Adenylate cyclaseAntagonistObserved in Chinese hamstInhibitProtein-coupled receptorsEndogenous cannabinoid1990Cholera toxinPsychoactiveMatsudaNicotinic ReceptorsEndocannabinoidsAnandamideNeuronsEndocannabinoid systemNeurotransmitter releaseSignaling pathwayPredominantlyInhibitionHeterodimersProteinsCNR1Cannabis plantPeripheralLigandsRegulationGABA1992DenselyGPCRModulatePathwaysStimulationFunctionalVivoActivityEffectsInteractionCAMPChemicalHumanComponentsCentralMainBodyStudies
Adenylate cyclase12
- Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis toxin-sensitive G-protein. (jneurosci.org)
- In this study we have examined the interactions of CB1 and D2 receptors on adenylate cyclase. (jneurosci.org)
- Both D1 and D2 dopamine receptors also couple to adenylate cyclase via G-proteins. (jneurosci.org)
- whereas dopamine D2 receptors inhibit adenylate cyclase via G i -proteins ( Sibley and Monsma, 1992 ). (jneurosci.org)
- Upon activation, CB1 receptor exhibits its effects mainly through activation of Gi, which decreases intracellular cAMP concentration by inhibiting its production enzyme, adenylate cyclase, and increases mitogen-activated protein kinase (MAP kinase) concentration. (wikipedia.org)
- Alternatively, in some rare cases CB1 receptor activation may be coupled to Gs proteins, which stimulate adenylate cyclase. (wikipedia.org)
- They inhibit adenylate cyclase activity in a dose-dependent, stereoselective, and pertussis toxin-sensitive manner. (dimabio.cn)
- Recent evidence, however, has supported a mechanism involving a G protein-coupled receptor found in brain and neural cell lines, and which inhibits adenylate cyclase activity in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. (plantpeople.co)
- Stimulation of postsynaptic GABA B receptors generally triggers inhibition of adenylate cyclase and activation of G protein-gated inwardly rectifying K + (GIRK/Kir3) channels, leading to cell hyperpolarisation (Kaupmann et al. (springer.com)
- ATCC CRL 1476) exhibited low levels of beta-adrenergic receptors as determined by specific binding of [125I]cyanopindolol ([125I]CYP) and marginal stimulation of adenylate cyclase in plasma membranes by (-)isoproterenol. (shengsci.com)
- Regulation of adenylate cyclase by cannabinoid drugs. (shengsci.com)
- The abilities of lipophilic cannabinoid drugs to regulate adenylate cyclase activity in neuroblastoma cell membranes were analyzed by thermodynamic studies. (shengsci.com)
Antagonist4
- This augmentation was blocked by the CB1 receptor antagonist SR141716A or the D2 antagonist sulpride. (jneurosci.org)
- Anandamide decreased the maximal nicotine-induced responses without significantly affecting its potency, indicating that it acts as a noncompetitive antagonist on nicotinic acetylcholine (nACh) a 7 receptors. (uaeu.ac.ae)
- Baicalin significantly increased the adipocyte response to physiological and pharmacological lipolytic stimuli (such as epinephrine - adrenergic agonist, DPCPX - adenosine A1 receptor antagonist, and amrinone - cAMP phosphodiesterase inhibitor). (bvsalud.org)
- Such effect was completely reversed both by the opioid receptor antagonist naloxone and by the unselective muscarinic receptor antagonist atropine. (researchgate.net)
Observed in Chinese hamst1
- Similar augmentation of cAMP accumulation after pertussis toxin treatment was observed in Chinese hamster ovary (CHO) cells transfected with, and stably expressing, the CB1 receptor. (jneurosci.org)
Inhibit3
- Previously, CB1 receptors have been shown to inhibit D1 receptor-mediated cAMP accumulation ( Bidaut-Russell and Howlett, 1991 ). (jneurosci.org)
- The CB1 receptor is expressed pre-synaptically at both glutaminergic and GABAergic interneurons and, in effect, acts as a neuromodulator to inhibit release of glutamate and GABA. (wikipedia.org)
- specifically, evidence showing that cannabinoids inhibit neuroinflammation and that immune cells express the entire machinery that constitutes a functional cannabinoid signaling system. (420magazine.com)
Protein-coupled receptors6
- Cannabinoids exert many of their effects through activation of G i -protein-coupled receptors. (jneurosci.org)
- The CB1 receptor shares the structure characteristic of all G-protein-coupled receptors, possessing seven transmembrane domains connected by three extracellular and three intracellular loops, an extracellular N-terminal tail, and an intracellular C-terminal tail. (wikipedia.org)
- The receptor may exist as a homodimer or form heterodimers or other GPCR oligomers with different classes of G-protein-coupled receptors. (wikipedia.org)
- The cannabinoid receptors are members of family 1 of the G-protein-coupled receptors. (dimabio.cn)
- Two cannabinoid G protein-coupled receptors have been cloned thus far, CB1 receptors (Matsuda et al. (420magazine.com)
- GABA B receptors are the G protein-coupled receptors for GABA, the main inhibitory neurotransmitter in the brain, and through coupling to different intracellular signal transduction mechanisms they mediate slow inhibitory postsynaptic potentials (IPSPs) (Bettler et al. (springer.com)
Endogenous cannabinoid3
- The effect of the endogenous cannabinoid ligand anandamide on the function of the cloned α 7 subunit of the nicotinic acetylcholine (ACh) receptor expressed in Xenopus oocytes was investigated by using the two-electrode voltage-clamp technique. (uaeu.ac.ae)
- In conclusion, these results demonstrate that the endogenous cannabinoid anandamide inhibits the function of nACh α 7 receptors expressed in Xenopus oocytes in a cannabinoid receptor-independent and non-competitive manner. (uaeu.ac.ae)
- This review discusses the anti-inflammatory properties of cannabinoid compounds at molecular, cellular and whole animal levels, first by examining the evidence for anti-inflammatory effects of cannabinoids obtained using in vivo animal models of clinical neuroinflammatory conditions, specifically rodent models of multiple sclerosis, and second by describing the endogenous cannabinoid (endocannabinoid) system components in immune cells. (420magazine.com)
19902
- 1990). The individual cannabinoid CB1 and CB2 receptor cDNA had been portrayed stably in CHO cells as defined previously (Felder et al. (rue2011.com)
- 1990), expressed primarily by neurons, and CB2 receptors (Munro et al. (420magazine.com)
Cholera toxin1
- Treatment of the pertussis toxin-treated cells with cholera toxin before CB1 receptor activation amplified the stimulatory pathway, suggesting that this response was mediated through a G s -type G-protein. (jneurosci.org)
Psychoactive2
- The cannabinoid delta-9-tetrahydrocannabinol is the principal psychoactive ingredient of marijuana. (dimabio.cn)
- Also, the receptor is more responsive to psychoactive cannabinoids than to non-psychoactive cannabinoids. (plantpeople.co)
Matsuda1
- Dr. Matsuda was the first person to accurately describe the structure and function of the CB1 and CB2 receptors. (plantpeople.co)
Nicotinic Receptors1
- Inhibitors of enzymes involved in anandamide metabolism including phenylmethylsulfonyl fluoride, superoxide dismutase, and indomethacin, or the anandamide transport inhibitor AM404 did not prevent anandamide inhibition of nicotinic responses, suggesting that anandamide itself acted on nicotinic receptors. (uaeu.ac.ae)
Endocannabinoids2
- The CB1 receptor is activated by cannabinoids, generated naturally inside the body (endocannabinoids) or exogenously, normally through cannabis or a related synthetic compound. (wikipedia.org)
- Endocannabinoids released by a depolarized neuron bind to CB1 receptors on pre-synaptic glutamatergic and GABAergic neurons, resulting in a respective decrease in either glutamate or GABA release. (wikipedia.org)
Anandamide3
- The primary endogenous agonist of the human CB1 receptor is anandamide. (wikipedia.org)
- In addition, inhibition of nicotinic responses by anandamide was not sensitive to either pertussis toxin treatment or to the membrane permeable cAMP analog 8-Br-cAMP (0.2 mM). (uaeu.ac.ae)
- Following the cloning of CB1 and CB2 receptors, two endocannabinoid ligands were identified and characterized: arachidonoylethanolamide (anandamide) (Devane et al. (420magazine.com)
Neurons7
- Within the striatum, CB1 receptors have been shown to be localized on the same neurons as G i -coupled dopamine D2 receptors. (jneurosci.org)
- In striatal neurons in primary culture, both the CB1 receptor agonist [3-(1,1-dimethylheptyl)-11-hydroxy-Δ 8 tetrahydrocannabinol] (HU210) and the D2 receptor agonist quinpirole inhibited forskolin-stimulated cAMP accumulation when applied separately. (jneurosci.org)
- Pertussis toxin treatment of striatal neurons prevented the inhibition of cAMP accumulation by D2 receptors but unmasked a cannabinoid receptor-mediated stimulatory effect on cAMP accumulation. (jneurosci.org)
- CB1 receptors have been identified on both subpopulations of medium spiny neurons ( Mailleux and Vanderhaeghen, 1992 ). (jneurosci.org)
- 1992). treatment of striatal neurons prevented the inhibition of cAMP accumulation by D2 receptors but unmasked a cannabinoid receptor-mediated stimulatory effect on cAMP deposition. (rue2011.com)
- In situ hybridization and immunohistochemical studies have shown that Purkinje cells (PCs), the output neurons of the cerebellar cortex, are the neuron type with the highest levels of GABA B receptors (Bowery et al. (springer.com)
- RESEARCH:5-HT1A (Serotonin-1A) receptor gene regulation and mental illness:Hypothesis: Down-regulation of the 5-HT1A receptor gene in serotonin neurons is required for the antidepressant actions of therapeutic compounds. (vdocuments.net)
Endocannabinoid system3
- Since then, in-depth research on the endocannabinoid system (ECS) has broadened our understanding of how and why cannabinoids such as THC and CBD interact with the human body. (plantpeople.co)
- Cannabinoids are chemical compounds capable of attaching to and activating the ECS receptors spread throughout the endocannabinoid system. (plantpeople.co)
- Cannabinoids support the endocannabinoid system, commonly referred to as the ECS, for short. (nanocraftcbd.com)
Neurotransmitter release1
- The CB1 receptor is a pre-synaptic heteroreceptor that modulates neurotransmitter release when activated in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. (wikipedia.org)
Signaling pathway2
- Stimulation of cAMP accumulation was not observed after pertussis toxin treatment of CHO cells expressing the human CB2 receptor, suggesting that this novel signaling pathway is unique to the cannabinoid CB1 receptor. (jneurosci.org)
- Arousal of cAMP deposition was not noticed after pertussis toxin treatment of CHO cells expressing the individual CB2 receptor, recommending that this book signaling pathway is exclusive towards the cannabinoid CB1 receptor. (rue2011.com)
Predominantly1
- Aside from these two receptors, evidence exists supporting the presence of yet uncloned cannabinoid receptors, a hypothesis predominantly based on pharmacological activity of cannabinoid compounds in CB1 and CB2 receptor-deficient mice or following the administration of 'selective' CB1 and CB2 receptor antagonists (Jarai et al. (420magazine.com)
Inhibition1
- This inhibition grows more pronounced when considered with the effect of activated CB1 receptors to limit calcium entry into the cell, which does not occur through cAMP but by a direct G-protein-mediated inhibition. (wikipedia.org)
Heterodimers1
- Functional GABA B receptors are obligate heterodimers composed of GABA B1 and GABA B2 subunits, and they are implicated in a number of disorders, including cognitive impairments, nociception, anxiety, depression and epilepsy (Bettler et al. (springer.com)
Proteins5
- Research suggests that the majority of CB1 receptors are coupled through Gi/o proteins. (wikipedia.org)
- The proteins encoded by this gene and the cannabinoid receptor 1 (brain) (CNR1) gene have the characteristics of a guanine nucleotide-binding protein (G-protein)-coupled receptor for cannabinoids. (dimabio.cn)
- These proteins have been found to be involved in the cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana. (dimabio.cn)
- Coupled with influx of extracellular calcium, Rut produced the endothelium-dependent vasorelaxant effect by activation of endothelium NOS and release of NO without pertussis toxin-sensitive Gi protein and other G proteins or phospholipase C activation being involved [ 8 ]. (biomedcentral.com)
- Understanding the proteins that regulate the 5-HT1A promoter will lead to insights on receptor regulation and provide new therapeutic targets relevant to depression, anxiety, obsessive compulsive disorder and other mental illnesses. (vdocuments.net)
CNR12
- Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. (wikipedia.org)
- The CB1 receptor is encoded by the gene CNR1, located on human chromosome 6. (wikipedia.org)
Cannabis plant2
- 2003). Here cannabinoids are defined as ingredients of the cannabis plant or other compounds that bind to and activate cannabinoid receptors, and Table 1 summarizes their pharmacological properties. (420magazine.com)
- Kind of like a pyramid, the cannabinoids flow down, from the cannabis plant. (nanocraftcbd.com)
Peripheral2
- The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. (wikipedia.org)
- During the process, they discovered a complex network of cannabinoid receptors in the central and peripheral nervous systems. (plantpeople.co)
Ligands1
- The CB1 receptor can also be allosterically modulated by synthetic ligands in a positive and negative manner. (wikipedia.org)
Regulation1
- However, the combination of EPI with bisphenols altered expression of genes associated with inflammation, cell stress, DNA damage, regulation of nuclear hormone receptor activity, cell cycle, mitochondrial function, primary ciliogenesis, and lipid metabolism in blubber. (bvsalud.org)
GABA6
- Metabotropic GABA B receptors mediate slow inhibitory effects presynaptically and postsynaptically through the modulation of different effector signalling pathways. (springer.com)
- Here, we analysed the distribution of GABA B receptors using highly sensitive SDS-digested freeze-fracture replica labelling in mouse cerebellar Purkinje cells. (springer.com)
- To understand the spatial relationship of GABA B receptors with two key effector ion channels, the G protein-gated inwardly rectifying K + (GIRK/Kir3) channel and the voltage-dependent Ca 2+ channel, biochemical and immunohistochemical approaches were performed. (springer.com)
- Co-immunoprecipitation analysis demonstrated that GABA B receptors co-assembled with GIRK and Ca V 2.1 channels in the cerebellum. (springer.com)
- Thus, GABA B receptors are associated with GIRK and Ca V 2.1 channels in different subcellular compartments. (springer.com)
- These data provide a better framework for understanding the different roles played by GABA B receptors and their effector ion channels in the cerebellar network. (springer.com)
19921
- 1992). CHO cells expressing the D2 receptor were provided generously by Dr stably. (rue2011.com)
Densely1
- CB1 receptors are expressed most densely in the central nervous system and are largely responsible for mediating the effects of cannabinoid binding in the brain. (wikipedia.org)
GPCR1
- G-protein receptor kinases (GRKs) help terminate GPCR signaling through receptor desensitization and downregulation and also modulate signaling via phosphorylation-independent functions. (hellobio.com)
Modulate1
- Growing evidence suggests that a major physiological function of the cannabinoid signaling system is to modulate neuroinflammation. (420magazine.com)
Pathways1
- The action on lipolysis is glucose-independent and covers both the adrenergic and adenosine A1 receptor pathways. (bvsalud.org)
Stimulation1
- This stimulation of cAMP was not Ca 2+ -sensitive and was unaffected by a range of protein kinase inhibitors. (jneurosci.org)
Functional1
- Induction of functional beta-adrenergic receptors in rat aortic smooth muscle cells by sodium butyrate. (shengsci.com)
Vivo1
- The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB1 receptors in the human brain with positron emission tomography. (wikipedia.org)
Activity1
- In summary, CB1 receptor activity has been found to be coupled to certain ion channels, in the following manner: Positively to inwardly rectifying and A-type outward potassium channels. (wikipedia.org)
Effects2
- Our aim is to identify immune functions modulated by cannabinoids that could account for their anti-inflammatory effects in these animal models. (420magazine.com)
- In order to understand the anti-inflammatory potential of cannabinoids in clinical neuroinflammation, it is necessary to examine their anti-inflammatory effects in animal models. (420magazine.com)
Interaction3
- However, an interaction between D2 and CB1 receptors has not been established. (jneurosci.org)
- The signaling properties of activated CB1 are furthermore modified by the presence of SGIP1, that hinders receptor internalization and decreases ERK1/2 signalling while augmenting the interaction with GRK3, β-arrestin-2. (wikipedia.org)
- Inflammation is a protective physiological response of an organism to chemical, physical, infectious agents, environmental toxins, ischemia or an antigen-antibody interaction. (biomedcentral.com)
CAMP2
- The cannabinoid receptor-stimulated accumulation of cAMP was blocked in a concentration-dependent manner by SR141716A, suggesting that the response was regulated through the CB1 receptor. (jneurosci.org)
- The cannabinoid receptor-stimulated deposition of cAMP was obstructed within a concentration-dependent way by SR141716A, recommending which the response was controlled through the CB1 receptor. (rue2011.com)
Chemical1
- Their unique chemical structures, receptors, and bioactions are being elucidated. (frontiersin.org)
Human2
- Four wild-type (drug-sensitive) human breast cancer cell lines (MCF-7, T47D,MDA-MB-231, MDA-MB-435) were used to evaluate the influence of acute and chronic exposure to ceramide and ceramide metabolites on MDR1 mRNA,P-gp, and resistance to chemotherapeutic agents. (sphingolipidclub.com)
- regulators of the rat and human 5-HT1A receptor genes using luciferase reporter fusion constructs transfected in cell lines. (vdocuments.net)
Components1
- Many cell types involved in this process express components of the cannabinoid signaling system that can be endogenously or pharmacologically controlled. (420magazine.com)
Central1
- We chose to focus on MS because it is characterized by relapsing-remitting and chronic inflammation in the central nervous system (CNS), and cannabinoids have been shown to affect its pathogenesis. (420magazine.com)
Main1
- Our ECS has two main receptors that take care of business: cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2). (nanocraftcbd.com)
Body1
- They were amazed to learn that this system wasn't isolated, but rather comprised of a network of ECS receptors distributed throughout the entire body. (plantpeople.co)
Studies1
- 1995). There are notable studies showing the anti-inflammatory properties of cannabinoid-like compounds, such as Δ9-tetrahydrocannabinol (THC) metabolites and the endogenous compound palmitoylethanolamide. (420magazine.com)