Results 51 to 60 of about 10,682 (172)

Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties [PDF]

Physiology & Behavior, 2008
The CB1 inverse agonist/antagonist SR141716A recently has been introduced for the management of obesity (rimonabant; Acomplia) and appears to have beneficial effects. However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression. The recent development of biochemically 'neutral' antagonists
Jack, Bergman, Marcus S, Delatte, Carol A, Paronis, Kiran, Vemuri, Ganesh A, Thakur, Alex, Makriyannis   +5 more
openaire   +2 more sources

Quinazoline-2,4(1H,3H)-dione derivatives as new class of CB1 Agonists: A pharmacophore-based virtual screening workflow and drug discovery [version 2; peer review: 2 approved]

F1000Research
Background The cannabinoid 1 (CB1) receptor is the primary target of Δ9-tetrahydrocannabinol (Δ9-THC), the psychoactive component of cannabis sativa (commonly known as “kif” in Morocco).
Fouad Khalil, Abdellah EL AISSOUQ, MOURAD STITOU, Mohamed Enneiymy, Said El Rhabori, Hicham Zaitan, Abdelkrim Ouammou   +6 more
doaj   +1 more source

Activation of cannabinoid receptors in breast cancer cells improves osteoblast viability in cancer-bone interaction model while reducing breast cancer cell survival and migration

Scientific Reports, 2022
The endocannabinoid system has been postulated to help restrict cancer progression and maintain osteoblastic function during bone metastasis. Herein, the effects of cannabinoid receptor (CB) type 1 and 2 activation on breast cancer cell and osteoblast ...
Tueanjai Khunluck, Kornkamon Lertsuwan, Chartinun Chutoe, Supagarn Sooksawanwit, Ingon Inson, Jarinthorn Teerapornpuntakit, Rutaiwan Tohtong, Narattaphol Charoenphandhu   +7 more
doaj   +1 more source

Systematic Modification of the Substitution Pattern of the 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Scaffold Enabled the Discovery of New Ligands with High Affinity and Selectivity for the Cannabinoid Type 2 Receptor

Molecules, 2023
Selective ligands of the CB2 receptor are receiving considerable attention due to their potential as therapeutic agents for a variety of diseases. Recently, 7-hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide derivatives were shown to act at the CB2 ...
Claudia Mugnaini, Magdalena Kostrzewa, Marta Casini, Poulami Kumar, Valeria Catallo, Marco Allarà, Laura Guastaferro, Antonella Brizzi, Marco Paolino, Andrea Tafi, Christelos Kapatais, Gianluca Giorgi, Federica Vacondio, Marco Mor, Federico Corelli, Alessia Ligresti   +15 more
doaj   +1 more source

The role of cannabinoid agonists and antagonists on folliculogenesis and evolutionary events in the mouse ovary [PDF]

Iranian Journal of Basic Medical Sciences
Objective(s): Cannabinoids, derivatives of Cannabis sativa L., can activate the endocannabinoid system via two endogenous receptors, CB1 and CB2. This system is crucial in regulating folliculogenesis, fertility, and reproductive function.
Vida Mirzaie, Touba Eslaminejad, Fatemeh Sheikhbahaei, Shayan Vafaei, Fatemeh Nabipour, Mina Behzadi, Seyyed Noureddin Nematollahi-Mahani   +6 more
doaj   +1 more source

Reduced CB1 Cannabinoid Receptor Expression in Alzheimer's Disease and Transgenic Mouse Models

AGING MEDICINE, EarlyView.
CB1 receptor (CB1R) expression was significantly reduced in the hippocampus, medial frontal gyrus, and superior temporal gyrus of Alzheimer's patients. CB1R levels negatively correlated with amyloid‐β and tau pathology. In addition, CB1R expression was also reduced in the cortex of 5xFAD mice and in the hippocampus of Tg4‐42 mice.
Nike von Borcke, Amrei Vivian Purwien, Annik Steiert, Henrike Hasecke, Yvonne Bouter   +4 more
wiley   +1 more source

Organized cannabinoid receptor distribution in neurons revealed by super-resolution fluorescence imaging

Nature Communications, 2020
Despite the importance of G-protein-coupled receptors in many cellular functions, their intracellular organisation is largely unknown. The authors identified periodically repeating clusters of cannabinoid receptor 1 hotspots within neuronal axons that ...
Hui Li, Jie Yang, Cuiping Tian, Min Diao, Quan Wang, Simeng Zhao, Shanshan Li, Fangzhi Tan, Tian Hua, Ya Qin, Chao-Po Lin, Dylan Deska-Gauthier, Garth J. Thompson, Ying Zhang, Wenqing Shui, Zhi-Jie Liu, Tong Wang, Guisheng Zhong   +17 more
doaj   +1 more source

Cannabidiol in Anorexia Nervosa: A Double‐Blind Randomized Placebo Controlled Pilot Study to Test Safety, Pharmacokinetics, and Symptom Change

International Journal of Eating Disorders, EarlyView.
ABSTRACT Objective Anorexia nervosa (AN) is a severe psychiatric disorder marked by an intense fear of gaining weight and persistent body dissatisfaction, both during periods of underweight and after weight restoration. The endocannabinoid system may offer therapeutic benefits, particularly in reducing anxiety.
Neha Sahota, David J. Grelotti, Tyler Nguyen, Walter H. Kaye, Skylar Swindle, Raymond Suhandynata, Spencer Seely, Megan E. Shott, Guido K. W. Frank   +8 more
wiley   +1 more source

The CB1 inverse agonist AM251, but not the CB1 antagonist AM4113, enhances retention of contextual fear conditioning in rats [PDF]

Pharmacology Biochemistry and Behavior, 2010
The effects of CB1 antagonist/inverse agonists on the acquisition and consolidation of conditioned fear remain uncertain. Recent studies suggest that the CB1 antagonist/inverse agonist AM251 affects acquisition or consolidation of both contextual and discretely cued fear memories.
Sink, K., Segovia, K., Collins-Praino, L., Markus, E., Vemuri, V., Makriyannis, A., Salamone, J.   +6 more
openaire   +3 more sources

Gray Matter Volume Loss in Parkinson's Disease Psychosis and Cannabinoid Receptor Gene Expression in the Brain

Movement Disorders, EarlyView.
Abstract Background Serotonergic and dopaminergic pathways are implicated in Parkinson's disease psychosis (PDP), but preliminary evidence also implicates the endocannabinoid system (ECS). Objectives We examined the association of gray matter volume loss in PDP patients with brain expression of the genes coding for CB1 (cannabinoid type 1) and CB2 ...
Sara Pisani, František Váša, Latha Velayudhan, Sagnik Bhattacharyya   +3 more
wiley   +1 more source