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Cannabinoid receptors

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https://www.readbyqxmd.com/read/28343112/the-impact-of-australian-legislative-changes-on-synthetic-cannabinoid-exposures-reported-to-the-new-south-wales-poisons-information-centre
#1
Rose Cairns, Jared A Brown, Naren Gunja, Nicholas A Buckley
BACKGROUND: The emergence of new psychoactive substances (NPS), including synthetic cannabinoid receptor agonists (SCRAs) poses novel challenges for drug regulation and public health. Misconceptions of safety and legality, coupled with the fact that NPS are undetectable on routine drugs screens contributes to their popularity. Concerns over the unpredictable toxicity and abuse potential of NPS has led to a variety of legislative responses worldwide. We wish to describe Australian trends in SCRA use, examining the effects of legislative changes on calls to Australia's largest poisons centre...
March 23, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28341460/cortical-adrenoceptor-expression-function-and-adaptation-under-conditions-of-cannabinoid-receptor-deletion
#2
B A S Reyes, A F Carvalho, P Szot, D J Kalamarides, Q Wang, L G Kirby, E J Van Bockstaele
A neurochemical target at which cannabinoids interact to have global effects on behavior is brain noradrenergic circuitry. Acute and repeated administration of a cannabinoid receptor synthetic agonist is capable of increasing multiple indices of noradrenergic activity. This includes cannabinoid-induced 1) increases in norepinephrine (NE) release in the medial prefrontal cortex (mPFC); 2) desensitization of cortical α2-adrenoceptor-mediated effects; 3) activation of c-Fos in brainstem locus coeruleus (LC) noradrenergic neurons; and 4) increases in anxiety-like behaviors...
March 21, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28339898/the-impact-of-the-psychoactive-substances-act-2016-on-the-online-availability-of-mdmb-chmica
#3
M Haden, D M Wood, P I Dargan
Background: In May 2016, the UK Government enacted the Psychoactive Substances Act which made it an offense to produce or supply many drugs including new psychoactive substances (NPS). Aim: We aimed to assess the impact of the Act on the availability of the synthetic cannabinoid receptor agonist methyl 2-[[1-(cyclohexylmethyl)indole-3-carbonyl]amino]-3,3-dimethylbutanoate (MDMB-CHMICA) from internet-based suppliers. Design: Internet snapshot availability study...
February 28, 2017: QJM: Monthly Journal of the Association of Physicians
https://www.readbyqxmd.com/read/28337258/neuroprotective-effect-of-win55-212-2-against-3-nitropropionic-acid-induced-toxicity-in-the-rat-brain-involvement-of-cb1-and-nmda-receptors
#4
Marisol Maya-López, Ana Laura Colín-González, Gabriela Aguilera, María Eduarda de Lima, Ana Colpo-Ceolin, Edgar Rangel-López, Juana Villeda-Hernández, Daniel Rembao-Bojórquez, Isaac Túnez, Armando Luna-López, Roberto Lazzarini-Lechuga, Viridiana Yazmín González-Puertos, Pedro Posadas-Rodríguez, Alejandro Silva-Palacios, Mina Königsberg, Abel Santamaría
The endocannabinoid system (ECS), and agonists acting on cannabinoid receptors (CBr), are known to regulate several physiological events in the brain, including modulatory actions on excitatory events probably through N-methyl-D-aspartate receptor (NMDAr) activity. Actually, CBr agonists can be neuroprotective. The synthetic CBr agonist WIN55,212-2 acts mainly on CB1 receptor. In turn, the mitochondrial toxin 3-nitropropionic acid (3-NP) produces striatal alterations in rats similar to those observed in the brain of Huntington's disease patients...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28337114/precondition-of-right-frontal-region-with-anodal-tdcs-can-restore-the-fear-memory-impairment-induced-by-acpa-in-male-mice
#5
Fariborz Manteghi, Mohammad Nasehi, Mohammad-Reza Zarrindast
Fear memory and learning cause behavioural patterns such as fight or flight responses, which increase survival probability, but unfit processing of fear memory and learning can lead to maladaptive behaviours and maladies such as phobias, Post-Traumatic Stress Disorder (PTSD) and anxiety disorders. The growing prevalence of these maladies shows the need to quest novel methods for their treatment. We used anodal transcranial direct current stimulation (tDCS) on the right frontal region as a precondition neuromodulator and arachidonylcyclopropylamide (ACPA), a selective CB1 cannabinoid receptor agonist, as a fear memory impairing agent to assess their effects on contextual and auditory fear conditioning (reliable model for fear studies)...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28334603/the-cb1-receptor-as-the-cornerstone-of-exostasis
#6
REVIEW
Pier Vincenzo Piazza, Daniela Cota, Giovanni Marsicano
The type-1 cannabinoid receptor (CB1) is the main effector of the endocannabinoid system (ECS), which is involved in most brain and body functions. In this Perspective, we provide evidence indicating that CB1 receptor functions are key determinants of bodily coordinated exostatic processes. First, we will introduce the concepts of endostasis and exostasis as compensation or accumulation for immediate or future energy needs and discuss how exostasis has been necessary for the survival of species during evolution...
March 22, 2017: Neuron
https://www.readbyqxmd.com/read/28334325/endocannabinoid-dependent-long-term-potentiation-of-synaptic-transmission-at-rat-barrel-cortex
#7
Laura Eva Maglio, José Antonio Noriega-Prieto, Maria Jesús Maraver, David Fernández de Sevilla
Brain-derived neurotrophic factor (BDNF) plays a critical role in modulating plasticity in sensory cortices. Indeed, a BDNF-dependent long-term potentiation (LTP) at distal basal excitatory synapses of Layer 5 pyramidal neurons (L5PNs) has been demonstrated in disinhibited rat barrel cortex slices. Although it is well established that this LTP requires the pairing of excitatory postsynaptic potentials (PSPs) with Ca2+ spikes, its induction when synaptic inhibition is working remains unexplored. Here we show that low-frequency stimulation at basal dendrites of L5PNs is able to trigger a PSP followed by an action potential (AP) and a slow depolarization (termed PSP-Ca2+ response) in thalamocortical slices without blocking synaptic inhibition...
March 1, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/28334226/loss-of-cannabinoid-cb-1-receptors-induces-cortical-migration-malformations-and-increases-seizure-susceptibility
#8
Javier Díaz-Alonso, Adán de Salas-Quiroga, Juan Paraíso-Luna, Daniel García-Rincón, Patricia P Garcez, Maddy Parsons, Clara Andradas, Cristina Sánchez, François Guillemot, Manuel Guzmán, Ismael Galve-Roperh
Neuronal migration is a fundamental process of brain development, and its disruption underlies devastating neurodevelopmental disorders. The transcriptional programs governing this process are relatively well characterized. However, how environmental cues instruct neuronal migration remains poorly understood. Here, we demonstrate that the cannabinoid CB 1 receptor is strictly required for appropriate pyramidal neuron migration in the developing cortex. Acute silencing of the CB 1 receptor alters neuronal morphology and impairs radial migration...
October 5, 2016: Cerebral Cortex
https://www.readbyqxmd.com/read/28331010/presynaptic-and-extrasynaptic-regulation-of-posterior-nucleus-of-thalamus
#9
Anthony Park, Ying Li, Radi Masri, Asaf Keller
The posterior nucleus of thalamus (PO) is a higher-order nucleus involved in sensorimotor processing, including nociception. An important characteristic of PO is its wide range of activity profiles that vary across states of arousal, thought to underlie differences in somatosensory perception subject to attention and degree of consciousness. Further, PO loses the ability to down-regulate its activity level in some forms of chronic pain, suggesting that regulatory mechanisms underlying the normal modulation of PO activity may be pathologically altered...
March 22, 2017: Journal of Neurophysiology
https://www.readbyqxmd.com/read/28327344/direct-activation-of-ca-2-and-voltage-gated-potassium-channels-of-large-conductance-by-anandamide-in-endothelial-cells-does-not-support-the-presence-of-endothelial-atypical-cannabinoid-receptor
#10
Alexander I Bondarenko, Olga Panasiuk, Iryna Okhai, Fabrizio Montecucco, Karim J Brandt, Francois Mach
Endocannabinoid anandamide induces endothelium-dependent relaxation commonly attributed to stimulation of the G-protein coupled endothelial anandamide receptor. The study addressed the receptor-independent effect of anandamide on large conductance Ca(2+)-dependent K(+) channels expressed in endothelial cell line EA.hy926. Under resting conditions, 10µM anandamide did not significantly influence the resting membrane potential. In a Ca(2+)-free solution the cells were depolarized by ~10 mV. Further administration of 10µM anandamide hyperpolarized the cells by ~8 mV...
March 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28326944/fatty-acid-binding-protein-inhibition-produces-analgesic-effects-through-peripheral-and-central-mechanisms
#11
Xiaoxue Peng, Keith Studholme, Martha P Kanjiya, Jennifer Luk, Diane Bogdan, Matthew W Elmes, Gregory Carbonetti, Simon Tong, Yu-Han Gary Teng, Robert C Rizzo, Huilin Li, Dale G Deutsch, Iwao Ojima, Mario J Rebecchi, Michelino Puopolo, Martin Kaczocha
Background Fatty-acid-binding proteins (FABPs) are intracellular carriers for endocannabinoids, N-acylethanolamines, and related lipids. Previous work indicates that systemically administered FABP5 inhibitors produce analgesia in models of inflammatory pain. It is currently not known whether FABP inhibitors exert their effects through peripheral or central mechanisms. Here, we examined FABP5 distribution in dorsal root ganglia and spinal cord and examined the analgesic effects of peripherally and centrally administered FABP5 inhibitors...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28326930/effects-of-jwh015-in-cytokine-secretion-in-primary-human-keratinocytes-and-fibroblasts-and-its-suitability-for-topical-transdermal-delivery
#12
Alicia Bort, Perla A Alvarado-Vazquez, Carolina Moracho-Vilrriales, Kristopher G Virga, Giuseppe Gumina, Alfonso Romero-Sandoval, Scott Asbill
Background JWH015 is a cannabinoid (CB) receptor type 2 agonist that produces immunomodulatory effects. Since skin cells play a key role in inflammatory conditions and tissue repair, we investigated the ability of JWH015 to promote an anti-inflammatory and pro-wound healing phenotype in human primary skin cells. Methods Human primary keratinocytes and fibroblasts were stimulated with lipopolysaccharide. The mRNA expression of cannabinoid receptors was determined using RT-PCR. The effects of JWH015 (0.05, 0...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28325733/overactivation-of-the-endocannabinoid-system-alters-the-anti-lipolytic-action-of-insulin-in-mouse-adipose-tissue
#13
Tania Muller, Laurent Demizieux, Stéphanie Troy-Fioramonti, Joseph Gresti, Jean-Paul Pais de Barros, Hélène Berger, Bruno Vergès, Pascal Degrace
Evidence has accumulated that obesity-related metabolic dysregulation is associated with overactivation of the endocannabinoid system (ECS), which involves cannabinoid receptor 1 (CB1R), in peripheral tissues, including adipose tissue (AT). The functional consequences of CB1R activation on AT metabolism remain unclear. Since excess fat mobilization is considered an important primary event contributing to the onset of insulin resistance, we combined in vivo and in vitro experiments to investigate whether activation of ECS could alter the lipolytic rate...
March 21, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28322830/antidiabetic-antidyslipidemic-and-toxicity-profile-of-env-2-a-potent-pyrazole-derivative-against-diabetes-and-related-diseases
#14
Eduardo Hernández-Vázquez, Hugo Ocampo-Montalban, Litzia Cerón-Romero, Miguel Cruz, Jaime Gomez-Zamudio, Guadalupe Hiriart-Valencia, Rafael Villalobos-Molina, Angelica Flores-Flores, Samuel Estrada-Soto
Diabetes is a major health problem and a predisposition factor for further degenerative complications and, therefore, novel therapies are urgently needed. Currently, cannabinoid receptor 1 (CB1 receptor) antagonists have been considered as promissory entities for metabolic disorders treatment. Accordingly, the purpose of this work was the evaluation of the sub-acute antidiabetic, anti-hyperglycemic, antidyslipidemic and toxicological profile of ENV-2, a potent hypoglycemic and antioxidant CB1 receptor antagonist...
March 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28322749/cannabinoid-receptor-1-contributes-to-sprouted-innervation-in-endometrial-ectopic-growth-through-mitogen-activated-protein-kinase-activation
#15
Hongxiu Han, Xizi Liang, Juan Wang, Qianqian Zhao, Mei Yang, Weifang Rong, Guohua Zhang
The endocannabinoid system regulates neurite outgrowth and neurogenesis during development of the central nervous system. Cannabinoid receptor 1 (CB1R) is expressed in neurons, including the somata and fibers, that innervate the endometrial ectopic cyst in rats. Here, we investigated the contribution of CB1R and its downstream signaling to the innervation of endometrial ectopic growth. We found that intrathecal injection of a CB1R agonist enhanced both the density of protein gene product (PGP) 9.5-immunoreactive sprouted nerve fibers and the protein level of PGP 9...
March 17, 2017: Brain Research
https://www.readbyqxmd.com/read/28320859/2-arachidonoylglycerol-ameliorates-inflammatory-stress-induced-insulin-resistance-in-cardiomyocytes
#16
Dipanjan Chanda, Yvonne Oligschlaeger, Ilvy Geraets, Yilin Liu, Xiaoqing Zhu, Jieyi Li, Miranda Nabben, Will Coumans, Joost J F P Luiken, Jan F C Glatz, Dietbert Neumann
Several studies have linked impaired glucose uptake and insulin resistance (IR) to functional impairment of the heart. Recently, endocannabinoids have been implicated in cardiovascular disease. However, the mechanisms involving endocannabinoid signaling, glucose uptake and IR in cardiomyocytes are understudied. Here, we report the endocannabinoid 2-Arachidonoylglycerol (2-AG) via stimulation of cannabinoid type-1 (CB1) receptor and Ca2+/Calmodulin-dependent protein kinase β (CaMKKβ) activates AMPK leading to increased glucose uptake...
March 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28315677/rimonabant-a-selective-cannabinoid1-receptor-antagonist-protects-against-light-induced-retinal-degeneration-in-vitro-and-in-vivo
#17
Tomoyo Imamura, Kazuhiro Tsuruma, Yuki Inoue, Tomohiro Otsuka, Yuta Ohno, Shiho Ogami, Shinsaku Yamane, Masamitsu Shimazawa, Hideaki Hara
The endocannabinoid system is involved in some neurodegenerative diseases such as Alzheimer's disease. An endogenous constellation of proteins related to cannabinoid1 receptor signaling, including free fatty acids, diacylglycerol lipase, and N-acylethanolamine-hydrolyzing acid amidase, are localized in the murine retina. Moreover, the expression levels of endogenous agonists of cannabinoid receptors are changed in the vitreous fluid. However, the role of the endocannabinoid system in the retina, particularly in the light-induced photoreceptor degeneration, remains unknown...
March 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315398/hepatic-expressions-of-cannabinoid-receptors-cb1-and-cb2-correlate-with-the-fibrogenesis-in-patients-with-chronic-hepatitis-b
#18
Erhei Dai, Lianshan Zhang, Lihong Ye, Shiqing Wan, Lulu Feng, Qi Qi, Fang Yao, Zhen Li
AIM: The endocannabinoid system is involved in the pathogenesis of liver fibrosis. However, most of the findings come from experiment researches on animal model or clinical trial on chronic hepatitis C. The roles of cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2) in hepatofibrosis on patients with chronic hepatitis B(CHB) have not been studied universally. This study aimed to explore the relationship between liver fibrosis and expressions of CB1 and CB2 on patients with CHB...
March 14, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28302862/arresting-the-development-of-addiction-the-role-of-%C3%AE-arrestin2-in-drug-abuse
#19
Kirsten A Porter-Stransky, David Weinshenker
The protein β-arrestin2 (βarr2) directly interacts with receptors and signaling pathways that mediate the behavioral effects of drugs of abuse, making it a prime candidate for therapeutic interventions. βarr2 drives desensitization and internalization of G protein-coupled receptors, including dopamine, opioid, and cannabinoid receptors, and can also trigger G protein-independent intracellular signaling. βarr2 mediates several drug-induced behaviors, but the relationship is complex and dependent on the type of behavior (e...
March 16, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28300292/hdac1-and-hdac3-underlie-dynamic-h3k9-acetylation-during-embryonic-neurogenesis-and-in-schizophrenia-like-animals
#20
Josef Večeřa, Eva Bártová, Jana Krejčí, Soňa Legartová, Denisa Komůrková, Jana Rudá-Kučerová, Tibor Štark, Eva Dražanová, Tomáš Kašpárek, Alexandra Šulcová, Frank J Dekker, Wiktor Szymanski, Christian Seiser, Georg Weitzer, Raphael Mechoulam, Vincenzo Micale, Stanislav Kozubek
Although histone acetylation is one of the most widely studied epigenetic modifications, there is still a lack of information regarding how the acetylome is regulated during brain development and pathophysiological processes. We demonstrate that the embryonic brain (E15) is characterized by an increase in H3K9 acetylation as well as decreases in the levels of HDAC1 and HDAC3. Moreover, experimental induction of H3K9 hyperacetylation led to the overexpression of NCAM in the embryonic cortex and depletion of Sox2 in the subventricular ependyma, which mimicked the differentiation processes...
March 16, 2017: Journal of Cellular Physiology
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