Results 191 to 200 of about 1,257,507 (228)
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Allosteric Modulation of the Cannabinoid CB1 Receptor
Molecular Pharmacology, 2005We 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 +16 more
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The role of CB1 receptors in psychostimulant addiction
Addiction Biology, 2008ABSTRACTRecent 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. +3 more
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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
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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
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Diaryl piperidines as CB1 receptor antagonists
Bioorganic & Medicinal Chemistry Letters, 2010The 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 +13 more
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The role of the CB1 receptor in the regulation of sleep
Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2008During 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
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Peripherally restricted CB1 receptor blockers
Bioorganic & Medicinal Chemistry Letters, 2013Antagonists (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 ...
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Pharmacology of cannabinoid CB1 and CB2 receptors
Pharmacology & Therapeutics, 1997There 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.
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Specific detection of CB1 receptors; cannabinoid CB1 receptor antibodies are not all created equal!
Journal of Neuroscience Methods, 2008The 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 +5 more
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Crystal Structure of the Human Cannabinoid Receptor CB1
Cell, 2016Suwen Zhao, Qiang Zhao, Mengchen Pu
exaly