Results 211 to 220 of about 562,936 (248)

Discovery of a novel class of selective human CB1 inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2008
Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context.
Nicolas, Foloppe, Nicola H, Allen, Carol H, Bentley, Teresa D, Brooks, Guy, Kennett, Antony R, Knight, Stefania, Leonardi, Anil, Misra, Nathaniel J T, Monck, Daniel M, Sellwood   +9 more
openaire   +2 more sources

Rational design of Gi-biased CB1 agonist with reduced side effects.

Cell
The cannabinoid receptor 1 (CB1) has emerged as a promising candidate for next-generation non-opioid therapies. However, the development of therapeutics targeting CB1 has been consistently hindered by significant adverse effects.
Yu-Ying Liao, Jin-Xin Che, Yunjing Gao, Jianheng Xue, Linjie Li, Lin Wu, Jia-Xue Hu, Meng-Ting Hu, Linghua Xie, Huibing Zhang, D.-D. Shen, Yingjun Dong, Shaokun Zang, Na Zhang, Hao Wang, Yan Zhang, Xiao-Wu Dong, Xiao-Ming Li   +17 more
semanticscholar   +1 more source

Synthetic cannabinoid receptor agonists: classification and nomenclature

Clinical toxicology, 2019
Introduction: The emergence of novel psychoactive substances has changed the epidemiology of drugs used recreationally throughout Europe and have posed significant challenges for clinicians, researchers and regulators.
A. Potts, C. Cano, S. Thomas, Sl Hill
semanticscholar   +1 more source

CB1 receptor inverse agonist pharmacotherapy for metabolic disorders

Drug Development Research, 2009
AbstractThe cannabinoid‐1 receptor (CB1R) has been implicated in the control of energy balance based on its anatomical localization, the interaction among the endocannabinoid system and other transmitter systems, and the appetite‐enhancing effect of tetrahydrocannabinol.
Tung M. Fong, Carol Addy, Ngozi Erondu, Steven B. Heymsfield   +3 more
openaire   +1 more source

The synthetic CB1 cannabinoid receptor selective agonists: Putative medical uses and their legalization

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2021
More than 500 molecules have been identified as components of Cannabis sativa (C. sativa), of which the most studied is Δ9-tetrahydrocannabinol (Δ9-THC). Several studies have suggested that Δ9-THC exerts diverse biological effects, ranging from fragmentation of DNA to behavioral disruptions.
Astrid, Coronado-Álvarez, Karen, Romero-Cordero, Lorena, Macías-Triana, Agnes, Tatum-Kuri, Alba, Vera-Barrón, Henning, Budde, Sérgio, Machado, Tetsuya, Yamamoto, Claudio, Imperatori, Eric, Murillo-Rodríguez   +9 more
openaire   +2 more sources

Induction of CB1 cannabinoid receptor by inflammation in primary afferent neurons facilitates antihyperalgesic effect of peripheral CB1 agonist

Pain, 2006
Cannabinoids act on various regions in the nervous system to modulate neuronal activity including nociception. Here, we investigated CB1 receptor expression in primary afferent neurons in the dorsal root ganglion (DRG) and the efficacy of a local (intraplantar) application of the selective CB1 agonist, 2-arachidonyl-2-chloroethylamide (ACEA), on ...
Fumimasa, Amaya, Goshun, Shimosato, Yasuhiko, Kawasaki, Satoru, Hashimoto, Yoshifumi, Tanaka, Ru-Rong, Ji, Masaki, Tanaka   +6 more
openaire   +2 more sources

Recent CB1 cannabinoid receptor antagonists and inverse agonists

Drug Development Research, 2009
AbstractAntagonists or inverse agonists of the cannabinoid CB1 receptor (CB1R) reported from the 2006–2007 period are reviewed. The compounds are either variations of the archetypical cannabinoid CB1 inverse agonist rimonabant (SR141716) or are other structures less obviously related to the archetype.
openaire   +1 more source

The effects of intracerebroventricular AM‐251, a CB1‐receptor antagonist, and ACEA, a CB1‐receptor agonist, on penicillin‐induced epileptiform activity in rats

Epilepsia, 2009
SummaryPurpose: Several results support the conclusion that the cannabinoid system has a role in generation and cessation of epileptic seizures. The aim of this study was to evaluate the effects of intracerebroventricular AM‐251 [N‐(piperidin‐1‐yl)‐5‐(4‐iodophenyl)‐1‐(2,4‐dichlorophenyl)‐4‐methyl‐1H‐pyrazole‐3‐carboxamide], a CB1‐receptor antagonist ...
Kozan, Ramazan, Ayyildiz, Mustafa, Agar, Erdal   +2 more
openaire   +3 more sources

Increased motivation for beer in rats following administration of a cannabinoid CB1 receptor agonist

European Journal of Pharmacology, 1999
A series of experiments examined the effects of the cannabinoid CB1 receptor agonist CP 55,940 ((-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hyd roxypropyl)cyclohexanol) on the motivation to consume beer, near-beer (a beer-like beverage containing
J E, Gallate, T, Saharov, P E, Mallet, I S, McGregor   +3 more
openaire   +2 more sources

Interaction of the CB1 agonist ACEA and propofol

European Journal of Anaesthesiology, 2005
P.-A. Brand, P. Meybohm, J. Scholz, F. Renhof, P. H. Tonner   +4 more
openaire   +1 more source