Search results for "Cannabinoid Receptor Agonists"

showing 10 items of 22 documents

Cannabinoid receptor expression in non-small cell lung cancer. Effectiveness of tetrahydrocannabinol and cannabidiol inhibiting cell proliferation an…

2020

Background/Objective Patients with non-small cell lung cancer (NSCLC) develop resistance to antitumor agents by mechanisms that involve the epithelial-to-mesenchymal transition (EMT). This necessitates the development of new complementary drugs, e.g., cannabinoid receptors (CB1 and CB2) agonists including tetrahydrocannabinol (THC) and cannabidiol (CBD). The combined use of THC and CBD confers greater benefits, as CBD enhances the effects of THC and reduces its psychotropic activity. We assessed the relationship between the expression levels of CB1 and CB2 to the clinical features of a cohort of patients with NSCLC, and the effect of THC and CBD (individually and in combination) on prolifer…

0301 basic medicineMaleCannabinoid receptorLung NeoplasmsPulmonologymedicine.medical_treatmentGene ExpressionBiochemistryLung and Intrathoracic TumorsReceptor Cannabinoid CB20302 clinical medicineContractile ProteinsReceptor Cannabinoid CB1Epidermal growth factorCarcinoma Non-Small-Cell LungMedicine and Health SciencesCannabidiolDronabinolAged 80 and overMultidisciplinaryChemistryQRDrugsMiddle AgedCancer Cell MigrationCell MotilityOncologyCell Processes030220 oncology & carcinogenesisMedicinelipids (amino acids peptides and proteins)Femalemedicine.drugResearch ArticleAdultEpithelial-Mesenchymal TransitionScienceChronic Obstructive Pulmonary DiseaseCell Migration03 medical and health sciencesCell Line Tumormental disordersmedicineGeneticsHumansEpithelial–mesenchymal transitionTetrahydrocannabinolCell ProliferationAgedA549 cellPharmacologyCannabinoid Receptor AgonistsPsychotropic DrugsCell growthCannabinoidsorganic chemicalsCancers and NeoplasmsBiology and Life SciencesProteinsCell Biologydigestive system diseasesActinsrespiratory tract diseasesNon-Small Cell Lung CancerCytoskeletal Proteins030104 developmental biologyA549 CellsCancer researchCannabinoidCannabidiolDevelopmental BiologyPLoS ONE
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Pharmacological activation of CB2 receptors counteracts the deleterious effect of ethanol on cell proliferation in the main neurogenic zones of the a…

2015

Chronic alcohol exposure reduces endocannabinoid activity and disrupts adult neurogenesis in rodents, which results in structural and functional alterations. Cannabinoid receptor agonists promote adult neural progenitor cell (NPC) proliferation. We evaluated the protective effects of the selective CB1 receptor agonist ACEA, the selective CB2 receptor agonist JWH133 and the fatty-acid amide-hydrolase (FAAH) inhibitor URB597, which enhances endocannabinoid receptor activity, on NPC proliferation in rats with forced consumption of ethanol (10%) or sucrose liquid diets for 2 weeks. We performed immunohistochemical and stereological analyses of cells expressing the mitotic phosphorylation of his…

:Phenomena and Processes::Physiological Phenomena::Physiological Processes::Growth and Development::Morphogenesis::Embryonic and Fetal Development::Organogenesis::Neurogenesis [Medical Subject Headings]CB1 receptorTubulina (proteína)Cannabinoid receptorCarbamatosEtanol:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Nuclear Proteins::Histones [Medical Subject Headings]Ventrículos lateralesSacarosaNeuronasSubgranular zone0302 clinical medicine:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Membrane Proteins::Receptors Cell Surface::Receptors G-Protein-Coupled::Receptors Cannabinoid::Receptor Cannabinoid CB1 [Medical Subject Headings]Histonas:Chemicals and Drugs::Organic Chemicals::Carboxylic Acids::Acids Acyclic::Carbamates [Medical Subject Headings]Receptor cannabinoide CB1Cannabinoid receptor type 2:Organisms::Eukaryota::Animals [Medical Subject Headings]:Phenomena and Processes::Metabolic Phenomena::Metabolism::Phosphorylation [Medical Subject Headings]:Anatomy::Cells::Stem Cells::Neural Stem Cells [Medical Subject Headings]:Anatomy::Nervous System::Neurons [Medical Subject Headings]health care economics and organizations:Anatomy::Nervous System::Central Nervous System::Brain::Cerebral Ventricles::Lateral Ventricles [Medical Subject Headings]Original Research:Chemicals and Drugs::Nucleic Acids Nucleotides and Nucleosides::Nucleosides::Deoxyribonucleosides::Deoxyuridine::Bromodeoxyuridine [Medical Subject Headings]0303 health sciencesAlcoholismoalcoholConsumo de alcoholNeurogenesis:Phenomena and Processes::Genetic Phenomena::Phenotype::Genetic Markers [Medical Subject Headings]:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Cannabinoid Receptor Modulators::Cannabinoid Receptor Agonists [Medical Subject Headings]Benzamidas:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Membrane Proteins::Receptors Cell Surface::Receptors G-Protein-Coupled::Receptors Cannabinoid::Receptor Cannabinoid CB2 [Medical Subject Headings]Endocannabinoid system3. Good healthbromodesoxiuridinaneurogenesisEndocannabinoidesmedicine.anatomical_structure:Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Hydrolases [Medical Subject Headings]ACEADietaAlcoholFosforilaciónAgonistmedicine.medical_specialtyHidrolasasmedicine.drug_classNeurogenesiseducation:Psychiatry and Psychology::Mental Disorders::Substance-Related Disorders::Alcohol-Related Disorders::Alcoholism [Medical Subject Headings]Subventricular zoneBiology:Phenomena and Processes::Physiological Phenomena::Nutritional Physiological Phenomena::Diet [Medical Subject Headings]:Anatomy::Nervous System::Central Nervous System::Brain::Prosencephalon::Telencephalon::Cerebrum::Cerebral Cortex::Hippocampus::Dentate Gyrus [Medical Subject Headings]lcsh:RC321-57103 medical and health sciencesCellular and Molecular NeuroscienceRatasInternal medicine:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Nerve Tissue Proteins::Tubulin [Medical Subject Headings]JWH133medicineGiro dentadolcsh:Neurosciences. Biological psychiatry. Neuropsychiatry030304 developmental biologyCélulas madre nerviosas:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Endocannabinoids [Medical Subject Headings]Dentate gyrusmarcadores genéticosCB2 receptor:Chemicals and Drugs::Carbohydrates::Polysaccharides::Oligosaccharides::Disaccharides::Sucrose [Medical Subject Headings]:Anatomy::Nervous System::Central Nervous System::Brain::Prosencephalon::Diencephalon::Hypothalamus [Medical Subject Headings]:Chemicals and Drugs::Organic Chemicals::Alcohols::Ethanol [Medical Subject Headings]Endocrinology:Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Rodentia::Muridae::Murinae::Rats [Medical Subject Headings]nervous system:Psychiatry and Psychology::Behavior and Behavior Mechanisms::Behavior::Drinking Behavior::Alcohol Drinking [Medical Subject Headings]:Chemicals and Drugs::Organic Chemicals::Amides::Benzamides [Medical Subject Headings]030217 neurology & neurosurgeryHipotálamoNeuroscience
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Cumyl-PEGACLONE: A comparatively safe new synthetic cannabinoid receptor agonist entering the NPS market?

2018

AdultMalePharmaceutical SciencePharmacology01 natural sciencesAnalytical ChemistryDesigner Drugs03 medical and health sciencesYoung Adult0302 clinical medicineEnvironmental ChemistryMedicineHumans030216 legal & forensic medicineSpectroscopyCannabinoid Receptor AgonistsPsychotropic Drugsbusiness.industryIllicit Drugs010401 analytical chemistrySynthetic cannabinoid receptor agonistMiddle Aged0104 chemical sciencesSubstance Abuse DetectionSubstance Abuse DetectionFemalebusinessCarbolinesDrug testing and analysis
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Cannabinoid and nitric oxide signaling interplay in the modulation of hippocampal hyperexcitability: study on electrophysiological and behavioral mod…

2015

A growing bulk of evidence suggests that cannabinoid system plays a pivotal role in the control of hyperexcitability phenomena. Notwithstanding, the anticonvulsant action of cannabinoids has not been fully addressed, in particular the involvement of potential cellular neuromodulators, for instance nitric oxide. In the current study, we focused on two distinct rat models of temporal lobe epilepsy, the Maximal Dentate Activation and the pilocarpine-induced acute seizures, providing both electrophysiological and behavioral data on cannabinoid and nitrergic system interplay. We evaluated the antiepileptic effects of WIN 55,212-2, (R)-(+)-[2,3-dihydro-5-methyl-3-(4- morpholinylmethyl) pyrrolo[1,…

AgonistAM251MaleCannabinoid receptorIndazolesmedicine.drug_classmedicine.medical_treatmentMorpholinesHippocampusPharmacologyNaphthalenesNitric OxideHippocampusSettore BIO/09 - FisiologiaEpilepsyPiperidinesReceptor Cannabinoid CB1medicineAnimalshippocampus temporal lobe epilepsy cannabinoids behavior percentage of protection electrophysiology.Rats WistarWIN 55212-2Cannabinoid Receptor AgonistsDose-Response Relationship DrugCannabinoidsGeneral NeurosciencePilocarpinemedicine.diseaseEndocannabinoid systemBenzoxazinesRatsDisease Models AnimalEpilepsy Temporal LobePyrazolesCannabinoidNitric Oxide SynthasePsychologyNeurosciencemedicine.drug
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Effects of Cannabinoid Exposure during Adolescence on the Conditioned Rewarding Effects of WIN 55212-2 and Cocaine in Mice: Influence of the Novelty-…

2016

Adolescent exposure to cannabinoids enhances the behavioural effects of cocaine, and high novelty-seeking trait predicts greater sensitivity to the conditioned place preference (CPP) induced by this drug. Our aim was to evaluate the influence of novelty-seeking on the effects of adolescent cannabinoid exposure. Adolescent male mice were classified as high or low novelty seekers (HNS and LNS) in the hole-board test. First, we evaluated the CPP induced by the cannabinoid agonist WIN 55212-2 (0.05 and 0.075 mg/kg, i.p.) in HNS and LNS mice. Then, HNS and LNS mice were pretreated i.p. with vehicle, WIN 55212-2 (0.1 mg/kg), or cannabinoid antagonist rimonabant (1 mg/kg) and were subsequently con…

AgonistMaleArticle Subjectmedicine.drug_classmedicine.medical_treatmentmedia_common.quotation_subjectMorpholinesConditioning ClassicalPharmacologyNaphthaleneslcsh:RC321-57103 medical and health sciencesMice0302 clinical medicineRimonabantCocaineRewardmedicineAnimalslcsh:Neurosciences. Biological psychiatry. Neuropsychiatrymedia_commonCannabinoid Receptor AgonistsAddictionAntagonistNovelty seekingCannabinoid Receptor AgonistsConditioned place preference030227 psychiatryBenzoxazinesNeurologyExploratory BehaviorNeurology (clinical)CannabinoidPsychologyCorrigendum030217 neurology & neurosurgeryResearch Articlemedicine.drugNeural plasticity
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Role of CB2 receptors and cGMP pathway on the cannabinoid-dependent antiepileptic effects in an in vivo model of partial epilepsy.

2014

This study aimed at providing an insight on the possible role of cannabi-noid (CB) type 2 receptors (CB2R) and cGMP pathway in the antiepileptic activity ofWIN 55,212-2, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-Yl]-1-naphthalenylmethanone, a non-selective CB agonist, in the maximal dentate activation (MDA) model of partial epilepsy in adult male rats. We evaluated the activity of a CB2 antagonist/inverse agonist AM630, [6-iodo-2-methyl-1-[2-(4-morpholinyl)ethyl]-1H-indol-3-yl](4-methoxyphenyl)methanone or 6-iodopravadoline, alone or in co-administration with WIN 55,212-2. Also, in the MDA model it was investigated the co-treatment of WIN55,212…

AgonistMaleIndolessGCmedicine.drug_classmedicine.medical_treatmentMorpholinesPharmacologyNaphthalenesSettore BIO/09 - FisiologiaHippocampusNitric oxideReceptor Cannabinoid CB2chemistry.chemical_compoundHippocampumedicineCannabinoid receptor type 2Inverse agonistAnimalsRats WistarReceptorCannabinoidCannabinoid Receptor AntagonistsCyclic GMPCannabinoid Receptor AgonistsElectrophysiology.ChemistryAntagonistElectric StimulationBenzoxazinesDisease Models AnimalNeurologyGuanylate CyclaseAnticonvulsantsNeurology (clinical)CannabinoidEpilepsies PartialSoluble guanylyl cyclaseTemporal Lobe Epilepsy AM630Epilepsy research
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CB1 cannabinoid receptor-mediated aggressive behavior

2013

This 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). Gene expression analyses of monoaminooxidase-A (MAO-A), catechol-o-methyl-transferase (COMT), 5-hydroxytriptamine transporter (5-HTT) and 5-HT1B serotonergic receptor (5HT1Br) in the median and dorsal raphe nuclei (MnR and DR, respectively) and in the amygdala (AMY) were performed by real time-PCR. Double immunohistochemistry studies evaluated COMT and CB1r co-localization in the raphe nuclei and in the cortical (AC…

AgonistMalemedicine.medical_specialtyCannabinoid receptorTime Factorsmedicine.drug_classmedicine.medical_treatmentPoison controlArachidonic AcidsSerotonergicCatechol O-MethyltransferaseAmygdalaCellular and Molecular NeuroscienceMiceDorsal raphe nucleusReceptor Cannabinoid CB1Internal medicinemedicineAnimalsInterpersonal RelationsMonoamine OxidasePharmacologyCannabinoid Receptor AgonistsMice KnockoutSerotonin Plasma Membrane Transport ProteinsAmygdalaSurgeryAggressionmedicine.anatomical_structureEndocrinologynervous systemGene Expression RegulationImpulsive BehaviorReceptor Serotonin 5-HT1BConditioning OperantRaphe NucleiCannabinoidRaphe nucleiPsychologyReinforcement Psychology
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WIN55,212-2, a cannabinoid receptor agonist, protects against nigrostriatal cell loss in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine mouse model…

2009

Parkinson's disease (PD) is characterized by the progressive loss of nigrostriatal dopamine neurons leading to motor disturbances and cognitive impairment. Current pharmacotherapies relieve PD symptoms temporarily but fail to prevent or slow down the disease progression. In this study, we investigated the molecular mechanisms by which the non-selective cannabinoid receptor agonist WIN55,212-2 (WIN) protects mouse nigrostriatal neurons from 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurotoxicity and neuroinflammation. Stereological analyses showed that chronic treatment with WIN (4 mg/kg, intraperitoneal), initiated 24 h after MPTP administration, protected against MPTP-ind…

Agonistmedicine.drug_classbusiness.industryPars compactaGeneral NeuroscienceMPTPCannabinoid Receptor AgonistsSubstantia nigraPharmacologynervous system diseaseschemistry.chemical_compoundnervous systemchemistryDopaminemedicineCannabinoid receptor type 2MPTP Poisoninglipids (amino acids peptides and proteins)businessmedicine.drugEuropean Journal of Neuroscience
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Cannabinoid CB1 receptor activation modulates spontaneous contractile activity in mouse ileal longitudinal muscle.

2007

The purpose of the present study was to examine whether cannabinoid receptor agonists influence spontaneous contractile activity of longitudinal muscle in mouse ileum in vitro. Isolated segments of mouse ileum displayed spontaneous contractions with an amplitude and frequency of about 300 mg and 30 cpm, respectively. The endocannabinoid anandamide (1-100 microM), the selective cannabinoid CB(1) receptor agonist, ACEA (0.1 microM-10 microM), but not the selective cannabinoid CB(2) receptor agonist, JWH 133 (0.1 microM-10 microM), reduced in a concentration-dependent manner the spontaneous mechanical activity. The inhibitory effect consisted in a decrease of the mean amplitude of longitudinal…

AtropineMaleAgonistmedicine.medical_specialtyCB1 receptorIndolesCannabinoid receptorPolyunsaturated Alkamidesmedicine.drug_classmedicine.medical_treatmentMouse ileumArachidonic AcidsTetrodotoxinIn Vitro TechniquesDepolarization-induced suppression of inhibitionHexamethoniumReceptor Cannabinoid CB2Micechemistry.chemical_compoundPiperidinesReceptor Cannabinoid CB1IleumInternal medicineCannabinoid Receptor ModulatorsmedicineAnimalsCannabinoidPharmacologyDose-Response Relationship DrugCannabinoidsChemistryMuscle SmoothCannabinoid Receptor AgonistsReceptor antagonistEndocannabinoid systemAcetylcholineMice Inbred C57BLNG-Nitroarginine Methyl EsterEndocrinologyApaminJWH-133PyrazolesCannabinoidRimonabantSpontaneous mechanical activityEndocannabinoidsMuscle Contraction
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Involvement of PAR-4 in Cannabinoid-Dependent Sensitization of Osteosarcoma Cells to TRAIL-Induced Apoptosis

2014

The synthetic cannabinoid WIN 55,212-2 is a potent cannabinoid receptor agonist with anticancer potential. Experiments were performed to determine the effects of WIN on proliferation, cell cycle distribution, and programmed cell death in human osteosarcoma MG63 and Saos-2 cells. Results show that WIN induced G2/M cell cycle arrest, which was associated with the induction of the main markers of ER stress (GRP78, CHOP and TRB3). In treated cells we also observed the conversion of the cytosolic form of the autophagosome marker LC3-I into LC3-II (the lipidated form located on the autophagosome membrane) and the enhanced incorporation of monodansylcadaverine and acridine orange, two markers of t…

AutophagosomeautophagyProgrammed cell deathCannabinoids ER stress autophagy TRAIL osteosarcoma cells GRP78/PAR-4 complex.Cannabinoid receptorMorpholinesCellApoptosisTRAILNaphthalenesBiologyGRP78/PAR-4 complex.Applied Microbiology and BiotechnologyTNF-Related Apoptosis-Inducing LigandCadaverineCell Line TumorSettore BIO/10 - BiochimicamedicineHumansRNA Small InterferingEndoplasmic Reticulum Chaperone BiPMolecular BiologyHeat-Shock ProteinsEcology Evolution Behavior and SystematicsCell ProliferationCannabinoid Receptor AgonistsOsteosarcomaCannabinoidsAutophagyCell Cycle Checkpointsosteosarcoma cellsCell BiologyCell cycleEndoplasmic Reticulum StressAcridine OrangeBenzoxazinesCell biologymedicine.anatomical_structureApoptosisAutophagosome membraneApoptosis Regulatory ProteinsER stressMicrotubule-Associated ProteinsResearch PaperDevelopmental Biology
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