Results 21 to 30 of about 10,682 (172)
Evaluating FABP5 as a Therapeutic Target for Pain Management. [PDF]
Eur J PainABSTRACT Background and Objective Fatty acid‐binding proteins (FABPs) are intracellular lipid transporters. Pharmacological inhibition of FABP5 is analgesic in preclinical visceral, inflammatory, neuropathic and joint pain models. Genetic knockout or knockdown of FABP5 induces analgesia in select visceral and inflammatory pain models.
Warren W +4 more
europepmc +2 more sources
Discovery of Potent Dual PPARα Agonists/CB1 Ligands [PDF]
ACS Medicinal Chemistry Letters, 2011 This letter describes the synthesis and in vitro and in vivo evaluation of dual ligands targeting the cannabinoid and peroxisome proliferator-activated receptors (PPAR). These compounds were obtained from fusing the pharmacophores of fibrates and the diarylpyrazole rimonabant, a cannabinoid receptor antagonist.
Pérez-Fernández, Ruth +9 more
openaire +3 more sources
Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling [PDF]
European Journal of Pharmacology, 2008 Cannabinoid drugs differ in their rank order of potency to produce analgesia versus other central nervous system effects. We propose that these differences are due to unique agonist-bound cannabinoid CB1 receptor conformations that exhibit different affinities for individual subsets of intracellular signal transduction pathways.
Teodora, Georgieva +9 more
openaire +2 more sources
Molecules, 2022 Selective modulation of peripheral cannabinoid receptors (CBRs) has potential therapeutic applications in medical conditions, including obesity, diabetes, liver diseases, GI disorders and pain.
George Amato +6 more
doaj +1 more source
Analysis of Tolerance and Behavioral/Physical Dependence during Chronic CB1 Agonist Treatment: Effects of CB1 Agonists, Antagonists, and Noncannabinoid Drugs [PDF]
The Journal of Pharmacology and Experimental Therapeutics, 2013 Behavioral studies of chronic CB(1) receptor activation may provide a pharmacological approach to understanding efficacy-related differences among CB(1) ligands as well as mechanistic commonalities between cannabinoid and noncannabinoid drugs. In the present studies, the effects of CB(1) agonists [(6aR,10aR)-3-(1-adamantyl)-6,6,9-trimethyl-6a,7,10,10a ...
Rajeev I, Desai +5 more
openaire +2 more sources
Biomolecules, 2020 Obesity rates are increasing worldwide and there is a need for novel therapeutic treatment options. The endocannabinoid system has been linked to homeostatic processes, including metabolism, food intake, and the regulation of body weight.
Thomas Murphy, Bernard Le Foll
doaj +1 more source
Distinct activation mechanisms regulate subtype selectivity of Cannabinoid receptors
Communications Biology, 2023 Design of cannabinergic subtype selective ligands is challenging because of high sequence and structural similarities of cannabinoid receptors (CB1 and CB2).
Soumajit Dutta, Diwakar Shukla
doaj +1 more source
Frontiers in Behavioral Neuroscience, 2021 Cannabinoid receptors 1 and 2 (CB1 and CB2, respectively) play an important role in maintaining the integrity of the blood–brain barrier (BBB). On the other hand, BBB dysfunction is a common feature in drug-resistant epilepsy.
María de los Ángeles Nuñez-Lumbreras +12 more
doaj +1 more source
Crystal structures of agonist-bound human cannabinoid receptor CB<sub>1</sub>. [PDF]
NatureHua T +18 more
europepmc +2 more sources
Impaired Excitatory Neurotransmission in the Urinary Bladder from the Obese Zucker Rat: Role of Cannabinoid Receptors. [PDF]
PLoS ONE, 2016 Metabolic syndrome (MS) is a known risk factor for lower urinary tract symptoms. This study investigates whether functional and expression changes of cannabinoid CB1 and CB2 receptors are involved in the bladder dysfunction in an obese rat model with ...
Igor Blaha +10 more
doaj +1 more source