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ketamine pharmacology

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https://www.readbyqxmd.com/read/28718892/methoxetamine-affects-brain-processing-involved-in-emotional-response-in-rats
#1
M T Zanda, P Fadda, S Antinori, M di Chio, W Fratta, C Chiamulera, L Fattore
BACKGROUND AND PURPOSE: Methoxetamine (MXE) is a novel psychoactive substance that is emerging on the Internet and induces dissociative effects and acute toxicity. Yet, its pharmacological effects are still poorly investigated. EXPERIMENTAL APPROACH: We examined a range of behavioural effects induced by acute intraperitoneal administration of MXE (0.5-5 mg/kg) in rats, and whether it causes rapid neuroadaptive molecular changes. KEY RESULTS: MXE (0...
July 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28701926/glutamate-deregulation-in-ketamine-induced-psychosis-a-potential-role-of-psd95-nmda-receptor-and-pmca-interaction
#2
Malwina Lisek, Bozena Ferenc, Maciej Studzian, Lukasz Pulaski, Feng Guo, Ludmila Zylinska, Tomasz Boczek
Ketamine causes psychotic episodes and is often used as pharmacological model of psychotic-like behavior in animals. There is increasing evidence that molecular mechanism of its action is more complicated than just N-methyl-D-aspartic acid (NMDA) receptor antagonism and involves interaction with the components of calcium homeostatic machinery, in particular plasma membrane calcium pump (PMCA). Therefore, in this study we aimed to characterize brain region-specific effects of ketamine on PMCA activity, interaction with NMDA receptor through postsynaptic density protein 95 (PSD95) scaffolding proteins and glutamate release from nerve endings...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28695335/glutamatergic-system-and-mtor-signaling-pathway-participate-in-the-antidepressant-like-effect-of-inosine-in-the-tail-suspension-test
#3
Filipe Marques Gonçalves, Vivian Binder Neis, Débora Kurrle Rieger, Tanara V Peres, Mark William Lopes, Isabella A Heinrich, Ana Paula Costa, Ana Lúcia S Rodrigues, Manuella P Kaster, Rodrigo Bainy Leal
Glutamatergic system and mTOR signaling pathway have been proposed to be important targets for pharmacological treatment of major depressive disorder. Previous studies have shown that inosine, an endogenous purine, is able to exert a remarkable antidepressant-like effect in mice. Nevertheless, the role of glutamatergic system and mTOR in this effect was not previously determined. This study was designed to investigate the possible modulation of NMDA receptors (NMDAR), AMPA receptors (AMPAR) and mTOR complex 1 (mTORC1) signaling pathway in the inosine anti-immobility effect in the tail suspension test (TST) in mice...
July 10, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28694097/behavioural-pharmacology-of-the-%C3%AE-5-gabaa-receptor-antagonist-s44819-enhancement-and-remediation-of-cognitive-performance-in-preclinical-models
#4
István Gacsályi, Krisztina Móricz, Gábor Gigler, János Wellmann, Katalin Nagy, István Ling, József Barkóczy, József Haller, Jeremy J Lambert, Gábor Szénási, Michael Spedding, Ferenc A Antoni
Previous work has shown that S44819 is a novel GABAA receptor (GABAAR) antagonist, which is selective for extrasynaptic GABAARs incorporating the α5 subunit (α5-GABAARs). The present study reports on the preclinical neuropsychopharmacological profile of S44819. Significantly, no sedative or pro-convulsive side effects of S44819 were found at doses up to 30 mg/kg i.p. Object recognition (OR) memory in intact mice was enhanced by S44819 (0.3 mg/kg p.o.) given before the acquisition trial. Mice treated with phencyclidine for two weeks and tested six days after the cessation of treatment failed to show OR memory...
July 8, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28674271/pharmacological-properties-of-various-anesthetic-protocols-in-10-day-old-neonatal-rats
#5
Atsushi Tsukamoto, Yui Konishi, Takako Kawakami, Chiharu Koibuchi, Reiichiro Sato, Eiichi Kanai, Tomo Inomata
In general, the anesthesia in neonates involves high risk. Although hypothermic anesthesia is recommended in rats up to the age of 7 days, neonatal anesthesia for later periods has not been standardized. The present study investigated the pharmacological properties of conventional anesthetic protocols in 10-day-old SD rats. The rats were anesthetized with four anesthetics: a combination of ketamine and xylazine (K/X); a combination of medetomidine, midazolam, and butorphanol (M/M/B); isoflurane; and sevoflurane...
June 30, 2017: Experimental Animals
https://www.readbyqxmd.com/read/28670835/role-of-the-spinal-trkb-nmda-receptor-link-in-the-bdnf-induced-long-lasting-mechanical-hyperalgesia-in-the-rat-a-behavioural-study
#6
J L Marcos, D Galleguillos, T Pelissier, A Hernández, L Velásquez, L Villanueva, L Constandil
BACKGROUND: Intrathecal/intracisternal BDNF in rodents produces long-lasting hyperalgesia/allodynia, which implies BDNF plays a role in the establishment and maintenance of central sensitization. Both self-regeneration of endogenous BDNF and neuroplastic modifications of spinal NMDA receptors downstream TrkB signalling could be involved in such enduring hyperalgesia. We investigated to what extent BDNF by itself could participate in the generation and maintenance of mechanical hyperalgesia using pharmacological tools...
July 3, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28659769/propofol-sevoflurane-and-ketamine-induce-a-reversible-increase-in-delta-gamma-and-theta-gamma-phase-amplitude-coupling-in-frontal-cortex-of-rat
#7
Dinesh Pal, Brian H Silverstein, Lana Sharba, Duan Li, Viviane S Hambrecht-Wiedbusch, Anthony G Hudetz, George A Mashour
Studies from human and non-human species have demonstrated a breakdown of functional corticocortical connectivity during general anesthesia induced by anesthetics with diverse molecular, neurophysiological, and pharmacological profiles. Recent studies have demonstrated that changes in long-range neural communication, and by corollary, functional connectivity, might be influenced by cross-frequency coupling (CFC) between the phase of slow oscillations and the amplitude of local fast oscillations. Phase-amplitude coupling (PAC) between slow oscillations and alpha rhythm during general anesthesia reveal distinct patterns depending on the anesthetic...
2017: Frontiers in Systems Neuroscience
https://www.readbyqxmd.com/read/28634445/antioxidant-treatment-with-n-acetyl-cysteine-prevents-the-development-of-cognitive-and-social-behavioral-deficits-that-result-from-perinatal-ketamine-treatment
#8
Aarron Phensy, Hasmik E Duzdabanian, Samantha Brewer, Anurag Panjabi, Christopher Driskill, Annuska Berz, George Peng, Sven Kroener
Alterations of the normal redox state can be found in all stages of schizophrenia, suggesting a key role for oxidative stress in the etiology and maintenance of the disease. Pharmacological blockade of N-methyl-D-aspartic acid (NMDA) receptors can disrupt natural antioxidant defense systems and induce schizophrenia-like behaviors in animals and healthy human subjects. Perinatal administration of the NMDA receptor (NMDAR) antagonist ketamine produces persistent behavioral deficits in adult mice which mimic a range of positive, negative, and cognitive symptoms that characterize schizophrenia...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28609318/biochemical-and-pharmacological-characterization-of-a-mice-model-of-complex-regional-pain-syndrome
#9
Vaskar Das, Jeffrey S Kroin, Mario Moric, Asokumar Buvanendran
BACKGROUND AND OBJECTIVES: Complex regional pain syndrome is a challenging disease to treat. Recently, a mouse fracture model of complex regional pain syndrome has been developed that has many signs of the clinical syndrome. However, many aspects of the sensory neuron biochemistry and behavioral and pharmacological characterization of this model remain to be clarified. METHODS: Mice were randomly assigned to fracture/cast or control (naive) groups. Fracture/cast mice underwent a closed distal tibia facture, with hindlimb wrapped in casting tape for 3 weeks...
July 2017: Regional Anesthesia and Pain Medicine
https://www.readbyqxmd.com/read/28597354/pharmacologic-considerations-for-pediatric-sedation-and-anesthesia-outside-the-operating-room-a-review-for-anesthesia-and-non-anesthesia-providers
#10
REVIEW
Narjeet Khurmi, Perene Patel, Molly Kraus, Terrence Trentman
Understanding the pharmacologic options for pediatric sedation outside the operating room will allow practitioners to formulate an ideal anesthetic plan, allaying anxiety and achieving optimal immobilization while ensuring rapid and efficient recovery. The authors identified relevant medical literature by searching PubMed, MEDLINE, Embase, Scopus, Web of Science, and Google Scholar databases for English language publications covering a period from 1984 to 2017. Search terms included pediatric anesthesia, pediatric sedation, non-operating room sedation, sedation safety, and pharmacology...
June 8, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28579941/chronic-ketamine-exposure-causes-white-matter-microstructural-abnormalities-in-adolescent-cynomolgus-monkeys
#11
Qi Li, Lin Shi, Gang Lu, Hong-Luan Yu, Fu-Ki Yeung, Nai-Kei Wong, Lin Sun, Kai Liu, David Yew, Fang Pan, De-Feng Wang, Pak C Sham
Acute and repeated exposures to ketamine mimic aspects of positive, negative, and cognitive symptoms of schizophrenia in humans. Recent studies by our group and others have shown that chronicity of ketamine use may be a key element for establishing a more valid model of cognitive symptoms of schizophrenia. However, current understanding on the long-term consequences of ketamine exposure on brain circuits has remained incomplete, particularly with regard to microstructural changes of white matter tracts that underpin the neuropathology of schizophrenia...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28562388/procedural-sedation-in-the-icu-and-emergency-department
#12
Nikhil Chawla, Adjoa Boateng, Ranjit Deshpande
PURPOSE OF REVIEW: Procedures are increasingly being performed in the acute care setting, outside of the operating rooms (OR). This article aims to review the current literature on out-of-OR procedural sedation with a focus on the ICU and emergency department, highlighting the following topics: multidisciplinary team approach, choice of pharmacologic agent, sedation scales, current safety guidelines, anticipating complications, appropriate monitoring and necessary resources. RECENT FINDINGS: Subjective assessment of sedation using sedation scales is controversial...
August 2017: Current Opinion in Anaesthesiology
https://www.readbyqxmd.com/read/28513099/syntheses-analytical-and-pharmacological-characterizations-of-the-legal-high-4-1-3-methoxyphenyl-cyclohexyl-morpholine-3-meo-pcmo-and-analogues
#13
Tristan Colestock, Jason Wallach, Matt Mansi, Nadine Filemban, Hamilton Morris, Simon P Elliott, Folker Westphal, Simon D Brandt, Adeboye Adejare
New psychoactive substances (NPS) are commonly referred to as "research chemicals", "designer drugs" or "legal highs." One NPS class is represented by dissociative anesthetics, which include analogues of the arylcyclohexylamine phencyclidine (PCP), ketamine, and diphenidine. A recent addition to the NPS market was 4-[1-(3-methoxyphenyl)cyclohexyl]morpholine (3-MeO-PCMo), a morpholine analogue of 3-MeO-PCP. Although suspected to have dissociative effects in users, information about its pharmacological profile is not available...
May 16, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28493642/adverse-events-with-ketamine-versus-ketofol-for-procedural-sedation-on-adults-a-double-blind-randomized-controlled-trial
#14
Fabien Lemoel, Julie Contenti, Didier Giolito, Mathieu Boiffier, Jocelyn Rapp, Jacques Istria, Marc Fournier, François-Xavier Ageron, Jacques Levraut
OBJECTIVES: The goal of our study was to compare the frequency and severity of recovery reactions between ketamine and ketamine-propofol 1:1 admixture ("ketofol"). METHODS: We performed a multicentric, randomized, double-blind trial in which adult patients received emergency procedural sedations with ketamine or ketofol. Our primary outcome was the proportion of unpleasant recovery reactions. Other outcomes were frequency of interventions required by these recovery reactions, rates of respiratory or hemodynamic events, emesis, and satisfaction of patients as well as providers...
May 11, 2017: Academic Emergency Medicine: Official Journal of the Society for Academic Emergency Medicine
https://www.readbyqxmd.com/read/28490900/complex-management-of-a-patient-with-refractory-primary-erythromelalgia-lacking-a-scn9a-mutation
#15
Sarah A Low, Wendye Robbins, Vivianne L Tawfik
A 41-year-old woman presented with burning and erythema in her extremities triggered by warmth and activity, which was relieved by applying ice. Extensive workup was consistent with adult-onset primary erythromelalgia (EM). Several pharmacological treatments were tried including local anesthetics, capsaicin, ziconotide, and dantrolene, all providing 24-48 hours of relief followed by symptom flare. Interventional therapies, including peripheral and sympathetic ganglion blocks, also failed. Thus far, clonidine and ketamine have been the only effective agents for our patient...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28482015/a-new-paradigm-for-evaluating-avoidance-escape-motivation
#16
Iku Tsutsui-Kimura, Youcef Bouchekioua, Masaru Mimura, Kenji F Tanaka
Backgrounds: Organisms have evolved to approach pleasurable opportunities and to avoid or escape from aversive experiences. These two distinct motivations are referred to as approach and avoidance/escape motivations and are both considered vital for survival. Despite several recent advances in understanding the neurobiology of motivation, most studies addressed approach but not avoidance/escape motivation. Here we develop a new experimental paradigm to quantify avoidance/escape motivation and examine the pharmacological validity...
May 6, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28481700/pediatric-status-epilepticus-improved-management-with-new-drug-therapies
#17
Alberto Verrotti, Michela Ambrosi, Piero Pavone, Pasquale Striano
Status Epilepticus (SE) is the most common neurological emergency of childhood. It requires prompt administration of appropriately selected anti-seizure medications. Areas covered: Following a distinction between estabilished and emergent drugs, we present pharmacological treatment options and their clinical utility in children, with a short mention on alternatives to drug treatment. We also propose an algorithm for the management of pediatric SE. For this review a Pubmed, Medline and Embase search was performed...
June 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28460699/case-study-of-high-dose-ketamine-for-treatment-of-complex-regional-pain-syndrome-in-the-pediatric-intensive-care-unit
#18
REVIEW
Tracy Ann Pasek, Kelli Crowley, Catherine Campese, Rachel Lauer, Charles Yang
Complex regional pain syndrome (CRPS) is a life-altering and debilitating chronic pain condition. The authors are presenting a case study of a female who received high-dose ketamine for the management of her CRPS. The innovative treatment lies not only within the pharmacologic management of her pain, but also in the fact that she was the first patient to be admitted to our pediatric intensive care unit solely for pain control. The primary component of the pharmacotherapy treatment strategy plan was escalating-dose ketamine infusion via patient-controlled-analgesia approved by the pharmacy and therapeutics committee guided therapy for this patient...
June 2017: Critical Care Nursing Clinics of North America
https://www.readbyqxmd.com/read/28457485/motor-activity-markers-of-circadian-timekeeping-are-related-to-ketamine-s-rapid-antidepressant-properties
#19
Wallace C Duncan, Elizabeth Slonena, Nadia S Hejazi, Nancy Brutsche, Kevin C Yu, Lawrence Park, Elizabeth D Ballard, Carlos A Zarate
BACKGROUND: The rapid clinical antidepressant effects of the glutamatergic modulator ketamine may be due to its ability to restore synaptic plasticity and related effects on sleep-wake and circadian systems. Preclinical studies indicate that ketamine alters expression of circadian clock-associated molecules, and clinical studies of ketamine on plasticity-related biomarkers further suggest an association with sleep slow waves and sleep homeostasis. METHODS: Wrist-activity monitors were used to examine the pharmacologic and rapid antidepressant effects of ketamine on markers of circadian timekeeping (amplitude and timing) in mood disorders...
March 28, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28454981/neuropharmacological-characterization-of-the-new-psychoactive-substance-methoxetamine
#20
Laura Hondebrink, Emma E J Kasteel, Anke M Tukker, Fiona M J Wijnolts, Anouk H A Verboven, Remco H S Westerink
The use of new psychoactive substances (NPS) is steadily increasing. One commonly used NPS is methoxetamine (MXE), a ketamine analogue. Several adverse effects have been reported following MXE exposure, while only limited data are available on its neuropharmacological modes of action. We investigated the effects of MXE and ketamine on several endpoints using multiple in vitro models. These included rat primary cortical cells, human SH-SY5Y cells, human induced pluripotent stem cell (hiPSC)-derived iCell(®) Neurons, DopaNeurons and astrocyte co-cultures, and human embryonic kidney (HEK293) cells...
April 25, 2017: Neuropharmacology
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