keyword
MENU ▼
Read by QxMD icon Read
search

CB1 CB2

keyword
https://www.readbyqxmd.com/read/29906493/the-tamoxifen-derivative-ridaifen-b-is-a-high-affinity-selective-cb-2-receptor-inverse-agonist-exhibiting-anti-inflammatory-and-anti-osteoclastogenic-effects
#1
Lirit N Franks, Benjamin M Ford, Toshifumi Fujiwara, Haibo Zhao, Paul L Prather
Selective estrogen receptor modulators (SERMs) target estrogen receptors (ERs) to treat breast cancer and osteoporosis. Several SERMs exhibit anti-cancer activity not related to ERs. To discover novel anti-cancer drugs acting via ER-independent mechanisms, derivatives of the SERM tamoxifen, known as the "ridaifen" compounds, have been developed that exhibit reduced or no ER affinity, while maintaining cytotoxicity. Tamoxifen and other SERMs bind to cannabinoid receptors with moderate affinity. Therefore, ER-independent effects of SERMs might be mediated via cannabinoid receptors...
June 12, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29902723/structure-activity-relationships-of-imidazothiazinones-and-analogs-as-antagonists-of-the-cannabinoid-activated-orphan-g-protein-coupled-receptor-gpr18
#2
Clara T Schoeder, Maria Kaleta, Andhika B Mahardhika, Agnieszka Olejarz-Maciej, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Christa E Müller
GPR18 is a cannabinoid-activated orphan G protein-coupled receptor (GPCR) that is selectively expressed on immune cells. Despite its significant potential as a drug target for inflammatory diseases and cancer immunotherapy, only very few GPR18 ligands have been described to date. In the present study we investigated the structure-activity relationships (SARs) of (Z)-2-(3-(4-chlorobenzyloxy)benzylidene)-6,7-dihydro-2H-imidazo[2,1-b][1,3]thiazin-3(5H)-one (PSB-CB5, 5), the most potent GPR18 antagonist described to date...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29896156/analysis-of-endocannabinoid-system-in-rat-testis-during-the-first-spermatogenetic-wave
#3
Marina Migliaccio, Giulia Ricci, Antonio Suglia, Francesco Manfrevola, Ken Mackie, Silvia Fasano, Riccardo Pierantoni, Teresa Chioccarelli, Gilda Cobellis
Endocannabinoids are lipid mediators, enzymatically synthesized and hydrolyzed, that bind cannabinoid receptors. Together with their receptors and metabolic enzymes, they form the "endocannabinoid system" (ECS). Anandamide (AEA) and 2-arachidonoylglycerol (2-AG) are the main endocannabinoids studied in testis. In this study, using the first wave of spermatogenesis as an in vivo model to verify the progressive appearance of germ cells in seminiferous tubules [i.e., spermatogonia, spermatocytes, and spermatids], we analyzed the expression of the main enzymes and receptors of ECS in rat testis...
2018: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29890719/the-role-of-cannabinoids-in-the-setting-of-cirrhosis
#4
REVIEW
Pratima Dibba, Andrew A Li, George Cholankeril, Umair Iqbal, Chiranjeevi Gadiparthi, Muhammad Ali Khan, Donghee Kim, Aijaz Ahmed
Although the mortality rates of cirrhosis are underestimated, its socioeconomic burden has demonstrated a significant global impact. Cirrhosis is defined by the disruption of normal liver architecture after years of chronic insult by different etiologies. Treatment modalities are recommended primarily in decompensated cirrhosis and specifically tailored to the different manifestations of hepatic decompensation. Antifibrogenic therapies are within an active area of investigation. The endocannabinoid system has been shown to play a role in liver disease, and cirrhosis specifically, with intriguing possible therapeutic benefits...
June 9, 2018: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/29890144/ischemia-reperfusion-model-impairs-endocannabinoid-signaling-and-na-k-atpase-expression-and-activity-in-kidney-proximal-tubule-cells
#5
Luzia S Sampaio, Fabio A Iannotti, Luciana Veneziani, Rosa T Borelli-Tôrres, Fabrizia De Maio, Fabiana Piscitelli, Ricardo A M Reis, Vincenzo Di Marzo, Marcelo Einicker-Lamas
LLC-PK1 cells, an immortalized epithelial cell line derived from pig renal proximal tubules, express all the major players of the endocannabinoid system (ECS) such as CB1, CB2 and TRPV1 receptor, as well as the main enzymes involved in the biosynthesis and degradation of the major endocannabinoids named 2-arachidonoylglycerol, 2-AG and anandamide, AEA. Here we investigated whether the damages caused by ischemic insult either in vitro using LLC-PK1 cells exposed to antimycin A (an inductor of ATP-depletion) or in vivo using Wistar rats in a classic renal ischemia and reperfusion (IR) protocol, lead to changes in AEA and 2-AG levels, as well as altered expression of genes from the main enzymes involved in the regulation of the ECS...
June 8, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29888782/activation-of-gpr55-increases-neural-stem-cell-proliferation-and-promotes-early-adult-hippocampal-neurogenesis
#6
Jeremy D Hill, Viviana Zuluaga-Ramirez, Sachin Gajghate, Malika Winfield, Yuri Persidsky
BACKGROUND AND PURPOSE: The cannabinoid system exerts functional regulation of neural stem cell (NSC) proliferation and adult neurogenesis, yet not all effects of cannabinoid-like compounds seen can be attributed to the cannabinoid 1 receptor (CB1 R) or cannabinoid 2 receptor (CB2 R). The recently de-orphaned GPR55 has been shown to be activated by numerous cannabinoid ligands suggesting that GPR55 is a third cannabinoid receptor. Here we examined the role of GPR55 activation in NSC proliferation and early adult neurogenesis...
June 11, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29883990/assessment-of-cannabinoids-agonist-and-antagonist-in-invasion-potential-of-k562-cancer-cells
#7
Fatemeh Gholizadeh, Mohammad Hossein Ghahremani, Shima Aliebrahimi, Amir Shadboorestan, Seyed Nasser Ostad
Background: The prominent hallmark of malignancies is the metastatic spread of cancer cells. Recent studies have reported that the nature of invasive cells could be changed after this phenomenon, causing chemotherapy resistance. It has been demonstrated that the up-regulated expression of matrix metalloproteinase (MMP) 2/MMP-9, as a metastasis biomarker, can fortify the metastatic potential of leukemia. Furthermore, investigations have confirmed the inhibitory effect of cannabinoid and endocannabinoid on the proliferation of cancer cells in vitro and in vivo...
June 9, 2018: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/29882158/localization-of-cannabinoid-receptors-cb1-cb2-gpr55-and-ppar%C3%AE-in-the-canine-gastrointestinal-tract
#8
Giorgia Galiazzo, Fiorella Giancola, Agnese Stanzani, Federico Fracassi, Chiara Bernardini, Monica Forni, Marco Pietra, Roberto Chiocchetti
The endocannabinoid system (ECS) is composed of cannabinoid receptors, their endogenous ligands, and the enzymes involved in endocannabinoid turnover. Modulating the activity of the ECS may influence a variety of physiological and pathophysiological processes. A growing body of evidence indicates that activation of cannabinoid receptors by endogenous, plant-derived, or synthetic cannabinoids may exert beneficial effects on gastrointestinal inflammation and visceral pain. The present ex vivo study aimed to investigate immunohistochemically the distribution of cannabinoid receptors CB1, CB2, G protein-coupled receptor 55 (GPR55), and peroxisome proliferation activation receptor alpha (PPARα) in the canine gastrointestinal tract...
June 7, 2018: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/29880989/one-step-stereoselective-synthesis-of-octahydrochromanes-via-the-prins-reaction-and-their-cannabinoid-activities
#9
Shuneize Slater, Pradeep B Lasonkar, Saqlain Haider, Moneerah J Alqahtani, Amar G Chittiboyina, Ikhlas A Khan
Novel, functionalized octahydrochromene derivatives were synthesized in a single step via the Prins reaction. Enantiomerically pure (+)-isopulegol was reacted with benzaldehyde to stereoselectively yield the corresponding octahydro-2 H -chromen-4-ol derivative containing five stereocenters. A total of 10 compounds were synthesized by altering the enantiomer of isopulegol and the substituted benzaldehyde, and the resulting enantiopure octahydrochromenes were screened in vitro against the cannabinoid receptor isoforms CB1 and CB2...
February 28, 2018: Tetrahedron Letters
https://www.readbyqxmd.com/read/29870711/molecular-and-functional-interaction-between-gpr18-and-cannabinoid-cb-2-g-protein-coupled-receptors-relevance-in-neurodegenerative-diseases
#10
Irene Reyes-Resina, Gemma Navarro, David Aguinaga, Enric I Canela, Clara T Schoeder, Michal Zaluski, Katarzyna Kiec-Kononowicz, Carlos A Saura, Christa E Müller, Rafael Franco
GPR18, still considered an orphan receptor, may respond to endocannabinoids, whose canonical receptors are CB1 and CB2 . GPR18 and CB2 receptors share a role in peripheral immune response regulation and are co-expressed in microglia, which are immunocompetent cells in the central nervous system (CNS). We aimed at identifying heteroreceptor complexes formed by GPR18 and CB1 R or CB2 R in resting and activated microglia. Receptor-receptor interaction was assessed using energy-transfer approaches, and receptor function by determining cAMP levels and ERK1/2 phosphorylation in heterologous cells and primary cultures of microglia...
June 2, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29858778/effects-of-dietary-clostridium-butyricum-on-the-growth-digestive-enzyme-activity-antioxidant-capacity-and-resistance-to-nitrite-stress-of-penaeus-monodon
#11
Yafei Duan, Jiasong Zhang, Jianhua Huang, Shigui Jiang
The present study investigated the effects of the dietary probiotic Clostridium butyricum (CB) on the growth, intestine digestive enzyme activity, antioxidant capacity and resistance to nitrite stress, and body composition of Penaeus monodon. For 56 days, shrimps were fed diets containing different levels of C. butyricum (1 × 109  CFU g-1 ), 0% (control), 0.5% (CB1), 1.0% (CB2), and 2.0% (CB3), as treatment groups, followed by an acute nitrite stress test for 48 h. The results indicated that dietary supplementation of C...
June 1, 2018: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/29842858/pharmacological-inhibiton-of-2-arachidonoilglycerol-hydrolysis-enhances-memory-consolidation-in-rats-through-cb2-receptor-activation-and-mtor-signaling-modulation
#12
Patrizia Ratano, Carla Petrella, Fabrizio Forti, Pamela Petrocchi Passeri, Maria Morena, Maura Palmery, Viviana Trezza, Cinzia Severini, Patrizia Campolongo
The endocannabinoid system is a key modulator of memory consolidation for aversive experiences. We recently found that the fatty acid amide hydrolase (FAAH) inhibitor URB597, which increases anandamide levels by inhibiting its hydrolysis, facilitates memory consolidation through a concurrent activation of both cannabinoid receptor type 1 (CB1) and 2 (CB2). Here, we investigated the role played on memory consolidation by the other major endocannabinoid, 2-arachidonoylglycerol (2-AG). To this aim, we tested the effects of pharmacological inhibition of monoacylglycerol lipase (MAGL) through systemic administration of the MAGL inhibitor JZL184 to rats immediately after training of the inhibitory avoidance task...
May 26, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29813086/elevated-levels-of-2-arachidonoylglycerol-promote-atherogenesis-in-apoe-mice
#13
Julian Jehle, Benedikt Schöne, Sayeh Bagheri, Elina Avraamidou, Melina Danisch, Imke Frank, Philipp Pfeifer, Laura Bindila, Beat Lutz, Dieter Lütjohann, Andreas Zimmer, Georg Nickenig
BACKGROUND: The endocannabinoid (eCB) 2-arachidonoylglycerol (2-AG) is a known modulator of inflammation and ligand to both, pro-inflammatory cannabinoid receptor 1 (CB1) and anti-inflammatory CB2. While the role of both receptors in atherogenesis has been studied extensively, the significance of 2-AG for atherogenesis is less well characterized. METHODS: The impact of 2-AG on atherogenesis was studied in two treatment groups of ApoE-/- mice. One group received the monoacylglycerol lipase (MAGL)-inhibitor JZL184 [5 mg/kg i...
2018: PloS One
https://www.readbyqxmd.com/read/29797785/computational-investigation-on-the-binding-modes-of-rimonabant-analogues-with-cb1-and-cb2
#14
Cheng Liu, Congmin Yuan, Pinwen Wu, Chen Zhu, Hao Fang, Lili Wang, Wei Fu
The human cannabinoid G protein coupled receptor 1 (CB1) is highly expressed in central nervous system. CB1-selective antagonists show therapeutic promise in a wide range of disorders, such as obesity-related metabolic disorders, dyslipidemia, drug abuse and type 2 diabetes. Rimonabant (SR141716A), MJ08 and MJ15 are selective CB1 antagonists with selectivity >1000 folds over CB2 despite of 42% sequence identity between CB1 and CB2. The integration of homology modeling, automated molecular docking and molecular dynamics simulation were used to investigate the binding modes of these selective inverse agonists/antagonists with CB1 and CB2 and their selectivity...
May 24, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29792186/involvement-of-the-cb-2-cannabinoid-receptor-in-cell-growth-inhibition-and-g0-g1-cell-cycle-arrest-via-the-cannabinoid-agonist-win-55-212-2-in-renal-cell-carcinoma
#15
Mohammed I Khan, Anna A Sobocińska, Klaudia K Brodaczewska, Katarzyna Zielniok, Malgorzata Gajewska, Claudine Kieda, Anna M Czarnecka, Cezary Szczylik
BACKGROUND: The anti-tumor properties of cannabinoids have been investigated in many in vitro and in vivo studies. Many of these anti-tumor effects are mediated via cannabinoid receptor types 1 and 2 (CB1 and CB2 ), comprising the endocannabinoid system (ECS). In this study, we investigated the ECS based on CB 1 and CB 2 receptor gene and protein expression in renal cell carcinoma (RCC) cell lines. In view of their further use for potential treatments, we thus investigated the roles of CB1 and CB2 receptors in the anti-proliferative action and signal transduction triggered by synthetic cannabinoid agonists [such as JWH-133 and WIN 55,212-2 (WIN-55)] in RCC cell lines...
May 23, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29773016/is-cannabidiol-a-promising-substance-for-new-drug-development-a-review-of-its-potential-therapeutic-applications
#16
Nida Noreen, Faqir Muhammad, Bushra Akhtar, Farooq Azam, Muhammad Irfan Anwar
The pharmacological importance of cannabidiol (CBD) has been in study for several years. CBD is the major nonpsychoactive constituent of plant Cannabis sativa and its administration is associated with reduced side effects. Currently, CBD is undergoing a lot of research which suggests that it has no addictive effects, good safety profile and has exhibited powerful therapeutic potential in several vital areas. It has wide spectrum of action because it acts through endocannabinoid receptors; CB1 and CB2 and it also acts on other receptors, such as GPR18, GPR55, GPR 119, 5HT1A, and TRPV2...
2018: Critical Reviews in Eukaryotic Gene Expression
https://www.readbyqxmd.com/read/29770478/the-endocannabinoid-alcohol-crosstalk-recent-advances-on-a-bi-faceted-target
#17
REVIEW
Gianluca Lavanco, Valentina Castelli, Anna Brancato, Giuseppe Tringali, Fulvio Plescia, Carla Cannizzaro
Increasing evidence focuses on the endocannabinoid system as a relevant player in the induction of aberrant synaptic plasticity and related addictive phenotype following chronic excessive alcohol drinking. Besides, the endocannabinoid system is implicated in the pathogenesis of alcoholic liver disease. Interestingly, whereas the involvement of CB1 cannabinoid receptors in alcohol rewarding properties is established, the central and peripheral action of CB2 cannabinoid signalling is still to be elucidated. This review aims at giving the input to deepen knowledge on the role of the endocannabinoid system, highlighting the advancing evidence that suggests that CB1 and CB2 receptors may play opposite roles in the regulation of both the reinforcing properties of alcohol in the brain and the mechanisms responsible for cell injury and inflammation in the hepatic tissue...
May 16, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29765535/effects-of-cb2-and-trpv1-receptors-stimulation-in-pediatric-acute-t-lymphoblastic-leukemia
#18
Francesca Punzo, Iolanda Manzo, Chiara Tortora, Elvira Pota, Velia D' Angelo, Giulia Bellini, Alessandra Di Paola, Federica Verace, Fiorina Casale, Francesca Rossi
T-Acute Lymphoblastic Leukemia (T-ALL) is less frequent than B-ALL, but it has poorer outcome. For this reason new therapeutic approaches are needed to treat this malignancy. The Endocannabinoid/Endovanilloid (EC/EV) system has been proposed as possible target to treat several malignancies, including lymphoblastic diseases. The EC/EV system is composed of two G-Protein Coupled Receptors (CB1 and CB2), the Transient Potential Vanilloid 1 (TRPV1) channel, their endogenous and exogenous ligands and enzymes. CB1 is expressed mainly in central nervous system while CB2 predominantly on immune and peripheral cells, therefore we chose to selectively stimulate CB2 and TRPV1...
April 20, 2018: Oncotarget
https://www.readbyqxmd.com/read/29759062/inhibition-of-2-ag-hydrolysis-differentially-regulates-blood-brain-barrier-permeability-after-injury
#19
Justin R Piro, Georgette L Suidan, Jie Quan, YeQing Pi, Sharon M O'Neill, Marissa Ilardi, Nikolay Pozdnyakov, Thomas A Lanz, Hualin Xi, Robert D Bell, Tarek A Samad
BACKGROUND: Acute neurological insults caused by infection, systemic inflammation, ischemia, or traumatic injury are often associated with breakdown of the blood-brain barrier (BBB) followed by infiltration of peripheral immune cells, cytotoxic proteins, and water. BBB breakdown and extravasation of these peripheral components into the brain parenchyma result in inflammation, oxidative stress, edema, excitotoxicity, and neurodegeneration. These downstream consequences of BBB dysfunction can drive pathophysiological processes and play a substantial role in the morbidity and mortality of acute and chronic neurological insults, and contribute to long-term sequelae...
May 14, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29754307/effects-of-cocaine-self-administration-and-its-extinction-on-the-rat-brain-cannabinoid-cb1-and-cb2-receptors
#20
Beata Bystrowska, Małgorzata Frankowska, Irena Smaga, Lucyna Pomierny-Chamioło, Małgorzata Filip
The aim of this study was to evaluate changes in the expression of cannabinoid type 1 (CB1) and 2 (CB2) receptor proteins in several brain regions in rats undergoing cocaine self-administration and extinction training. We used a triad-yoked procedure to distinguish between the motivational and pharmacological effects of cocaine. Using immunohistochemistry, we observed a significant decrease in CB1 receptor expression in the prefrontal cortex, dorsal striatum, and the basolateral and basomedial amygdala following cocaine (0...
May 12, 2018: Neurotoxicity Research
keyword
keyword
72433
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"