Results 161 to 170 of about 27,120 (180)
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2016
Type-1 cannabinoid receptor (CB1), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both central nervous system and peripheral tissues. Today, its biochemical identification and pharmacological characterization, as well as the screening of thousands of novel ligands that might be useful ...
Catani, VM, GASPERI, VALERIA
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Type-1 cannabinoid receptor (CB1), one of the main targets of endocannabinoids, plays a key role in several pathophysiological conditions that affect both central nervous system and peripheral tissues. Today, its biochemical identification and pharmacological characterization, as well as the screening of thousands of novel ligands that might be useful ...
Catani, VM, GASPERI, VALERIA
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Rimonabant—A Selective CB1 Antagonist
Annals of Pharmacotherapy, 2005OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical efficacy, and safety of rimonabant, a new selective cannabinoid receptor antagonist. DATA SOURCES: Primary literature and review articles were obtained via a MEDLINE search (1966–November 2004) using the key terms obesity, smoking cessation, cannabinoid, rimonabant, SR 141716, and SR ...
Steven Thomas, Boyd +1 more
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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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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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CB1 cannabinoid receptor-mediated aggressive behavior
Neuropharmacology, 2013This study examined the role of cannabinoid CB1 receptors (CB1r) in aggressive behavior. Social encounters took place in grouped and isolated mice lacking CB1r (CB1KO) and in wild-type (WT) littermates. Cognitive impulsivity was evaluated in the delayed reinforcement task (DRT).
Rodríguez-Arias, Marta +7 more
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CB1 Cannabinoid Receptor-Mediated Cell Migration
The Journal of Pharmacology and Experimental Therapeutics, 2000Recent studies have suggested that cell migratory responses are often mediated by G(i) protein-coupled receptors. Because it is known that CB1 cannabinoid receptors are coupled to pertussis toxin-sensitive G proteins, we proposed that CB1 may mediate cell migration.
Z H, Song, M, Zhong
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Oximes short-acting CB1 receptor agonists
Bioorganic & Medicinal Chemistry, 2018New oximes short-acting CB1 agonists were explored by the introduction of an internal oxime and polar groups at the C3 alkyl tail of Δ8-THC. The scope of the research was to drastically alter two important physicochemical properties hydrophobicity (log P) and topological surface area (tPSA) of the compound, which play a critical role in tissue ...
Michael S. Malamas +8 more
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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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CNS & Neurological Disorders - Drug Targets, 2011
Cannabinoids are antinociceptive in animal models of acute pain, tissue injury and nerve injury induced nociception and act via their cognate receptors, cannabinoid receptor 1 and 2. This review examines the underlying biology of the endocannabinoids and behavioural, neurophysiological, neuroanatomical evidence supporting the notion of pain modulation ...
Rashmi, Talwar, Vijay Kumar, Potluri
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Cannabinoids are antinociceptive in animal models of acute pain, tissue injury and nerve injury induced nociception and act via their cognate receptors, cannabinoid receptor 1 and 2. This review examines the underlying biology of the endocannabinoids and behavioural, neurophysiological, neuroanatomical evidence supporting the notion of pain modulation ...
Rashmi, Talwar, Vijay Kumar, Potluri
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Neuropharmacology, 2006
Presynaptic terminals of cerebellar granule neurons are primary targets of cannabinoids, which act through type 1 G alpha(i/o)-coupled cannabinoid receptors (CB1) to modulate glutamate release. To study CB1 signaling investigators use primary cultures of granule neurons, typically grown in medium supplemented with elevated KCl to improve long-term ...
Mary Lou, Vallano +3 more
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Presynaptic terminals of cerebellar granule neurons are primary targets of cannabinoids, which act through type 1 G alpha(i/o)-coupled cannabinoid receptors (CB1) to modulate glutamate release. To study CB1 signaling investigators use primary cultures of granule neurons, typically grown in medium supplemented with elevated KCl to improve long-term ...
Mary Lou, Vallano +3 more
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