marco Aurélio Martins, Eliezer J Barreiro, Lídia Moreira Lima
Prior investigations showed that increased levels of cyclic AMP down-regulate lung inflammatory changes, stimulating the interest in phosphodiesterase (PDE)4 as therapeutic target. Here, we described the synthesis, pharmacological profile and docking properties of a novel sulfonamide series (5 and 6a-k) designed as PDE4 inhibitors. Compounds were screened for their selectivity against the four isoforms of human PDE4 using an IMAP fluorescence polarized protocol. The effect on allergen- or LPS-induced lung inflammation and airway hyper-reactivity (AHR) was studied in A/J mice, while the xylazine/ketamine-induced anesthesia test was employed as a behavioral correlate of emesis in rodents...
2016: PloS One
Brian E Driver, Robert F Reardon
Some patients are agitated and unable to tolerate conventional preoxygenation methods, including face mask oxygen or noninvasive positive-pressure ventilation. Sedation with ketamine for preoxygenation, also known as delayed sequence intubation, is a technique that can be used to achieve preoxygenation in this patient population. No complications of delayed sequence intubation have previously been reported. A 60-year-old woman presented with acute hypoxic respiratory failure. Despite application of high-flow oxygen (60 L/min) with a nonrebreather face mask, her oxygen saturation remained at 93%...
September 27, 2016: Annals of Emergency Medicine
Eunyoung Han, Nam Ji Kwon, Ling-Yi Feng, Jih-Heng Li, Heesun Chung
In Asian countries, such as China, Taiwan, and Hong Kong, ketamine (KT) is one of the most prevalent illicit use drugs. KT is regulated by various drug-related laws in many countries, such as Korea, Taiwan, China, U.S.A, Netherlands, UK, Australia, Mexico, and Canada. This review research explored pharmacology and side effects of KT, the illicit use patterns of KT, the analytical methods of KT in biological samples, and the concentrations of KT from abusers and non-abusers. Many side effects of KT have been reported mental and physical problems...
September 12, 2016: Forensic Science International
Baoji Hu, Chengbao Li, Mengzhi Pan, Ming Zhong, Yu Cao, Nannan Zhang, Hongbin Yuan, Hongwei Duan
BACKGROUND: The ideal measures to prevent postoperative catheter-related bladder discomfort (CRBD) remain unestablished. We conducted the systematic review and meta-analysis to clarify the significance of potential interventions. METHODS: We followed the Preferred Reporting Items for Systematic review and Meta-Analysis statement guidelines, and searched databases from MEDLINE, EMBASE, and referred Cochrane Library for randomized clinical trials (RCTs) published before December 2014...
September 2016: Medicine (Baltimore)
Helena M Abelaira, Gislaine Z Réus, Zuleide M Ignácio, Maria Augusta B Dos Santos, Airam B de Moura, Danyela Matos, Júlia P Demo, Júlia B I da Silva, Lucineia G Danielski, Fabricia Petronilho, André F Carvalho, João Quevedo
Studies indicated that mammalian target of rapamycin (mTOR), oxidative stress, and inflammation are involved in the pathophysiology of major depressive disorder (MDD). Ketamine, an N-methyl-D-aspartate (NMDA) receptor antagonist, has been identified as a novel MDD therapy; however, the antidepressant mechanism is not fully understood. In addition, the effects of ketamine after mTOR inhibition have not been fully investigated. In the present study, we examined the behavioral and biochemical effects of ketamine in the prefrontal cortex (PFC), hippocampus, amygdala, and nucleus accumbens after inhibition of mTOR signaling in the PFC...
September 2, 2016: Molecular Neurobiology
Anna Höflich, Andreas Hahn, Martin Küblböck, Georg S Kranz, Thomas Vanicek, Sebastian Ganger, Marie Spies, Christian Windischberger, Siegfried Kasper, Dietmar Winkler, Rupert Lanzenberger
Over the last years, a number of studies have been conducted to clarify the neurobiological correlates of ketamine application. However, comprehensive information regarding the influence of ketamine on cortical activity is still lacking. Using resting-state functional MRI and integrating pharmacokinetic information, a double-blind, randomized, placebo-controlled, crossover study was performed to determine the effects of ketamine on neuronal activation. During a 55 min resting-state fMRI scan, esketamine (Ketanest S(®)) was administered intravenously to 35 healthy volunteers...
August 30, 2016: Brain Structure & Function
A Fodor, B Klausz, B Toth, D Zelena
OBJECTIVE: A disturbance of sensorimotor gating measured by prepulse inhibition of acoustic startle (PPI) is one of the best tests of the schizophrenia-like behavior. Vasopressin was implicated in the development of schizophrenia; therefore, the naturally occurring vasopressin-deficient Brattleboro rat has been suggested to be a reliable non-pharmacological animal model. However, previous studies focusing on PPI deficit did not use proper control and despite clear gender differences in the development of the disorder, the effect of gender has been mostly neglected...
January 2016: Endocrine Regulations
Ashley K Losing, Justin M Jones, Adis Keric, Steven E Briggs, David D Leedahl
Ketamine is a promising alternative agent for pain control that offers benefit to traditional strategies, particularly in the setting of rib fracture. Current pharmacologic therapies have clear adverse effects, and other options may be invasive, cost prohibitive, or marginally effective. We describe three consecutive patients with traumatic injuries including rib fracture for which a ketamine infusion was utilized as part of their pain control strategy.  For each patient, use of a ketamine infusion trended toward reduced opioid requirements with stable pain scores...
July 2016: Bulletin of Emergency and Trauma
Kaundinya Gopinath, Eric Maltbie, Naoko Urushino, Doty Kempf, Leonard Howell
RATIONALE: There is a significant interest in the NMDA-receptor antagonist ketamine due to its efficacy in treating depressive disorders and its induction of psychotic-like symptoms that make it a useful tool for modeling psychosis. Pharmacological MRI in awake nonhuman primates provides a highly translational model for studying the brain network dynamics involved in producing these drug effects. OBJECTIVE: The present study evaluated ketamine-induced changes in functional connectivity (FC) in awake rhesus monkeys...
October 2016: Psychopharmacology
Asya Makhro, Qinghai Tian, Lars Kaestner, Dmitry Kosenkov, Giuseppe Faggian, Max Gassmann, Colin Schwarzwald, Anna Bogdanova
This study focuses on characterization of the cardiac N-methyl D-aspartate receptors (NMDARs) as a target for endogenous and synthetic agonists and antagonists. Using isolated perfused rat hearts, we have shown that intracoronary administration of the NMDAR agonists and antagonists has a pronounced effect on autonomous heart function. Perfusion of rat hearts with autologous blood supplemented with NMDAR agonists was associated with induction of tachycardia, sinus arrhythmia and ischemia occurring within physiological plasma concentration range for glutamate and glycine...
August 10, 2016: Journal of Cardiovascular Pharmacology
Heather Kang, Pojeong Park, Zuner A Bortolotto, Simon D Brandt, Tristan Colestock, Jason Wallach, Graham L Collingridge, David Lodge
To avoid legislation based on chemical structure, research chemicals, frequently used for recreational purposes, are continually being synthesized. N-Ethyl-1,2-diphenylethanamine (ephenidine) is a diarylethylamine that has recently become popular with recreational users searching for dissociative hallucinogenic effects. In the present study, the pharmacological basis of its neural actions has been investigated, initially by assessing its profile in central nervous system receptor binding assays and subsequently in targeted electrophysiological studies...
August 9, 2016: Neuropharmacology
Julius Z Wermelt, Richard K Ellerkmann
Emergence Delirium in children after general anesthesia is a common and self limitating event. Although it might be seen as being harmless it can cause other serious complications and might leave both parents and other caregivers with a negative impression behind. Although the cause may still not be clear, potential predictors can be named: preschool age, the use of fast acting volatile anesthestics, higher preoperative anxiety levels and postoperative pain.A child-focused approach to reduce preoperative anxiety focusing on distraction methods rather than pharmacological sedation may be the key as well as sufficient postoperative pain control and the use of total intravenous anesthesia...
July 2016: Anästhesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie: AINS
Sattar Ostadhadi, Mohammad Ahangari, Vahid Nikoui, Abbas Norouzi-Javidan, Samira Zolfaghari, Farahnaz Jazaeri, Mohsen Chamanara, Reyhaneh Akbarian, Ahmad-Reza Dehpour
Lamotrigine is an anticonvulsant agent that shows clinical antidepressant properties. The aim of the present study was to investigate the involvement of N-methyl-d-aspartate (NMDA) receptors and nitric oxide-cyclic guanosine monophosphate (NO-cGMP) synthesis in possible antidepressant-like effect of lamotrigine in forced swimming test (FST) in mice. Intraperitoneal administration of lamotrigine (10mg/kg) decreased the immobility time in the FST (P<0.01) without any effect on locomotor activity in the open-field test (OFT), while higher dose of lamotrigine (30mg/kg) reduced the immobility time in the FST (P<0...
August 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Gábor Benkovics, Ida Fejős, András Darcsi, Erzsébet Varga, Milo Malanga, Éva Fenyvesi, Tamás Sohajda, Lajos Szente, Szabolcs Béni, Julianna Szemán
Herein we report on the synthesis, characterization and the novel capillary electrophoretic use of octakis-(2,3-di-O-methyl-6-O-carboxymethyl)-γ-cyclodextrin sodium salt (ODMCM). ODMCM is the first single-isomer carboxymethyl-γ-cyclodextrin that is fully methylated on its secondary side and carries ionizable carboxymethyl functions on its primary side. ODMCM was prepared with high isomeric purity through a four-step synthetic procedure. The purity of each intermediate was characterized by appropriate chromatographic methods, while the isomeric purity of the carboxymethylated product was determined by an HPLC method using a CD-Screen-IEC column and by a capillary electrophoretic method using indirect UV detection, as well...
October 7, 2016: Journal of Chromatography. A
Evelyn Hearne, Marie Claire Van Hout
An array of dissociative novel psychoactive substances, including "methoxetamine," "3-MeO-PCP," and "methoxphenidine," have emerged as substitutes for the illicit substance "ketamine." A netographic research methodology aimed to describe online, dissociative novel psychoactive substance users' perceptions of risk, informed knowledge around use, and indigenous harm-reduction practices as advocated within online drug fora, so as to provide credible information which can be used to inform public online health education and drug prevention...
September 2016: Journal of Psychoactive Drugs
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