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https://www.readbyqxmd.com/read/29145497/rare-genetic-variants-in-the-endocannabinoid-system-genes-cnr1-and-dagla-are-associated-with-neurological-phenotypes-in-humans
#1
Douglas R Smith, Christine M Stanley, Theodore Foss, Richard G Boles, Kevin McKernan
Rare genetic variants in the core endocannabinoid system genes CNR1, CNR2, DAGLA, MGLL and FAAH were identified in molecular testing data from 6,032 patients with a broad spectrum of neurological disorders. The variants were evaluated for association with phenotypes similar to those observed in the orthologous gene knockouts in mice. Heterozygous rare coding variants in CNR1, which encodes the type 1 cannabinoid receptor (CB1), were found to be significantly associated with pain sensitivity (especially migraine), sleep and memory disorders-alone or in combination with anxiety-compared to a set of controls without such CNR1 variants...
2017: PloS One
https://www.readbyqxmd.com/read/29145068/anorexigenic-effects-induced-by-rvd-hemopressin-%C3%AE-administration
#2
Claudio Ferrante, Lucia Recinella, Sheila Leone, Annalisa Chiavaroli, Chiara Di Nisio, Sara Martinotti, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Szabolcs Dvorácskó, Csaba Tömböly, Luciano De Petrocellis, Michele Vacca, Luigi Brunetti, Giustino Orlando
BACKGROUND: Hemopressin, VD-hemopressin(α) and RVD-hemopressin(α) are hemoglobin α chain derived-peptides which have been found in mouse brain, and where they modulate cannabinoid (CB) receptor function. The nonapeptide hemopressin has been reported to inhibit feeding after both central and peripheral administration, possibly playing a role of antagonist/inverse agonist of CB1 receptors, and consequently blocking the orexigenic effects of endogenous cannabinoids. VD-hemopressin(α) and RVD- hemopressin(α), are N-terminal extended forms of hemopressin...
June 3, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29143219/glutamatergic-gabaergic-and-endocannabinoid-neurotransmissions-within-the-dorsal-hippocampus-modulate-the-cardiac-baroreflex-function-in-rats
#3
Nilson Carlos Ferreira-Junior, Davi Campos Lagatta, Leonardo Barbosa Moraes Resstel
The dorsal hippocampus (DH) is involved in the modulation of the cardiac baroreflex function. There is a wide expression of the NMDA and AMPA/Kainate receptors within the DH. Glutamate administration into the DH triggers both tachycardia and pressor responses. Moreover, GABAergic interneurons and endocannabinoid system play an important role in modulation of the activity of glutamatergic neurons within the DH. Therefore, the present work aimed to evaluate the involvement of the glutamatergic, GABAergic, and endocannabinoid neurotransmissions within the DH in cardiac baroreflex function in rats...
November 15, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/29142285/blockade-of-cb1-cannabinoid-receptor-alters-gut-microbiota-and-attenuates-inflammation-and-diet-induced-obesity
#4
Pegah Mehrpouya-Bahrami, Kumaraswamy Naidu Chitrala, Mitra S Ganewatta, Chuanbing Tang, E Angela Murphy, Reilly T Enos, Kandy T Velazquez, Jamie McCellan, Mitzi Nagarkatti, Prakash Nagarkatti
Obesity is characterized by chronic low-grade, systemic inflammation, altered gut microbiota, and gut barrier disruption. Additionally, obesity is associated with increased activity of endocannabinoid system (eCB). However, the clear connection between gut microbiota and the eCB system in the regulation of energy homeostasis and adipose tissue inflammation and metabolism, remains to be established. We investigated the effect of treatment of mice with a cannabinoid receptor 1 (CB1) antagonist on Diet-Induced Obesity (DIO), specifically whether such a treatment that blocks endocannabinoid activity can induce changes in gut microbiota and anti-inflammatory state in adipose tissue...
November 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138877/%C3%AE-9-tetrahydrocannabinol-like-discriminative-stimulus-effects-of-five-novel-synthetic-cannabinoids-in-rats
#5
Michael B Gatch, Michael J Forster
RATIONALE AND OBJECTIVES: Novel synthetic cannabinoid compounds continue to appear in the market advertised as legal alternatives to marijuana and the older synthetic cannabinoid compounds which are now controlled substances. Most of these newer compounds have been found to act at CB1 receptors, so the purpose of this study was to study the abuse liability of these compounds. METHODS: Five of these compounds (BB-22, FUB-PB-22, 5F-AMB, NM2201, and MAB-CHMINACA) were tested for their ability to produce discriminative stimulus effects similar to Δ(9)-tetrahydrocannabinol (Δ(9)-THC) in rats...
November 14, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29134561/cannabinoid-receptor-type-1-agonist-acea-protects-neurons-from-death-and-attenuates-endoplasmic-reticulum-stress-related-apoptotic-pathway-signaling
#6
Talita A Vrechi, Fernanda Crunfli, Andressa P Costa, Andréa S Torrão
Neurodegeneration is the result of progressive destruction of neurons in the central nervous system, with unknown causes and pathological mechanisms not yet fully elucidated. Several factors contribute to neurodegenerative processes, including neuroinflammation, accumulation of neurotoxic factors, and misfolded proteins in the lumen of the endoplasmic reticulum (ER). Endocannabinoid signaling has been pointed out as an important modulatory system in several neurodegeneration-related processes, inhibiting the inflammatory response and increasing neuronal survival...
November 13, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29133950/treating-a-novel-plasticity-defect-rescues-episodic-memory-in-fragile-x-model-mice
#7
W Wang, B M Cox, Y Jia, A A Le, C D Cox, K M Jung, B Hou, D Piomelli, C M Gall, Gary Lynch
Episodic memory, a fundamental component of human cognition, is significantly impaired in autism. We believe we report the first evidence for this problem in the Fmr1-knockout (KO) mouse model of Fragile X syndrome and describe potentially treatable underlying causes. The hippocampus is critical for the formation and use of episodes, with semantic (cue identity) information relayed to the structure via the lateral perforant path (LPP). The unusual form of synaptic plasticity expressed by the LPP (lppLTP) was profoundly impaired in Fmr1-KOs relative to wild-type mice...
November 14, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/29131068/maternal-cannabinoid-use-alters-cannabinoid-cb1-and-endothelin-etb-receptor-expression-in-the-brains-of-dams-but-not-their-offspring
#8
Aarti Amlani, Mary G Hornick, Kevin Cooper, Preetha Prazad, Ramona Donovan, Anil Gulati
According to the 2015 National Survey on Drug Use and Health, cannabis (marijuana) is the most commonly used recreational drug in the US. Among pregnant women aged 14-55 years, 3.4% were cannabis users. Presently, little is known about the neurodevelopmental effect of cannabis use during pregnancy and/or nursing on neonates. Endothelin (ET) is essential for normal development of the central nervous system (CNS). Decreases in ETB receptor expression correlate with a decline in nerve growth factor (NGF) and an increase in vascular endothelial growth factor (VEGF) in postnatal brain...
November 4, 2017: Developmental Neuroscience
https://www.readbyqxmd.com/read/29130941/remote-ischemia-preconditioning-attenuates-blood-spinal-cord-barrier-breakdown-in-rats-undergoing-spinal-cord-ischemia-reperfusion-injury-associated-with-activation-and-upregulation-of-cb1-and-cb2-receptors
#9
Na Jing, Bo Fang, Zhi-Lin Wang, Hong Ma
BACKGROUND/AIMS: Remote ischemic preconditioning (RIPC) has protective effects on spinal cord ischemia reperfusion (I/R) injury, but the potential mechanisms remain unclear. In our study, the effects and underlying mechanisms of RIPC on blood-spinal cord barrier (BSCB) breakdown following I/R injury were investigated. METHODS: animals underwent intraperitoneal administration with cannabinoid-1 (CB1) receptor antagonist AM251, cannabinoid-2 (CB2) receptor antagonist AM630 or vehicle 15 minutes before three 3-minute occlusion-reperfusion cycles on the right femoral artery or a sham operation...
October 31, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29128806/emotional-disorders-induced-by-hemopressin-and-rvd-hemopressin-%C3%AE-administration-in-rats
#10
Sheila Leone, Lucia Recinella, Annalisa Chiavaroli, Sara Martinotti, Claudio Ferrante, Adriano Mollica, Giorgia Macedonio, Azzurra Stefanucci, Szabolcs Dvorácskó, Csaba Tömböly, Luciano De Petrocellis, Michele Vacca, Luigi Brunetti, Giustino Orlando
BACKGROUND: The endocannabinoid (eCB) system plays an important role in regulating emotional disorders, and is involved, directly or indirectly, in psychiatric diseases, such as anxiety and depression. Hemopressin, a hemoglobin α chain-derived peptide, and RVD-hemopressin(α), a N-terminally extended form of hemopressin, act as antagonist/inverse agonist and negative allosteric modulator of the cannabinoid 1 (CB1) receptor, respectively. METHODS: Considering the possible involvement of these peptides on emotional behaviour, the aim of our study was to investigate the behavioural effects of a single intraperitoneal (ip) injection of hemopressin (0...
June 23, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29128791/acpa-and-jwh-133-modulate-the-vascular-tone-of-superior-mesenteric-arteries-through-cannabinoid-receptors-bkca-channels-and-nitric-oxide-dependent-mechanisms
#11
Evelyn López-Dyck, Felipa Andrade-Urzúa, Alejandro Elizalde, Tania Ferrer-Villada, Adan Dagnino-Acosta, Miguel Huerta, Zyanya Osuna-Calleros, Cinthia Rangel-Sandoval, Enrique Sánchez-Pastor
BACKGROUND: Some cannabinoids, a family of compounds derived from Cannabis sativa (marijuana), have previously shown vasodilator effects in several studies, a feature that makes them suitable for the generation of a potential treatment for hypertension. The mechanism underlying this vasodilator effect in arteries is still controversial. In this report, we explored how the synthetic cannabinoids ACPA (CB1-selective agonist) and JWH-133 (CB2-selective agonist) regulate the vascular tone of rat superior mesenteric arteries...
July 1, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29127599/cb1-receptors-mediated-inhibition-of-atp-induced-ca-2-i-increase-in-cultured-rat-spinal-dorsal-horn-neurons
#12
Jingdong Long, Xiaolu Lei, Meiyun Chen, Shulei Yang, Tao Sun, Junwei Zeng, Deqian Yu, Hong Tian, Xiaohong Liu
Spinal cannabinoid receptor 1 (CB1R) and purinergic P2X receptors (P2XR) play a critical role in the process of pathological pain. Both CB1R and P2XR are expressed in spinal dorsal horn (DH) neurons. It is not clear whether CB1 receptor activation modulates the function of P2X receptor channels within dorsal horn. For this reason, we observed the effect of CP55940 (cannabinoid receptor agonist) on ATP-induced Ca(2+) mobilization in cultured rat DH neurons. The changes of intracellular calcium concentration ([Ca(2+)]i) were detected with confocal laser scanning microscopy using fluo-4/AM as a calcium fluorescent indicator...
November 10, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/29126730/optimization-of-pharmacokinetic-properties-by-modification-of-a-carbazole-based-cannabinoid-receptor-subtype-2-cb2-ligand
#13
Dominik Heimann, Frederik Börgel, Henk de Vries, Kim Bachmann, Victoria E Rose, Bastian Frehland, Dirk Schepmann, Laura H Heitman, Bernhard Wünsch
Recently, the development of the fluorinated PET tracer [(18)F]1a for imaging of CB2 receptors in the central nervous system was reported. [(18)F]1a showed high CB2 affinity and selectivity over the CB1 subtype, but rapid biotransformation in mice. In addition to the amide hydrolysis, oxidative N-dealkylation and carbazole oxidation were postulated as main metabolic pathways. Based on these results, novel carbazole derivatives with additional 6-substituents (23a, 24a), modified hydrogenation state (26a) and enlarged fluoroalkyl substituent (13a, 13b) were synthesized and pharmacologically evaluated...
October 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29121220/pathway-specific-control-of-striatal-neuron-vulnerability-by-corticostriatal-cannabinoid-cb1-receptors
#14
Andrea Ruiz-Calvo, Irene B Maroto, Raquel Bajo-Grañeras, Anna Chiarlone, Ángel Gaudioso, José J Ferrero, Eva Resel, José Sánchez-Prieto, José A Rodríguez-Navarro, Giovanni Marsicano, Ismael Galve-Roperh, Luigi Bellocchio, Manuel Guzmán
The vast majority of neurons within the striatum are GABAergic medium spiny neurons (MSNs), which receive glutamatergic input from the cortex and thalamus, and form two major efferent pathways: the direct pathway, expressing dopamine D1 receptor (D1R-MSNs), and the indirect pathway, expressing dopamine D2 receptor (D2R-MSNs). While molecular mechanisms of MSN degeneration have been identified in animal models of striatal damage, the molecular factors that dictate a selective vulnerability of D1R-MSNs or D2R-MSNs remain unknown...
October 31, 2017: Cerebral Cortex
https://www.readbyqxmd.com/read/29120578/role-of-cannabinoid-cb2-receptor-gene-cnr2-polymorphism-in-children-with-immune-thrombocytopenic-purpura-in-beni-suef-governorate-in-egypt
#15
Dina A Ezzat, Amira A Hammam, Waleed M El-Malah, Rasha A Khattab, Eman M Mangoud
The cannabinoid system is involved in the immune regulation by modulation of Th cells type 1 and 2. It is composed of the CB2 receptor which is expressed at 10 to 100 folds greater levels on immune cells than the CB1 receptors. The CB2 is encoded by the cannabinoid CB receptor gene (CNR2) gene. This study aims to investigate the polymorphism in CNR2 gene variation rs 35761398 (Q63R) in Egyptian children with immune thrombocytopenic purpura and to investigate the relation between this gene polymorphism and either the susceptibility to or the chronicity of the disease...
January 2017: Egyptian Journal of Immunology
https://www.readbyqxmd.com/read/29113898/finding-order-in-chemical-chaos-continuing-characterization-of-synthetic-cannabinoid-receptor-agonists
#16
REVIEW
Julie A Marusich, Jenny L Wiley, Timothy W Lefever, Purvi R Patel, Brian F Thomas
Diversion of synthetic cannabinoids from the lab to drugs of abuse has become increasingly prevalent in recent years. Moreover, as earlier synthetic cannabinoids were banned, manufacturers introduced a new supply of novel compounds to serve as replacements. Hence, the chemical diversity of synthetic cannabinoid analogs has also rapidly increased. The present study examined 8 new synthetic cannabinoids: AM-1220, AM-2232, AM-2233, AM-679, EAM-2201, JWH-210, JHW-251, and MAM-2201. Each compound was assessed for binding affinity and functional activation of CB1 and CB2 receptors, and pharmacological equivalence with Δ(9)-tetrahydrocannabinol (THC) in THC drug discrimination...
November 4, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29111736/structure-affinity-relationships-and-structure-kinetic-relationships-of-1-2-diarylimidazol-4-carboxamide-derivatives-as-human-cannabinoid-1-receptor-antagonists
#17
Lizi Xia, Henk de Vries, Eelke B Lenselink, Julien Louvel, Michael J Waring, Leifeng Cheng, Sara Pahlén, Maria J Petersson, Peter Schell, Roine I Olsson, Laura H Heitman, Robert J Sheppard, Adriaan P IJzerman
We report on the synthesis and biological evaluation of a series of 1,2-diarylimidazol-4-carboxamide derivatives developed as CB1 receptor antagonists. These were evaluated in a radioligand displacement binding assay, a [(35)S]GTPγS binding assay, and in a competition association assay that enables the relatively fast kinetic screening of multiple compounds. The compounds show high affinities and a diverse range of kinetic profiles at the CB1 receptor, and their structure-kinetic relationships (SKRs) were established...
November 7, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29111112/anti-migraine-effect-of-%C3%A2-9-tetrahydrocannabinol-in-the-female-rat
#18
Ram Kandasamy, Cole T Dawson, Rebecca M Craft, Michael M Morgan
Current anti-migraine treatments have limited efficacy and many side effects. Although anecdotal evidence suggests that marijuana is useful for migraine, this hypothesis has not been tested in a controlled experiment. Thus, the present study tested whether administration of ∆(9)-tetrahydrocannabinol (THC) produces anti-migraine effects in the female rat. Microinjection of the TRPA1 agonist allyl isothiocyanate (AITC) onto the dura mater produced migraine-like pain for 3h as measured by depression of home cage wheel running...
October 28, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29110748/perinatal-maternal-high-fat-diet-induces-early-obesity-and-sex-specific-alterations-of-the-endocannabinoid-system-in-white-and-brown-adipose-tissue-of-weanling-rat-offspring
#19
Mariana M Almeida, Camilla P Dias-Rocha, André S Souza, Mariana F Muros, Leonardo S Mendonca, Carmen C Pazos-Moura, Isis H Trevenzoli
Perinatal maternal high-fat (HF) diet programmes offspring obesity. Obesity is associated with overactivation of the endocannabinoid system (ECS) in adult subjects, but the role of the ECS in the developmental origins of obesity is mostly unknown. The ECS consists of endocannabinoids, cannabinoid receptors (cannabinoid type-1 receptor (CB1) and cannabinoid type-2 receptor (CB2)) and metabolising enzymes. We hypothesised that perinatal maternal HF diet would alter the ECS in a sex-dependent manner in white and brown adipose tissue of rat offspring at weaning in parallel to obesity development...
November 7, 2017: British Journal of Nutrition
https://www.readbyqxmd.com/read/29109060/cannabinoid-1-receptor-neutral-antagonist-reduces-binge-like-alcohol-consumption-and-alcohol-induced-accumbal-dopaminergic-signaling
#20
Andrea Balla, Bin Dong, Borehalli M Shilpa, Kiran Vemuri, Alexandros Makriyannis, Subhash C Pandey, Henry Sershen, Raymond F Suckow, K Yaragudri Vinod
Binge alcohol (ethanol) drinking is associated with profound adverse effects on our health and society. Rimonabant (SR141716A), a CB1 receptor inverse agonist, was previously shown to be effective for nicotine cessation and obesity. However, studies using rimonabant were discontinued as it was associated with an increased risk of depression and anxiety. In the present study, we examined the pharmacokinetics and effects of AM4113, a novel CB1 receptor neutral antagonist on binge-like ethanol drinking in C57BL/6J mice using a two-bottle choice drinking-in-dark (DID) paradigm...
November 3, 2017: Neuropharmacology
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