Results 161 to 170 of about 21,385 (196)

Aminopyrazine CB1 receptor inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2008
A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential.
David J, Wustrow, George D, Maynard, Jun, Yuan, He, Zhao, Jianmin, Mao, Qin, Guo, Mark, Kershaw, Jack, Hammer, Robbin M, Brodbeck, Kristen E, Near, Dan, Zhou, David S, Beers, Bertrand L, Chenard, James E, Krause, Alan J, Hutchison   +14 more
openaire   +2 more sources

Diaryl piperidines as CB1 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.
Jack D, Scott, Sarah W, Li, Hongwu, Wang, Yan, Xia, Charles L, Jayne, Michael W, Miller, Ruth A, Duffy, George C, Boykow, Timothy J, Kowalski, Brian D, Spar, Andrew W, Stamford, Samuel, Chackalamannil, Jean E, Lachowicz, William J, Greenlee   +13 more
openaire   +2 more sources

Allosteric Modulation of the Cannabinoid CB1 Receptor

Molecular Pharmacology, 2005
We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5-fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2 ...
Martin R, Price, Gemma L, Baillie, Adèle, Thomas, Lesley A, Stevenson, Morag, Easson, Richard, Goodwin, Adèle, McLean, Lorraine, McIntosh, Gillian, Goodwin, Glenn, Walker, Paul, Westwood, Julia, Marrs, Fiona, Thomson, Phillip, Cowley, Arthur, Christopoulos, Roger G, Pertwee, Ruth A, Ross   +16 more
openaire   +2 more sources

The role of CB1 receptors in psychostimulant addiction

Addiction Biology, 2008
ABSTRACTRecent studies have implicated the endocannabinoid (eCB) system in the neuronal mechanisms underlying substance dependence. Here, we review results of studies using cannabinoid receptor subtype 1 (CB1) knockout mice as well as CB1 antagonists to elucidate the role of this neurotransmitter system in psychostimulant addiction. The overall picture
Wiskerke, J., Pattij, T., Schoffelmeer, A.N.M., de Vries, T.J.   +3 more
openaire   +5 more sources

Peripherally restricted CB1 receptor blockers

Bioorganic & Medicinal Chemistry Letters, 2013
Antagonists (inverse agonists) of the cannabinoid-1 (CB1) receptor showed promise as new therapies for controlling obesity and related metabolic function/liver disease. These agents, representing diverse chemical series, shared the property of brain penetration due to the initial belief that therapeutic benefit was mainly based on brain receptor ...
openaire   +2 more sources

The role of the CB1 receptor in the regulation of sleep

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2008
During the 1990s, transmembranal proteins in the central nervous system (CNS) that recognize the principal compound of marijuana, the delta-9-tetrahydrocannabinol (Delta9-THC) were described. The receptors were classified as central or peripheral, CB1 and CB2, respectively. To this date, it has been documented the presence in the CNS of specific lipids
openaire   +2 more sources

Specific detection of CB1 receptors; cannabinoid CB1 receptor antibodies are not all created equal!

Journal of Neuroscience Methods, 2008
The study of endogenous cannabinoid CB1 receptor proteins in neuronal tissues and cells relies on the availability of highly specific antibodies. We have tested the ability of a series of CB1 antibodies to detect endogenous receptors in brain as well as hemagglutinin (HA)-tagged receptors transfected into HEK-293 cells using a combination of ...
Natasha L, Grimsey, Catherine E, Goodfellow, Emma L, Scotter, Megan J, Dowie, Michelle, Glass, E Scott, Graham   +5 more
openaire   +2 more sources

Cannabinoid Receptor 1 (CB1)

2021
CB1 receptors mediate most central nervous system effects ascribed to the phytocannabinoid Δ-9-tetrahydrocannabinol (THC). CB1 receptors are guanine nucleotide-binding regulatory protein-coupled receptors that primarily activate Gi/o proteins, resulting in the inhibition of adenylyl cyclase.
Glenn R. Rech, Samer N. Narouze
openaire   +1 more source

Pharmacology of cannabinoid CB1 and CB2 receptors

Pharmacology & Therapeutics, 1997
There are at least two types of cannabinoid receptors, CB1 and CB2, both coupled to G-proteins. CB1 receptors are present in the central nervous system and CB1 and CB2 receptors in certain peripheral tissues. The existence of endogenous cannabinoid receptor agonists has also been demonstrated.
openaire   +2 more sources

LY320135, a Novel Cannabinoid CB1 Receptor Antagonist, Unmasks Coupling of the CB1 Receptor to Stimulation of cAMP Accumulation

The Journal of Pharmacology and Experimental Therapeutics, 1998
LY320135 is a selective antagonist for the brain CB1 receptor, having greater than 70-fold higher affinity for the CB1 than the peripheral CB2 receptor. The Ki values for LY320135 at the CB1 and CB2 receptors, transfected and stably expressed in cell lines, were 224 nM and > 10 microM, respectively.
C C, Felder, K E, Joyce, E M, Briley, M, Glass, K P, Mackie, K J, Fahey, G J, Cullinan, D C, Hunden, D W, Johnson, M O, Chaney, G A, Koppel, M, Brownstein   +11 more
openaire   +2 more sources