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Serotonin Cannabinoids

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https://www.readbyqxmd.com/read/28660730/fatty-acid-amide-hydrolase-faah-inactivation-confers-enhanced-sensitivity-to-nicotine-induced-dopamine-release-in-the-mouse-nucleus-accumbens
#1
Francisco J Pavon, Antonia Serrano, Nimish Sidhpura, Ilham Polis, David Stouffer, Fernando Rodriguez de Fonseca, Benjamin F Cravatt, Rémi Martin-Fardon, Loren H Parsons
Nicotine exerts its rewarding effects by promoting an increase in dopamine (DA) release in the nucleus accumbens (NAc), and this process is influenced by the endocannabinoid system. Fatty acid amide hydrolase (FAAH) is the main enzyme responsible for the degradation of the endocannabinoid anandamide and other non-cannabinoid N-acylethanolamines. Previous research has reported that both genetic deletion and pharmacological inhibition of FAAH enhance nicotine-induced conditioned place preference at low doses...
June 29, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28625856/nitroglycerin-increases-serotonin-transporter-expression-in-rat-spinal-cord-but-anandamide-modulated-this-effect
#2
Gábor Nagy-Grócz, Zsuzsanna Bohár, Annamária Fejes-Szabó, Klaudia Flóra Laborc, Eleonóra Spekker, Lilla Tar, László Vécsei, Árpád Párdutz
Migraine is one of the most prevalent neurological diseases, which affects 16% of the total population. The exact pathomechanism of this disorder is still not well understood, but it seems that serotonin and its transporter have a crucial role in the pathogenesis. One of the animal models of migraine is the systemic administration of nitroglycerin (NTG), a nitric oxide (NO) donor. NO can initiate a central sensitization process in the trigeminal system, which is also present in migraineurs. Recent studies showed that the endocannabinoid system has a modulatory role on the trigeminal activation and sensitization...
June 15, 2017: Journal of Chemical Neuroanatomy
https://www.readbyqxmd.com/read/28583049/n-arachidonoyl-serotonin-a-dual-faah-and-trpv1-blocker-inhibits-the-retrieval-of-contextual-fear-memory-role-of-the-cannabinoid-cb1-receptor-in-the-dorsal-hippocampus
#3
Pedro H Gobira, Isabel V Lima, Luara A Batista, Antônio C de Oliveira, Leonardo B Resstel, Carsten T Wotjak, Daniele C Aguiar, Fabricio A Moreira
Anandamide, an endocannabinoid, inhibits aversive responses by activating the CB1 cannabinoid receptor. At high concentrations, however, anandamide may exert pro-aversive activities mediated by the transient receptor potential vanilloid type-1 channel (TRPV1). Accordingly, N-arachidonoyl-serotonin (AA-5-HT), a dual blocker of the anandamide-hydrolysing enzyme fatty acid amide hydrolase (FAAH) and the TRPV1 channel, induces anxiolytic-like effects. Here we tested the hypothesis that AA-5-HT inhibits the expression of contextual fear conditioning by facilitating CB1 receptor signalling in the dorsal hippocampus of mice...
June 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28577135/a-review-of-adjunctive-cns-medications-used-for-the-treatment-of-post-surgical-pain
#4
REVIEW
Ajit Rai, Howard Meng, Aliza Weinrib, Marina Englesakis, Dinesh Kumbhare, Liza Grosman-Rimon, Joel Katz, Hance Clarke
Inadequate post-operative pain management can have significant impacts on patients' quality of life. Effective management of acute pain after surgery is important for early mobilization and discharge from hospital, patient satisfaction, and overall well-being. Utilizing multimodal analgesic strategies has become the mainstay of acute post-operative pain management. A comprehensive search was performed, assessing the published or otherwise publically available literature on different central nervous system (CNS) drugs [excluding opioids, non-steroidal anti-inflammatory drugs (NSAIDs), and acetaminophen] and their uses to treat acute post-surgical pain...
July 2017: CNS Drugs
https://www.readbyqxmd.com/read/28539670/simvastatin-and-bezafibrate-ameliorate-emotional-disorder-induced-by-high-fat-diet-in-c57bl-6-mice
#5
Hui Wang, Jia Zhou, Qiong Zhen Liu, Lu Lu Wang, Jing Shang
High fat diet (HFD)-induced metabolic disorders may lead to emotional disorders. This study aimed to explore the effect of simvastatin (SMV) and bezafibrate (BZ) on improving HFD-induced emotional changes, and tried to identify their different mechanisms. The intraperitoneal glucose tolerance test (IPGTT) was used to evaluate glucose control ability; and behavior tests including open field tests (OFT), forced swimming tests (FST), tail suspension tests (TST) and sucrose preference (SPT), were then performed to evaluate emotional changes...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28409931/1-4-18-f-fluorobenzyl-4-tetrahydrofuran-2-yl-methyl-piperazine-a-novel-suitable-radioligand-with-low-lipophilicity-for-imaging-%C3%AF-1-receptors-in-the-brain
#6
Yingfang He, Fang Xie, Jiajun Ye, Winnie Deuther-Conrad, Bixiao Cui, Liang Wang, Jie Lu, Jörg Steinbach, Peter Brust, Yiyun Huang, Jie Lu, Hongmei Jia
We have designed and synthesized novel piperazine compounds with low lipophilicity as σ1 receptor ligands. 1-(4-Fluorobenzyl)-4-[(tetrahydrofuran-2-yl)methyl]piperazine (10) possessed a low nanomolar σ1 receptor affinity and a high selectivity toward the vesicular acetylcholine transporter (>2000-fold), σ2 receptors (52-fold), and adenosine A2A, adrenergic α2, cannabinoid CB1, dopamine D1, D2L, γ-aminobutyric acid A (GABAA), NMDA, melatonin MT1, MT2, and serotonin 5-HT1 receptors. The corresponding radiotracer [(18)F]10 demonstrated high brain uptake and extremely high brain-to-blood ratios in biodistribution studies in mice...
May 25, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28356298/activation-of-cb1-receptors-by-2-arachidonoylglycerol-attenuates-vasoconstriction-induced-by-u46619-and-angiotensin-ii-in-human-and-rat-pulmonary-arteries
#7
Olga Karpińska, Marta Baranowska-Kuczko, Monika Kloza, Ewa Ambrożewicz, Tomasz Kozłowski, Irena Kasacka, Barbara Malinowska, Hanna Kozłowska
Recent evidence suggests that endocannabinoids acting via cannabinoid CB1 receptors may modulate vascular responses of various vasoconstrictors in the rodent systemic vasculature. The aim of the study was to investigate whether endocannabinoids modulate the contractile responses evoked by a thromboxane A2 analog (U46619), angiotensin II (Ang II), serotonin (5-HT) and phenylephrine which stimulate distinct Gq/11-protein coupled receptors (TP, AT1, 5-HT2 and α1-adrenergic) in isolated endothelium-intact human (hPAs) and rat pulmonary arteries (rPAs)...
March 29, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28349316/cannabis-cannabinoids-and-sleep-a-review-of-the-literature
#8
REVIEW
Kimberly A Babson, James Sottile, Danielle Morabito
PURPOSE OF REVIEW: The current review aims to summarize the state of research on cannabis and sleep up to 2014 and to review in detail the literature on cannabis and specific sleep disorders from 2014 to the time of publication. RECENT FINDINGS: Preliminary research into cannabis and insomnia suggests that cannabidiol (CBD) may have therapeutic potential for the treatment of insomnia. Delta-9 tetrahydrocannabinol (THC) may decrease sleep latency but could impair sleep quality long-term...
April 2017: Current Psychiatry Reports
https://www.readbyqxmd.com/read/28282499/non-opioid-medications-for-the-relief-of-chronic-breathlessness-current-evidence
#9
REVIEW
Carlo Barbetta, David C Currow, Miriam J Johnson
To evaluate systematically randomised clinical trials investigating non-opioid medications for the management and treatment of chronic breathlessness. Areas covered: The evidence for the role of benzodiazepines, anxiolytics, selective serotonin re-uptake inhibitors (SSRIs), tricyclic antidepressants, antihistamines, cannabinoids, nebulized furosemide and herbal-based treatments were critically reviewed. Search of the Clinical Trials Registry (Clinicaltrial.gov) identified ongoing studies expected to generate new data in the near future in several classes of non-opioid medications for their net effect on chronic breathlessness...
April 2017: Expert Review of Respiratory Medicine
https://www.readbyqxmd.com/read/28194132/molecular-imaging-markers-to-track-huntington-s-disease-pathology
#10
REVIEW
Heather Wilson, Rosa De Micco, Flavia Niccolini, Marios Politis
Huntington's disease (HD) is a progressive, monogenic dominant neurodegenerative disorder caused by repeat expansion mutation in the huntingtin gene. The accumulation of mutant huntingtin protein, forming intranuclear inclusions, subsequently leads to degeneration of medium spiny neurons in the striatum and cortical areas. Genetic testing can identify HD gene carriers before individuals develop overt cognitive, psychiatric, and chorea symptoms. Thus, HD gene carriers can be studied in premanifest stages to understand and track the evolution of HD pathology...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28144708/differential-effects-of-cannabinoid-cb1-inverse-agonists-and-antagonists-on-impulsivity-in-male-sprague-dawley-rats-identification-of-a-possibly-clinically-relevant-vulnerability-involving-the-serotonin-5ht1a-receptor
#11
Peter J McLaughlin, Julia E Jagielo-Miller, Emily S Plyler, Kerry K Schutte, V Kiran Vemuri, Alexandros Makriyannis
RATIONALE: Cannabinoid CB1 inverse agonists hold therapeutic promise as appetite suppressants but have produced suicidal behaviors among a small subpopulation in clinical trials. Anatomical and pharmacological evidence implicate the 5HT1A serotonin receptor in suicide in humans and impulsivity in humans and animals. OBJECTIVE: The objective of the study is to assess whether 5HT1A blockade is necessary for CB1 ligands to produce impulsivity. METHODS: Sprague Dawley rats were administered the CB1 inverse agonist AM 251, the CB1 antagonist AM 6527, or the peripherally restricted antagonist AM 6545, with or without pretreatment with the 5HT1A antagonist WAY 100,635 (WAY) on the paced fixed consecutive number (FCN) task, which measures choice to terminate a chain of responses prematurely...
March 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28108358/neurochemical-and-metabolic-effects-of-acute-and-chronic-alcohol-in-the-human-brain-studies-with-positron-emission-tomography
#12
REVIEW
Nora D Volkow, Corinde E Wiers, Ehsan Shokri-Kojori, Dardo Tomasi, Gene-Jack Wang, Ruben Baler
The use of Positron emission tomography (PET) to study the effects of acute and chronic alcohol on the human brain has enhanced our understanding of the mechanisms underlying alcohol's rewarding effects, the neuroadaptations from chronic exposure that contribute to tolerance and withdrawal, and the changes in fronto-striatal circuits that lead to loss of control and enhanced motivation to drink that characterize alcohol use disorders (AUD). These include studies showing that alcohol's reinforcing effects may result not only from its enhancement of dopaminergic, GABAergic and opioid signaling but also from its caloric properties...
January 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27938441/a-dual-inhibitor-of-faah-and-trpv1-channels-shows-dose-dependent-effect-on-depression-like-behaviour-in-rats
#13
Christian Kirkedal, Gregers Wegener, Fabricio Moreira, Sâmia Regiane Lourenco Joca, Nico Liebenberg
OBJECTIVE: The cannabinoid receptor 1 (CB1) and transient receptor potential cation channel subfamily V member 1 (TRPV1) are proposed to mediate opposite behavioural responses. Their common denominator is the endocannabinoid ligand anandamide (AEA), which is believed to mediate antidepressant-like effect via CB1-R stimulation and depressive-like effect via TRPV1 activation. This is supposed to explain the bell-shaped dose-response curve for anandamide in preclinical models. METHODS: We investigated this assumption by administering the dual inhibitor of AEA hydrolysis and TRPV1 activation N-arachidonoyl-serotonin (AA-5HT) into the medial prefrontal cortex of rats...
December 12, 2016: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/27805543/descending-serotonergic-and-noradrenergic-systems-do-not-regulate-the-antipruritic-effects-of-cannabinoids
#14
Zeynep Gizem Todurga, Ozgur Gunduz, Cetin Hakan Karadag, Ahmet Ulugol
BACKGROUND: For centuries, cannabinoids have been known to be effective in pain states. Itch and pain are two sensations sharing a lot in common. OBJECTIVE: The goal of this research was to observe whether the cannabinoid agonist WIN 55,212-2 reduces serotonin-induced scratching behaviour and whether neurotoxic destruction of descending serotonergic and noradrenergic pathways mediate the antipruritic effect of WIN 55,212-2. Material and methods Scratching behaviour was induced by intradermal injection of serotonin (50 µg/50 µl/mouse) to Balb/c mice...
December 2016: Acta Neuropsychiatrica
https://www.readbyqxmd.com/read/27746343/revealing-the-role-of-the-endocannabinoid-system-modulators-sr141716a-urb597-and-vdm-11-in-sleep-homeostasis
#15
Eric Murillo-Rodríguez, Sergio Machado, Nuno Barbosa Rocha, Henning Budde, Ti-Fei Yuan, Oscar Arias-Carrión
The endocannabinoid system comprises receptors (CB1 and CB2 cannabinoid receptors), enzymes (Fatty Acid Amide Hydrolase [FAAH], which synthesizes the endocannabinoid anandamide), as well as the anandamide membrane transporter (AMT). Importantly, previous experiments have demonstrated that the endocannabinoid system modulates multiple neurobiological functions, including sleep. For instance, SR141716A (the CB1 cannabinoid receptor antagonist) as well as URB597 (the FAAH inhibitor) increase waking in rats whereas VDM-11 (the blocker of the AMT) enhances sleep in rodents...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27737792/effects-of-alprazolam-and-cannabinoid-related-compounds-in-an-animal-model-of-panic-attack
#16
Luara A Batista, Andrea S Haibara, Luiz C Schenberg, Fabricio A Moreira
Selective stimulation of carotid chemoreceptors by intravenous infusion of low doses of potassium cyanide (KCN) produces short-lasting escape responses that have been proposed as a model of panic attack. In turn, preclinical studies suggest that facilitation of the endocannabinoid system attenuate panic-like responses. Here, we compared the effects of cannabinoid-related compounds to those of alprazolam, a clinically effective panicolytic, on the duration of the escape reaction induced by intravenous infusion of KCN (80μg) in rats...
October 11, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27734824/-cannabinoid-and-cathinone-designer-drugs-the-workings-and-selected-methods-of-analysis
#17
REVIEW
Jadwiga Nędza, Renata Polaniak, Rafał J Bułdak, Milena Majchrzak, Joanna Margasiń-Ska, Marcin Rojkiewicz, Rafał Celiński, Elżbieta Grochowska-Niedworok
Recently, there has been an increase in the consumption of designer drugs, substances aimed at producing psychoactive, energizing, euphoric or anesthetic effects. Designer drugs are substitutes of actual narcotics, whose possession is banned under Polish law according to the Act of 29 July 2005. The latest reports suggest that the number of synthetic psychoactive substances is increasing. In the span of 2012, a total of 28 new synthetic cannabinoids were discovered in member states of the European Union. Synthetic psychoactive substances appear in different forms on the market: tablets (often very colourful and interestingly-shaped), seeds, dried product (sprayed with synthetic substance and redried), crystals or powder...
July 29, 2016: Polski Merkuriusz Lekarski: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/27686024/interaction-between-hippocampal-serotonin-and-cannabinoid-systems-in-reactivity-to-spatial-and-object-novelty-detection
#18
Mohammad Nasehi, Elnaz Rostam-Nezhad, Mohaddeseh Ebrahimi-Ghiri, Mohammad-Reza Zarrindast
Functional interaction between cannabinoid and serotonin neuronal systems have been reported in different tasks related to memory assessment. The present study investigated the effect of serotonin 5-HT4 agents into the dorsal hippocampus (the CA1 region) on spatial and object novelty detection deficits induced by activation of cannabinoid CB1 receptors (CB1Rs) using arachidonylcyclopropylamide (ACPA) in a non-associative behavioral task designed to forecast the ability of rodents to encode spatial and non-spatial relationships between distinct stimuli...
September 26, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27685776/the-false-positive-responses-of-analgesic-drugs-to-the-intradermal-serotonin-and-compound-48-80-induced-scratches-as-an-animal-model-of-itch
#19
Fatih Ilkaya, Ozgur Yesilyurt, Melik Seyrek, Ozgur Gunduz, Tayfun Ide, Ahmet Akar, Ahmet Ulugol, Hasan Guzel, Ahmet Dogrul, Durmus Ucar, Caner Gunaydin
Intradermal injection of pruritogens such as serotonin, histamine and compound 48/80 into the skin and then, the evaluation of the scratching behavior is the commonly used animal model to advance pruritic research and drug development. However, predictive validity of this model is poorly documented. There is a close interaction between itch and pain sensations with regard to mediation through an anatomically and functionally identical neuronal pathway. One approach is whether the existing animal model of itch differentiates itch or pain to show efficacy of clinically effective analgesic drugs as a back translation...
2016: Acta Neurobiologiae Experimentalis
https://www.readbyqxmd.com/read/27544303/anandamide-reverses-depressive-like-behavior-neurochemical-abnormalities-and-oxidative-stress-parameters-in-streptozotocin-diabetic-rats-role-of-cb1-receptors
#20
Helen de Morais, Camila P de Souza, Luisa M da Silva, Daniele M Ferreira, Cristiane Hatsuko Baggio, Ana Carolina Vanvossen, Milene Cristina de Carvalho, José Eduardo da Silva-Santos, Leandro José Bertoglio, Joice M Cunha, Janaina M Zanoveli
The pathophysiology associated with increased prevalence of depression in diabetics is not completely understood, although studies have pointed the endocannabinoid system as a possible target. Then, we aimed to investigate the role of this system in the pathophysiology of depression associated with diabetes. For this, diabetic (DBT) male Wistar rats were intraperitoneally treated with cannabinoid CB1 (AM251, 1mg/kg) or CB2 (AM630, 1mg/kg) receptor antagonists followed by anandamide (AEA, 0.005mg/kg) and then submitted to the forced swimming test (FST)...
October 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
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