Results 201 to 210 of about 562,936 (248)

1-Benzhydryl-3-phenylurea and 1-Benzhydryl-3-phenylthiourea Derivatives:  New Templates among the CB1 Cannabinoid Receptor Inverse Agonists

Journal of Medicinal Chemistry, 2005
New 1-benzhydryl-3-phenylurea derivatives and their 1-benzhydryl-3-phenylthiourea isosteres were synthesized and evaluated for their human CB1 and CB2 cannabinoid receptor affinity. These compounds proved to be selective CB1 cannabinoid receptor ligands,
Giulio G Muccioli, Johan Wouters, Jacques H Poupaert   +2 more
exaly   +2 more sources

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Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists

Bioorganic and Medicinal Chemistry Letters, 2005
Structure-activity relationship studies for two series of 2-benzyloxy-5-(4-chlorophenyl)-6-(2,4-dichlorophenyl)pyridines having either a 3-cyano or 3-carboxamide moiety resulted in the preparation of the 2-(3,4-difluorobenzyloxy)-3-nitrile analog 10d and the 2-(3,4-difluorobenzyloxy)-3-(N-propylcarboxamide) analog 16c, (hCB1 IC(50)=1.3 and 1.7 nM ...
Alison M Strack, Paul E Finke, D Sloan Stribling   +2 more
exaly   +4 more sources

AM630 is an inverse agonist at the human cannabinoid CB1 receptor

Life Sciences, 1998
The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPgammaS binding to cell membranes was determined.
R S, Landsman, A, Makriyannis, H, Deng, P, Consroe, W R, Roeske, H I, Yamamura   +5 more
openaire   +2 more sources

Prediction of the binding affinities and selectivity for CB1 and CB2 ligands using homology modeling, molecular docking, molecular dynamics simulations, and MM-PBSA binding free energy calculations.

ACS Chemical Neuroscience, 2020
Cannabinoids are a group of chemical compounds that have been used for thousands of years due to their psychoactive function and systemic physiological effects.
Bei-Hong Ji, Shuhan Liu, Xibing He, V. H. Man, X. Xie, Junmei Wang   +5 more
semanticscholar   +1 more source

SR141716A is an inverse agonist at the human cannabinoid CB1 receptor

European Journal of Pharmacology, 1997
The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from ...
R S, Landsman, T H, Burkey, P, Consroe, W R, Roeske, H I, Yamamura   +4 more
openaire   +2 more sources

Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain.

European Journal of Pharmacology, 1997
We measured (-)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohe xyl]-phenol (CP 55,940)-, (-)11-OH-delta8-tetrahydrocannabinol-dimethylheptyl (HU-210)-, anandamide- and delta9-tetrahydrocannabinol-stimulated G protein activation in mouse brain using the [35S]GTPgammaS functional assay.
T. Burkey, R. M. Quock, P. Consroe, F. Ehlert, Y. Hosohata, W. Roeske, H. I. Yamamura   +6 more
semanticscholar   +3 more sources

Cannabinoid receptor 2 selective agonists and Alzheimer's disease: An insight into the therapeutic potentials

Journal of Neuroscience Research, 2021
Endocannabinoid system has been extensively studied in recent decades, particularly the cannabinoid receptors CB1 and CB2, due to their important role in neuroinflammation.
Sai Varshini Magham, Praveen Thaggikuppe Krishnamurthy, Neenu Shaji, Lalithkumar Mani, Shivaramakrishnan Balasubramanian   +4 more
semanticscholar   +1 more source

Alterations in behavioral flexibility by cannabinoid CB1 receptor agonists and antagonists

Psychopharmacology, 2006
Cannabinoid CB1 receptors are expressed in the prefrontal cortex, but their role in mediating executive functions such as behavioral flexibility is unclear.The present study examined the effect of pharmacological activation or blockade of the cannabinoid CB1 receptors on behavioral flexibility using a strategy set-shifting task conducted on a cross ...
M. Hill, Larissa M. Froese, Anna C. Morrish, Jane C. Sun, S. Floresco   +4 more
semanticscholar   +3 more sources

CB1 allosteric modulators and their therapeutic potential in CNS disorders.

Progress in Neuro-psychopharmacology and Biological Psychiatry, 2020
CB1 is the most abundant GPCR found in the mammalian brain. It has garnered considerable attention as a potential therapeutic drug target. CB1 is involved in a wide range of physiological and psychiatric processes and has the potential to be targeted in ...
C. Mielnik, Vincent M. Lam, R. Ross
semanticscholar   +1 more source

A cryptic pocket in CB1 drives peripheral and functional selectivity

Nature
The current opioid overdose epidemic highlights the urgent need to develop safer and more effective treatments for chronic pain1. Cannabinoid receptor type 1 (CB1) is a promising non-opioid target for pain relief, but its clinical use has been limited by
V. Rangari, E. O’Brien, A. Powers, Richard A. Slivicki, Zachariah Bertels, Kevin Appourchaux, Deniz Aydin, Nokomis Ramos-Gonzalez, Juliet M. Mwirigi, Li Lin, Elizaveta Mangutov, Briana L. Sobecks, Yaseen Awad-Agbaria, Manoj B Uphade, Jhoan Aguilar, T. Peddada, Yuki Shiimura, Xi-Ping Huang, Jakayla Folarin-Hines, Maria Payne, Anirudh Kalathil, Balazs R. Varga, B. Kobilka, Amynah A. Pradhan, Michael D. Cameron, K. K. Kumar, Ron O. Dror, R. Gereau, S. Majumdar   +28 more
semanticscholar   +1 more source