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Preeti Singh, Pranshu Sharma, Udayraj P Nakade, Abhishek Sharma, Manju Gari, Soumen Choudhury, Amit Shukla, Satish Kumar Garg
BACKGROUND: Endocannabinoids level are reported to increase in sepsis, however, the role of vascular cannabinoid receptor-1 (CB1R) in sepsis-induced vascular hyporeactivity is yet to be unravelled. METHODS: Polymicrobial sepsis was induced by caecal ligation and puncture in mice. Isometric tension in isolated aortic rings during early (6 h) and late (20 h) phases of sepsis was recorded and expression of mRNA of monoacylglycerol lipase (MAGL) and cannabinoid receptor-1 (CB1R) was investigated...
July 19, 2018: Pharmacological Reports: PR
Sherrica Tai, Tamara Vasiljevik, Alexander M Sherwood, Sarah Eddington, Catheryn D Wilson, Thomas E Prisinzano, William E Fantegrossi
BACKGROUND: Cannabinoids may be useful in the treatment of CNS disorders including drug abuse and addiction, where both CB1R antagonists / inverse agonists and CB2R agonists have shown preclinical efficacy. TV-5-249 and TV-6-41, two novel aminoalkylindoles with dual action as neutral CB1R antagonists and CB2R agonists, previously attenuated abuse-related effects of ethanol in mice. PURPOSE: To further characterize these drugs, TV-5-249 and TV-6-41 were compared with the CB1R antagonist / inverse agonist rimonabant in assays relevant to adverse effects and cannabinoid withdrawal...
September 25, 2018: Drug and Alcohol Dependence
Heikki Laurikainen, Lauri Tuominen, Maria Tikka, Harri Merisaari, Reetta-Liina Armio, Elina Sormunen, Faith Borgan, Mattia Veronese, Oliver Howes, Merja Haaparanta-Solin, Olof Solin, Jarmo Hietala
The endocannabinoid system (ECS) has a widespread neuromodulatory function in the central nervous system and is involved in important aspects of brain function including brain development, cortical rhythms, plasticity, reward, and stress sensitivity. Many of these effects are mediated via the cannabinoid CB1 receptor (CB1R) subtype. Animal studies convincingly show an interaction between the ECS and sex hormones, as well as a sex difference of higher brain CB1R in males. Human in vivo studies of sex difference have yielded discrepant findings...
October 5, 2018: NeuroImage
Miguel Ángel Luján, Adriana Castro-Zavala, Laia Alegre-Zurano, Olga Valverde
Cannabinoid derivatives have shown promising results for treating neuropsychiatric disorders, including drug addiction. Recent studies on the therapeutic effects of Cannabidiol (CBD) on drug abuse showed mixed results, especially with psychostimulant substances such as cocaine. To determine whether CBD can attenuate cocaine reinforcement, we assessed behavioural responses induced by cocaine in mice, using the behavioural sensitization, conditioned place preference and intravenous self-administration paradigms...
September 28, 2018: Neuropharmacology
Alqassem Y Hakami, Fahad S Alshehri, Youssef Sari
Studies on cannabinoids have reported contradictory findings, showing both aversion and rewarding outcomes in conditioned place preference (CPP). Various possibilities have been suggested to explain the aversive properties of cannabinoids, including the pharmacokinetics profile and dose selection. In this study, we have established a CPP method to investigate the effects of modulating astroglial glutamate transporters in cannabinoid dependence using a cannabinoid receptor 1 (CB1R) agonist, CP 55,940 (CP). Previous reports using CPP paradigm demonstrated the involvement of glutamatergic system in seeking behavior of several drugs of abuse such as cocaine, heroin and nicotine...
September 23, 2018: Behavioural Brain Research
Jian-Zhong Chen, Hai-Yan Qian, Zhi-Long Wang, Li-Li Chen, You-Lu Pan, Xiao-Yu Xie, Xin Xie
In this paper, we described the design and synthesis of new series of heteroarylpyrimidine/ heteroaryltriazine derivatives on the basis of quinazoline-2,4(1H,3H)-diones to be CB2R-selective ligands using a bioisosterism strategy. In the meantime, acetamide group was applied to displace the enamine linker of the lead for the purpose of stereoisomerism elimination and hydrophilicity increase. As results, some of synthesized compounds showed high bioactivity and selectivity for CB2R in calcium mobilization assays, and four of them displayed CB2R agonist activity with EC50 values below 30 nM...
September 24, 2018: ChemMedChem
Ana María Cruz-Martínez, Juan Gabriel Tejas-Juárez, Juan Manuel Mancilla-Díaz, Benjamín Florán-Garduño, Verónica Elsa López-Alonso, Rodrigo Erick Escartín-Pérez
Endocannabinoids and their receptors not only contribute to the control of natural processes of appetite regulation and energy balance but also have an important role in the pathogenesis of obesity. CB1 receptors (CB1R) are expressed in several hypothalamic nuclei, including the paraventricular nucleus (PVN), where induce potent orexigenic responses. Activation of CB1R in the PVN induces hyperphagia by modulating directly or indirectly orexigenic and anorexigenic signals; however, interaction among these mediators has not been clearly defined...
September 11, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Cristina Siller-Pérez, Antonio Fuentes-Ibañez, Erika L Sotelo-Barrera, Norma Serafín, Roberto A Prado-Alcalá, Patrizia Campolongo, Benno Roozendaal, Gina L Quirarte
The endocannabinoid (eCB) system is highly stress sensitive and known to modulate memory formation of emotionally arousing experiences across different corticolimbic structures. eCB signaling within these circuits is also essentially involved in regulating non-genomically mediated glucocorticoid hormone effects on memory. It has long been thought that the dorsal striatum, which plays a major role in procedural memory and habit formation, is considerably less impacted by stressful experiences; however, recent findings indicate that stress and glucocorticoids also affect striatal-dependent memory processes...
August 30, 2018: Psychoneuroendocrinology
F Barutta, S Bellini, R Mastrocola, R Gambino, F Piscitelli, V di Marzo, B Corbetta, K Vemuri, A Makriyannis, L Annaratone, G Bruno, G Gruden
BACKGROUND AND PURPOSE: The endocannabinoid (EC) system has been implicated in the pathogenesis of diabetic nephropathy (DN). We investigated the effects of peripheral blockade of the endocannabinoid receptor of type 1 (CB1R) as add-on treatment to ACE-inhibition in type 1 diabetic (DM) mice with established albuminuria. EXPERIMENTAL APPROACH: Renal functional parameters (albumin excretion rate, creatinine clearance), tubular injury, renal structure, both EC and EC receptor levels, and markers of podocyte dysfunction, fibrosis and inflammation were studied in streptozotocin-induced DM mice treated for 14 weeks with vehicle, the ACE-inhibitor perindopril (2 mg/Kg/die), the peripheral restricted CB1R antagonist AM6545 (10 mg/Kg/die) or both...
September 5, 2018: British Journal of Pharmacology
Gaëtan Philippot, Stefan Hallgren, Torsten Gordh, Anders Fredriksson, Robert Fredriksson, Henrik Viberg
Acetaminophen (AAP; also known as paracetamol) is the most used and only recommended analgesic and antipyretic among pregnant women and young children. However, recent findings in both humans and rodents suggest a link between developmental exposure to AAP and adverse neurobehavioral effects later in life. We hypothesized that the cannabinoid receptor type 1 (CB1R) may be involved in the developmental neurotoxicity of AAP, owing to its interaction with the endocannabinoid system. Here we test if CB1R agonist WIN 55 212-2 (WIN) and AAP can interact when exposure occurs during a neurodevelopmental stage known for increased growth rate and for its vulnerability to AAP exposure...
August 25, 2018: Toxicological Sciences: An Official Journal of the Society of Toxicology
Yinghua Yu, Craig Patch, Katrina Weston-Green, Yuan Zhou, Kuiyang Zheng, Xu-Feng Huang
SCOPE: A high-fat, but low-fiber, diet is associated with obesity and cognitive dysfunction, while dietary fiber supplementation can improve cognition. METHODS AND RESULTS: This study examines whether dietary fibers, galacto-oligosaccharides (GOS) and resistant starch (RS), could prevent high-fat (HF)-diet-induced alterations in neurotransmitter receptor densities in brain regions associated with cognition and appetite. Rats are fed a HF diet, HF diet with GOS, HF diet with RS, or a low-fat (LF, control) diet for 4 weeks...
August 27, 2018: Molecular Nutrition & Food Research
Maria E Secci, Paola Mascia, Claudia Sagheddu, Sarah Beggiato, Miriam Melis, Andrea C Borelli, Maria C Tomasini, Leigh V Panlilio, Charles W Schindler, Gianluigi Tanda, Sergi Ferré, Charles W Bradberry, Luca Ferraro, Marco Pistis, Steven R Goldberg, Robert Schwarcz, Zuzana Justinova
The reinforcing effects of Δ9 -tetrahydrocannabinol (THC) in rats and monkeys, and the reinforcement-related dopamine-releasing effects of THC in rats, can be attenuated by increasing endogenous levels of kynurenic acid (KYNA) through systemic administration of the kynurenine 3-monooxygenase inhibitor, Ro 61-8048. KYNA is a negative allosteric modulator of α7 nicotinic acetylcholine receptors (α7nAChRs) and is synthesized and released by astroglia, which express functional α7nAChRs and cannabinoid CB1 receptors (CB1Rs)...
August 27, 2018: Molecular Neurobiology
Vikram Joshi, Shivakumar Subbanna, Madhu Shivakumar, Balapal S Basavarajappa
Fetal alcohol spectrum disorders (FASD) represent a wide array of defects that arise from ethanol exposure during development. However, the underlying molecular mechanisms are limited. In the current report, we aimed to further evaluate the cannabinoid receptor type 1 (CB1R)-mediated mechanisms in a postnatal ethanol-exposed animal model. We report that the exposure of postnatal day 7 (P7) mice to ethanol generates p25, a CDK5-activating peptide, in a time- and CB1R-dependent manner in the hippocampus and neocortex brain regions...
August 22, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
Victoria S Cavener, Andrew Gaulden, Dante Pennipede, Puja Jagasia, Jashim Uddin, Lawrence J Marnett, Sachin Patel
Elucidating the underlying molecular mechanisms regulating fear and extinction learning may offer insights that can lead to novel treatments for debilitating anxiety and trauma-related disorders including posttraumatic stress disorder. The endocannabinoid (eCB) system is a retrograde inhibitory signaling pathway involved in regulating central responses to stress. The eCB 2-arachidonoylglycerol (2-AG) has recently been proposed to serve as a homeostatic signal mitigating adverse effects of stress exposure, however, less well understood is 2-AG's role in fear learning and fear extinction...
2018: Frontiers in Neuroscience
Roberta Imperatore, Livia D'Angelo, Omid Safari, Hamidreza Ahmadniaye Motlagh, Fabiana Piscitelli, Paolo de Girolamo, Luigia Cristino, Ettore Varricchio, Vincenzo di Marzo, Marina Paolucci
Hypocretins/Orexins neuropeptides are known to regulate numerous physiological functions, such as energy homeostasis, food intake, sleep/wake cycle, arousal and wakefulness, in vertebrates. Previous studies on mice have revealed an intriguing orexins/endocannabinoids (ECs) signaling interaction at both structural and functional levels, with OX-A behaving as a strong enhancer of 2-arachydonoyl-glycerol (2-AG) biosynthesis. In this study, we describe, for the first time in the brain of zebrafish, the anatomical distribution and co-expression of orexin (OX-2R) and endocannabinoid (CB1R) receptors, suggesting a functional interaction...
2018: Frontiers in Neuroanatomy
Ryan R Wyrofsky, Beverly A S Reyes, Daohai Yu, Lynn G Kirby, Elisabeth J Van Bockstaele
Cannabinoids are capable of modulating mood, arousal, cognition and behavior, in part via their effects on the noradrenergic nucleus locus coeruleus (LC). Dysregulation of LC signaling and norepinephrine (NE) efflux in the medial prefrontal cortex (mPFC) can lead to the development of psychiatric disorders, and CB1r deletion results in alterations of α2- and β1-adrenoceptors in the mPFC, suggestive of increased LC activity. To determine how CB1r deletion alters LC signaling, whole-cell patch-clamp electrophysiology was conducted in LC-NE neurons of male and female wild type (WT) and CB1r-knock out (KO) mice...
September 2018: European Journal of Neuroscience
Margherita Brindisi, Giuseppe Borrelli, Simone Brogi, Alessandro Grillo, Samuele Maramai, Marco Paolino, Mascia Benedusi, Alessandra Pecorelli, Giuseppe Valacchi, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Marco Allarà, Alessia Ligresti, Patrizia Minetti, Giuseppe Campiani, Vincenzo di Marzo, Stefania Butini, Sandra Gemma
The unique role of fatty acid amide hydrolase (FAAH) in terminating endocannabinoid (EC) signaling supports its relevance as a therapeutic target. Inhibition of EC metabolizing enzymes elicits indirect agonism of cannabinoid receptors (CBRs) and therapeutic efficacy devoid of psychotropic effects. Based on our previous ligands, and aiming at the discovery of new selective FAAH inhibitors, we developed a series of 12 new compounds characterized by functionalized tricyclic scaffolds. All the developed compounds display negligible activity on monoacylglycerol lipase (MAGL) and CBRs...
August 7, 2018: ChemMedChem
Shivakumar Subbanna, Vikram Joshi, Balapal S Basavarajappa
Postnatal ethanol exposure has been shown to cause persistent defects in hippocampal synaptic plasticity and disrupt learning and memory processes. However, the mechanisms responsible for these abnormalities are less well studied. We evaluated the influence of postnatal ethanol exposure on several signaling and epigenetic changes and on expression of the activity-regulated cytoskeletal (Arc) protein in the hippocampus of adult offspring under baseline conditions and after a Y-maze spatial memory (SP) behavior (activity)...
July 20, 2018: Neuroscience
Brenda Sbarski, Irit Akirav
Chronic direct activation of cannabinoid CB1 receptors (CB1r) may lead to downregulation of CB1r which may in turn result in a depression-like phenotype in certain individuals. We examined the effects of chronic cannabinoid receptor activation before exposure to an emotional traumatic event on CB1r expression in the basolateral amygdala (BLA) and CA1 and on protracted anxiety- and depression-like behaviors. We used exposure to severe shock and situational reminders (SRs) in an inhibitory apparatus as a model for emotional trauma...
August 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
Rodolfo Sánchez-Zavaleta, Hernán Cortés, José Arturo Avalos-Fuentes, Ubaldo García, José Segovia Vila, David Erlij, Benjamín Florán
Recent studies suggested the expression of CB2 receptors in neurons of the CNS, however, most of these studies have only explored one aspect of the receptors, i.e., expression of protein, messenger RNA, or functional response, and more complete studies appear to be needed to establish adequately their role in the neuronal function. Electron microscopy studies showed the presence of CB2r in asymmetric terminals of the substantia nigra pars reticulata (SNr), and its mRNA appeared is expressed in the subthalamic nucleus...
November 2018: Synapse
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