Receptor, Cannabinoid, CB1
Receptor, Cannabinoid, CB2
Receptors, Cannabinoid
A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.
Cannabinoids
Cannabinoid Receptor Modulators
Pyrazoles
Cannabinoid Receptor Agonists
Dronabinol
Endocannabinoids
Cyclohexanols
Polyunsaturated Alkamides
Amides composed of unsaturated aliphatic FATTY ACIDS linked with AMINES by an amide bond. They are most prominent in ASTERACEAE; PIPERACEAE; and RUTACEAE; and also found in ARISTOLOCHIACEAE; BRASSICACEAE; CONVOLVULACEAE; EUPHORBIACEAE; MENISPERMACEAE; POACEAE; and SOLANACEAE. They are recognized by their pungent taste and for causing numbing and salivation.
Cannabinoid Receptor Antagonists
Naphthalenes
Receptors, Drug
Drug Inverse Agonism
Monoacylglycerol Lipases
Cannabis
Dose-Response Relationship, Drug
Rats, Sprague-Dawley
Hallucinogens
Drugs capable of inducing illusions, hallucinations, delusions, paranoid ideations, and other alterations of mood and thinking. Despite the name, the feature that distinguishes these agents from other classes of drugs is their capacity to induce states of altered perception, thought, and feeling that are not experienced otherwise.
Croton Oil
Carbamates
Derivatives of carbamic acid, H2NC(=O)OH. Included under this heading are N-substituted and O-substituted carbamic acids. In general carbamate esters are referred to as urethanes, and polymers that include repeating units of carbamate are referred to as POLYURETHANES. Note however that polyurethanes are derived from the polymerization of ISOCYANATES and the singular term URETHANE refers to the ethyl ester of carbamic acid.
TRPV Cation Channels
Self Administration
Guanosine 5'-O-(3-Thiotriphosphate)
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
Rats, Wistar
Indoles
Analgesics, Non-Narcotic
Catalepsy
A condition characterized by inactivity, decreased responsiveness to stimuli, and a tendency to maintain an immobile posture. The limbs tend to remain in whatever position they are placed (waxy flexibility). Catalepsy may be associated with PSYCHOTIC DISORDERS (e.g., SCHIZOPHRENIA, CATATONIC), nervous system drug toxicity, and other conditions.
Ligands
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Conditioning, Operant
Mice, Knockout
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
Anisoles
Neurons
Brain
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
Hyperalgesia
Receptors, Opioid, mu
Heroin
Periaqueductal Gray
Radioligand Assay
Drug Tolerance
Progressive diminution of the susceptibility of a human or animal to the effects of a drug, resulting from its continued administration. It should be differentiated from DRUG RESISTANCE wherein an organism, disease, or tissue fails to respond to the intended effectiveness of a chemical or drug. It should also be differentiated from MAXIMUM TOLERATED DOSE and NO-OBSERVED-ADVERSE-EFFECT LEVEL.
Injections, Intraperitoneal
Psychotropic Drugs
Pain
Hippocampus
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
Synaptic Transmission
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
Alkanesulfonates
Corpus Striatum
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
Calcium Channel Blockers
Drug Interactions
CHO Cells
Pyrrolidinones
Substance Withdrawal Syndrome
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Disease Models, Animal
Nucleus Accumbens
Collection of pleomorphic cells in the caudal part of the anterior horn of the LATERAL VENTRICLE, in the region of the OLFACTORY TUBERCLE, lying between the head of the CAUDATE NUCLEUS and the ANTERIOR PERFORATED SUBSTANCE. It is part of the so-called VENTRAL STRIATUM, a composite structure considered part of the BASAL GANGLIA.
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
Cocaine
An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.
Reward
Receptors, Presynaptic
Neuralgia
Adenosine A2 Receptor Antagonists
Pain Measurement
Receptor, Adenosine A2A
Amygdala
Inhibitory Postsynaptic Potentials
Morphine
Cricetinae
Analysis of Variance
Feeding Behavior
Receptors, G-Protein-Coupled
Reinforcement Schedule
Cricetulus
Cerebellum
The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.
Presynaptic Terminals
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
Cyclic AMP
Receptors, Dopamine D2
Marijuana Abuse
Rats, Long-Evans
An outbred strain of rats developed in 1915 by crossing several Wistar Institute white females with a wild gray male. Inbred strains have been derived from this original outbred strain, including Long-Evans cinnamon rats (RATS, INBRED LEC) and Otsuka-Long-Evans-Tokushima Fatty rats (RATS, INBRED OLETF), which are models for Wilson's disease and non-insulin dependent diabetes mellitus, respectively.
Patch-Clamp Techniques
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Inflammation
Excitatory Postsynaptic Potentials
Neural Inhibition
Analgesics, Opioid
Prefrontal Cortex
The rostral part of the frontal lobe, bounded by the inferior precentral fissure in humans, which receives projection fibers from the MEDIODORSAL NUCLEUS OF THE THALAMUS. The prefrontal cortex receives afferent fibers from numerous structures of the DIENCEPHALON; MESENCEPHALON; and LIMBIC SYSTEM as well as cortical afferents of visual, auditory, and somatic origin.
Peripheral Nervous System Diseases
Cells, Cultured
Ileum
Enzyme Inhibitors
Glutamic Acid
Immunohistochemistry
RNA, Messenger
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Cerebral Cortex
HEK293 Cells
Protein Binding
A critical role for the cannabinoid CB1 receptors in alcohol dependence and stress-stimulated ethanol drinking. (1/1474)
Although many people drink alcohol regularly, only some become addicted. Several studies have shown that genetic and environmental factors contribute to individual differences in the vulnerability to the effects of alcohol (Nestler, 2000; Kreek, 2001; Crabbe, 2002). Among the environmental factors, stress is perhaps the most important trigger for relapse after a period of abstinence (Koob and Nestler, 1997; Piazza and Le Moal, 1998; Koob and Le Moal, 2001; Weiss et al., 2001). Here we show that ethanol withdrawal symptoms were completely absent in cannabinoid CB1 receptor-deficient mice, although acute effects of ethanol and ethanol tolerance and preference were basically normal. Furthermore, foot-shock stress had no affect on alcohol preference in Cnr1-/- mice, although it induced a dramatic increase in Cnr1+/+ animals. These results reveal a critical role for the CB1 receptor in clinically important aspects of alcohol dependence and provide a rationale for the use of CB1 receptor antagonists in the treatment of alcohol addiction. (+info)Cannabinoid CB(1) receptor-mediated inhibition of hippocampal acetylcholine release is preserved in aged mice. (2/1474)
1. The cannabinoid CB(1) receptor inverse agonist/antagonist SR 141716 increases acetylcholine release in rodent hippocampus and improves memory in some experimental paradigms. Since drugs like SR 141716 may represent a novel class of cognition-enhancing drugs, we wanted to check whether the function of the CB(1) receptor is preserved during ageing. 2. Hippocampal and striatal slices from 2- to 3- and 24- to 28-month-old C57BL/6J mice were preincubated with [(3)H]-choline or [(3)H]-noradrenaline ([(3)H]-NA) and superfused. 3. The cannabinoid receptor agonist WIN 55212-2 inhibited, and SR 141716 facilitated, the electrically (3 Hz) evoked tritium overflow in hippocampal slices (preincubated with [(3)H]-choline) from young and aged mice to the same extent. The evoked overflow per se was less by 33% in slices from aged animals. 4. WIN 55212-2 and SR 141716 did not affect, but the muscarinic receptor agonist oxotremorine inhibited, the evoked (3 Hz) overflow in striatal slices (preincubated with [(3)H]-choline) from young and aged mice to the same extent. The evoked overflow per se tended to be less in slices from aged animals. 5. The evoked (0.3 Hz) overflow in hippocampal slices (preincubated with [(3)H]-NA) was not affected by WIN 55212-2 and SR 141716, but was inhibited by histamine (via H(3) receptors) in slices from young mice and, to a somewhat less extent, in slices from aged mice. The evoked overflow per se did not differ between age groups. 6. In conclusion, the function of the CB(1) receptor involved in the tonic inhibition of hippocampal acetylcholine release is preserved in aged mice. (+info)A3 adenosine and CB1 receptors activate a PKC-sensitive Cl- current in human nonpigmented ciliary epithelial cells via a G beta gamma-coupled MAPK signaling pathway. (3/1474)
(1) We examined A3 adenosine and CB1 cannabinoid receptor-coupled signaling pathways regulating Cl(-) current in a human nonpigmented ciliary epithelial (NPCE) cell line. (2) Whole-cell patch-clamp recordings demonstrated that the A3 receptor agonist, IB-MECA, activates an outwardly rectifying Cl(-)current (I(Cl,Aden)) in NPCE cells, which was inhibited by the adenosine receptor antagonist, CGS-15943 or by the protein kinase C (PKC) activator, phorbol 12,13 dibutyrate (PDBu). (3) Treatment of NPCE cells with pertussis-toxin (PTX), or transfection with the COOH-terminus of beta-adrenergic receptor kinase (ct-betaARK), inhibited I(Cl,Aden). The phosphatidyl inositol 3-kinase (PI3K) inhibitor, wortmannin, had no effect on I(Cl,Aden); however, the mitogen-activated protein kinase kinase (MEK) inhibitor, PD98059, inhibited I(Cl,Aden). (4) Reverse transcription-polymerase chain reaction experiments and immunocytochemistry confirmed mRNA and protein expression for the CB1 receptor in NPCE cells, and the CB1 receptor agonist, Win 55,212-2, activated a PDBu-sensitive Cl(-) current (I(Cl,Win)). (5) Transfection of NPCE cells with the human CB1 (hCB1) receptor, increased I(Cl,Win), consistent with increased receptor expression, and I(Cl,Win) in hCB1 receptor-transfected cells was decreased after application of a CB1 receptor inverse agonist, SR 141716. (6) Constitutive activity for CB1 receptors was not significant in NPCE cells as transfection with hCB1 receptors did not increase basal Cl(-) current, nor was basal current inhibited by SR 141716. (7) I(Cl,Win) was inhibited by PTX preincubation, by transfection with ct-betaARK and by the MEK inhibitor, PD98059, but unaffected by the PI3K inhibitor, wortmannin. (8) We conclude that both A3 and CB1 receptors activate a PKC-sensitive Cl(-) current in human NPCE cells via a G(i/o)/Gbetagamma signaling pathway, in a manner independent of PI3K but involving MAPK. (+info)Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor. (4/1474)
1 Two cannabinoid receptors, CB1 and CB2, have been identified. The CB1 receptor is preferentially expressed in brain, and the CB2 receptor in cells of leukocyte lineage. We identified the mRNA for the CB1 receptor in human neuroblastoma SH-SY5Y cells, and the mRNA and protein for the CB2 receptor in human microglia and THP-1 cells. 2 Delta(9)-and Delta(8)-tetrahydrocannabinol (THC) were toxic when added directly to SH-SY5Y neuroblastoma cells. The toxicity of Delta(9)- THC was inhibited by the CB1 receptor antagonist SR141716A but not by the CB2 receptor antagonist SR144528. The endogenous ligand anandamide was also toxic, and this toxicity was enhanced by inhibitors of its enzymatic hydrolysis. 3 The selective CB2 receptor ligands JWH-015 and indomethacin morpholinylamide (BML-190), when added to THP-1 cells before stimulation with lipopolysaccharide (LPS) and IFN-gamma, reduced the toxicity of their culture supernatants to SH-SY5Y cells. JWH-015 was more effective against neurotoxicity of human microglia than THP-1 cells. The antineurotoxic activity of JWH-015 was blocked by the selective CB2 receptor antagonist SR144528, but not by the CB1 receptor antagonist SR141716A. This activity of JWH-015 was synergistic with that of the 5-lipoxygenase (5-LOX) inhibitor REV 5901. 4 Cannabinoids inhibited secretion of IL-1beta and tumor necrosis factor-alpha (TNF-alpha) by stimulated THP-1 cells, but these effects could not be directly correlated with their antineurotoxic activity. 5 Specific CB2 receptor ligands could be useful anti-inflammatory agents, while avoiding the neurotoxic and psychoactive effects of CB1 receptor ligands such as Delta(9)-THC. (+info)Cannabinoid1 receptor in the dorsal vagal complex modulates lower oesophageal sphincter relaxation in ferrets. (5/1474)
Delta9-tetrahydrocannabinol (delta9-THC) is an effective anti-emetic; however, other potential gastrointestinal therapeutic effects of delta9-THC are less well-known. Here, we report a role of delta9-THC in a vago-vagal reflex that can result in gastro-oesophageal reflux, that is, gastric distension-evoked lower oesophageal sphincter (LOS) relaxation. Oesophageal, LOS and gastric pressures were measured using a miniaturized, manometric assembly in decerebrate, unanaesthetized ferrets.Gastric distension (30 ml) evoked LOS relaxation (70 +/- 8% decrease from baseline). Delta9-THC administered systemically (0.2 mg kg-1, iv.) or directly to the dorsal hindbrain surface (0.002 mg),significantly attenuated the nadir of the gastric distention-evoked LOS relaxation, and time to reach maximal response. Similar increases to maximal effect were observed after treatment with the cannabinoid receptor agonist WIN 55,212-2 (0.2 mg kg-1 iv.). The effect of systemic delta9-THC on gastric distention-evoked LOS relaxation was reversed by a selective cannabinoid1 (CBI) receptor antagonist, SR141617A (1 mg kg-1 i.v.). Since this reflex is vagally mediated, we used a CB1 receptor antiserum and immunocytochemistry to determine its distribution in ferret vagal circuitry. CBI receptor staining was present in cell bodies within the area postrema, nucleus tractus solitarius (NTS) and nodose ganglion. Intense terminal-like staining was noted within the NTS and dorsal motor vagal nucleus (DMN). Neither nodose ganglionectomy nor vagotomy altered the CB1 receptor terminal-like staining in the dorsal vagal complex. Retrogradely labelled gastric- or LOS-projecting DMN neurones did not express CBI receptors within their soma. Therefore, CBI receptor staining in the NTS and DMN is not due to primary vagal afferents or preganglionic neurones. These novel findings suggest that delta9-THC can modulate reflex LOS function and that the most likely site of action is via the CBI receptor within the NTS. This effect of delta9-THC may have implications in treatment of gastro-oesophageal reflux and other upper gut disorders. (+info)Cannabinoid receptor type 1 modulates excitatory and inhibitory neurotransmission in mouse colon. (6/1474)
The effects of cannabinoid receptor agonists and antagonists on smooth muscle resting membrane potentials and on membrane potentials following electrical neuronal stimulation in a myenteric neuron/smooth muscle preparation of wild-type and cannabinoid receptor type 1 (CB1)-deficient mice were investigated in vitro. Double staining for CB1 and nitric oxide synthase (neuronal) was performed to identify the myenteric CB1-expressing neurons. Focal electrical stimulation of the myenteric plexus induced a fast (f) excitatory junction potential (EJP) followed by a fast and a slow (s) inhibitory junction potential (IJP). Treatment of wild-type mice with the endogenous CB1 receptor agonist anandamide reduced EJP while not affecting fIJP and sIJP. EJP was significantly higher in CB1-deficient mice than in wild-type littermate controls, and anandamide induced no effects in CB1-deficient mice. N-arachidonoyl ethanolamide (anandamide), R-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3,-de]- 1,4-benzoxazin-6-yl]-1-naphtalenylmethanone, a synthetic CB1 receptor agonist, nearly abolished EJP and significantly reduced the fIJP in wild-type mice. N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazole-caroxa mide (SR141716A), a CB1-specific receptor antagonist, was able to reverse the agonist effects induced in wild-type mice. SR141716A, when given alone, significantly increased EJP in wild-type mice without affecting IJP in wild-type and EJP in CB1-deficient mice. Interestingly, SR141716A reduced fIJP in CB1-deficient mice. In the mouse colon, nitrergic myenteric neurons do not express CB1, implying that CB1 is expressed in cholinergic neurons, which is in line with the functional data. Finally, excitatory and inhibitory neurotransmission in the mouse colon is modulated by activation of CB1 receptors. The significant increase in EJP in CB1-deficient mice strongly suggests a physiological involvement of CB1 in excitatory cholinergic neurotransmission. (+info)Toxicological and structural features of organophosphorus and organosulfur cannabinoid CB1 receptor ligands. (7/1474)
Potent cannabinoid CB1 receptor ligands include anandamide [N-(2-hydroxyethyl)arachidonamide], Delta9-tetrahydrocannabinol, and 3H-CP 55,940 at the agonist site and selected organophosphorus esters (including some pesticides) and organosulfur compounds at a proposed closely coupled "nucleophilic" site. This study considers the toxicological and structural features of alkylfluorophosphonates, benzodioxaphosphorin oxides, alkanesulfonyl fluorides, and analogs acting at the nucleophilic site. Binding at the agonist site, using3H-CP 55,940 in assays with mouse brain membranes, is inhibited byO-isopropyl dodecylfluorophosphonate (compound 2), dodecanesulfonyl fluoride (compound 14) and dodecylbenzodioxaphosphorin oxide with IC50 values of 2-11 nM. Compounds 2 and 14 are also effectivein vivo, with 84% inhibition of mouse brain CB1 binding 4 h after intraperitoneal dosage at 30 mg/kg. Compound 14-inhibited CB1 in mouse brain requires about 3-4 days for recovery of 50% activity, suggesting covalent derivatization. Delayed toxicity (mortality in 0.3-5 days) from compounds 2, 14, and octanesulfonyl fluoride (18) is more closely associated with in vivo inhibition of brain neuropathy target esterase-lysophospholipase (NTE-LysoPLA) than with that of CB1 or acetylcholinesterase. NTE-LysoPLA inhibited by sulfonyl fluorides 14 and 18 cannot "age," a proposed requirement for NTE phosphorylated by organophosphorus-delayed neurotoxicants. Several octane- and dodecanesulfonamides with N-(2-hydroxyethyl) and other substituents based on anandamide give depressed mobility and recumbent posture in mice, but the effects do not correlate with potency for CB1 inhibition in vitro. Specific toxicological responses are not clearly associated with organophosphorus- or organosulfur-induced inhibition of the proposed CB1 nucleophilic site in mouse brain. On the other hand, the most potent CB1 inhibitors examined here are also NTE-LysoPLA inhibitors and cause delayed toxicity in mice. (+info)The cannabinoid system and immune modulation. (8/1474)
Studies on the effects of marijuana smoking have evolved into the discovery and description of the endocannabinoid system. To date, this system is composed of two receptors, CB1 and CB2, and endogenous ligands including anandamide, 2-arachidonoyl glycerol, and others. CB1 receptors and ligands are found in the brain as well as immune and other peripheral tissues. Conversely, CB2 receptors and ligands are found primarily in the periphery, especially in immune cells. Cannabinoid receptors are G protein-coupled receptors, and they have been linked to signaling pathways and gene activities in common with this receptor family. In addition, cannabinoids have been shown to modulate a variety of immune cell functions in humans and animals and more recently, have been shown to modulate T helper cell development, chemotaxis, and tumor development. Many of these drug effects occur through cannabinoid receptor signaling mechanisms and the modulation of cytokines and other gene products. It appears the immunocannabinoid system is involved in regulating the brain-immune axis and might be exploited in future therapies for chronic diseases and immune deficiency. (+info)
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Characterization of Cannabinoid Receptors - Current Protocols
Positive Allosteric Modulation of Cannabinoid Receptor Type 1 Suppresses Pathological Pain Without Producing Tolerance or...
2015 December Monthly Meeting
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Synergistic Effect between Maternal Infection and Adolescent Cannabinoid Exposure on Serotonin 5HT1A Receptor Binding in the...
Effects of cannabis
There are at least two types of cannabinoid receptors (CB1 and CB2). Most cannabinoids are lipophilic (fat soluble) compounds ... Pertwee RG (January 1997). "Pharmacology of cannabinoid CB1 and CB2 receptors". Pharmacology & Therapeutics. 74 (2): 129-80. ... Cannabinoids produce a "marked depression of motor activity" via activation of neuronal cannabinoid receptors belonging to the ... The binding of cannabinoids to cannabinoid receptors decrease adenylyl cyclase activity, inhibit calcium N channels, and ...
Voacamine
... exhibits cannabinoid CB1 receptor antagonistic activity. There is considerable confusion about the absolute ... "Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity". Bioorganic & Medicinal Chemistry Letters. ...
WIN 56,098
It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. Its activity at CB1 ... WIN 55,212-2 WIN 55,225 Howlett AC, Berglund B, Melvin LS (October 1995). "Cannabinoid Receptor Agonists and Antagonists". ... Cannabinoids, Aminoalkylindoles, WIN compounds, Morpholines, Anthracenes, All stub articles, Cannabinoid stubs). ...
N-Acylamides
Anandamide activates the cannabinoid receptors CB1 and CB2. FAAH knockout mice show increased anandamide levels in vivo and ... an orthologue of vertebrate cannabinoid receptors in the urochordate Ciona intestinalis". Gene. 302 (1-2): 95-101. doi:10.1016/ ... cannabinoid-receptor dependent behaviors including antinociception and anxiolysis. GPR18, GPR55, GPR92 have also been proposed ... An example of this is the lipid signaling system involving transient receptor potential channels (TRP), which interact with N- ...
RVD-Hpα
... of cannabinoid CB1 receptors. It is shown that pepcan-12 opposite acts as a potent CB2 cannabinoid receptor positive allosteric ... which was originally proposed to act as a selective agonist for the CB1 cannabinoid receptor. It is a 12-amino acid polypeptide ... "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proceedings of the National Academy of Sciences of the United ... Recently it was shown that RVD-Hpα (also called Pepcan-12) is a potent negative allosteric modulator at CB1 receptors, together ...
LY-320,135
January 1998). "LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of ... LY-320,135 is a drug used in scientific research which acts as a selective antagonist of the cannabinoid receptor CB1. It was ... Pertwee RG (February 2005). "Inverse agonism and neutral antagonism at cannabinoid CB1 receptors". Life Sciences. 76 (12): 1307 ... Cannabinoids, CB1 receptor antagonists, Benzofuran ethers at the benzene ring, Resorcinol ethers, Aromatic ketones, ...
Cannabinol
... is a mildly psychoactive cannabinoid that binds to the cannabinoid receptors with more selectivity for CB2 over CB1 found in ... CBN acts as a partial agonist at the CB1 receptors, but has a higher affinity to CB2 receptors; however, it has lower ... "Novel cannabinol probes for CB1 and CB2 cannabinoid receptors". Journal of Medicinal Chemistry. 43 (20): 3778-3785. doi:10.1021 ... Both THC and CBN activate the CB1 (Ki = 211.2 nM) and CB2 (Ki = 126.4 nM) receptors. It is metabolised to 11-OH-CBN, which is a ...
Hemopressin
It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors. Longer forms of hemopressin containing 2-3 ... May 2010). "The peptide hemopressin acts through CB1 cannabinoid receptors to reduce food intake in rats and mice". J. Neurosci ... December 2007). "Hemopressin is an inverse agonist of CB1 cannabinoid receptors". Proc. Natl. Acad. Sci. U.S.A. 104 (51): 20588 ... is also an agonist at CB1 cannabinoid receptors. Hemopressin is not an endogenous peptide but rather an extraction artefact [ ...
Drinabant
Cannabinoid receptor antagonist Lange JH, Kruse CG (2008). "Cannabinoid CB1 receptor antagonists in therapeutic and structural ... Reggio, Patricia H. (2009). "Toward the design of cannabinoid CB1 receptor inverse agonists and neutral antagonists". Drug ... Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly ... Lee HK, Choi EB, Pak CS (2009). "The current status and future perspectives of studies of cannabinoid receptor 1 antagonists as ...
Rimonabant
... is an inverse agonist of the cannabinoid CB1 receptor. Originally thought to be selective for the CB1 receptor, ... CB1 receptor antagonists, Chlorobenzenes, Piperidines, Pyrazoles, Withdrawn drugs, Cannabinoids, Mu-opioid receptor antagonists ... Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class. Rimonabant is ... Pi-Sunyer FX, Aronne LJ, Heshmati HM, Devin J, Rosenstock J (Feb 2006). "Effect of rimonabant, a cannabinoid-1 receptor blocker ...
GW-405,833
Clayton N, Marshall FH, Bountra C, O'Shaughnessy CT (April 2002). "CB1 and CB2 cannabinoid receptors are implicated in ... Cannabinoid stubs, Cannabinoids, Aminoalkylindoles, Benzoylindoles, Morpholines, Phenol ethers, Chlorobenzenes, CB2 receptor ... GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, ... Marriott KS, Huffman JW (2008). "Recent advances in the development of selective ligands for the cannabinoid CB(2) receptor". ...
GAT100
Cannabinoids, CB1 receptor antagonists, Isothiocyanates, All stub articles, Cannabinoid stubs). ... GAT100 is a negative allosteric modulator of the cannabinoid CB1 receptor. Org 27569 PSNCBAM-1 ZCZ-011 Kulkarni PM, Kulkarni AR ... June 2016). "Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100 ... January 2016). "Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s ...
Cannabidiol
... has low affinity for the cannabinoid CB1 and CB2 receptors, although it acts as an antagonist of CB1/CB2 agonists, ... which acts on the cannabinoid receptor type 1 (CB1) as a partial agonist, CBD instead is a negative allosteric modulator of CB1 ... Pertwee RG (January 2008). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9- ... Cannabidiol may be an antagonist of GPR55, a G protein-coupled receptor and putative cannabinoid receptor that is expressed in ...
NESS-0327
Cannabinoids, CB1 receptor antagonists, Hydrazides, Chloroarenes, Pyrazoles, Piperazines, All stub articles, Cannabinoid stubs) ... July 2003). "Synthesis and characterization of NESS 0327: a novel putative antagonist of the CB1 cannabinoid receptor". The ... August 2002). "Design, synthesis and biological activity of rigid cannabinoid CB1 receptor antagonists". Chemical & ... and more selective for the CB1 receptor over CB2, than the more commonly used ligand rimonabant, with a Ki at CB1 of 350fM (i.e ...
Endocannabinoid enhancer
323-. ISBN 978-981-4287-59-3. Bambico, Francis Rodriguez; Gobbi, Gabriella (2008). "The cannabinoid CB1 receptor and the ... Cannabinoid receptor Synthetic cannabinoid Cannabinoid receptor antagonist George I. Papakostas; Maurizio Fava (2010). ... v t e (Articles with short description, Short description matches Wikidata, Cannabinoids, Endocannabinoids, All stub articles, ...
List of psychedelic drugs
"Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor". British Journal of Pharmacology. 172 (20): ... "The pharmacology of cannabinoid receptors and their ligands: an overview". International Journal of Obesity. 30 (S1): S13-S18. ... Cannabis and cannabinoids : pharmacology, toxicology, and therapeutic potential. Grotenhermen, Franjo., Russo, Ethan. New York ... κ-opioid receptor agonist), the active constituent of Salvia divinorum sage Salvinorin B methoxymethyl ether†, a semi-synthetic ...
N-Acylethanolamine
... is an endogenous agonist of the cannabinoid receptors (CB1 and CB2), and the physiological ligand for the cannabinoid CB2 ... and the CB1 receptor binding remain similarly reduced after 2-4 weeks of abstinence, suggests an involvement of CB1 receptors ... Activation of CB1 cannabinoid receptors in NAc, are necessary and sufficient to express the rewarding properties of social ... The cannabinoid type 1 receptors (CB1) and their endogenous ligands, the endocannabinoids, present in peripheral organs, such ...
KIAA2013
This system is made up of cannabinoid receptors 1 and 2 (CB1 and CB2) as well as the various ligands and enzymes that interact ... Both cannabinoid receptors are labeled as class A G-Protein Coupled Receptors, and CB2 is highly expressed within the human ... Oyagawa CR, Grimsey NL (2021-01-01). Shukla AK (ed.). "Cannabinoid receptor CB1 and CB2 interacting proteins: Techniques, ... 2019). "Systematic Affinity Purification Coupled to Mass Spectrometry Identified p62 as Part of the Cannabinoid Receptor CB2 ...
2-Arachidonoylglycerol
January 1999). "Evidence that the cannabinoid CB1 receptor is a 2-arachidonoylglycerol receptor. Structure-activity ... an endogenous agonist of the CB1 receptor and the primary endogenous ligand for the CB2 receptor. It is an ester formed from ... "Analysis of cannabinoid receptor binding and mRNA expression and endogenous cannabinoid contents in the developing rat brain ... CB1 receptor agonists, Glycine receptor antagonists, Glycerol esters, Arachidonyl compounds). ...
Delta-8-Tetrahydrocannabinol
It is a partial agonist of CB1 and CB2 cannabinoid receptors with about half the potency of ∆9-THC in most but not all measures ... This may be because it binds differently to CB1, the cannabinoid receptor that regulates much of THC's mind-altering effect.[ ... 8-THC has been reported to have a Ki value of 44 ± 12 nM at the CB1 receptor and 44 ± 17 nM at the CB2 receptor. These values ... Pertwee RG (January 2008). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9- ...
Metamizole
Despite this, studies in animals have found that the CB1 cannabinoid receptor is not involved in the analgesia induced by ... Elmas P, Ulugol A (November 2013). "Involvement of cannabinoid CB1 receptors in the antinociceptive effect of dipyrone". ... The result is a pair of cannabinoid and NSAID arachidonic acid conjugates[clarification needed] (although not in the strict ...
AM-251 (drug)
AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are ... CB1 receptor antagonists, Piperidines, Pyrazoles, Hydrazides, Iodoarenes, Chloroarenes, AM cannabinoids, Pyrazolecarboxamides, ... Discovery and development of Cannabinoid Receptor 1 Antagonists Lan R, Liu Q, Fan P, Lin S, Fernando SR, McCallion D, et al. ( ... The resulting compound exhibits slightly better binding affinity for the CB1 receptor (with a Ki value of 7.5 nM) than ...
AM-694
It is used in scientific research for mapping the distribution of CB1 receptors. AM-694 is an agonist for cannabinoid receptors ... a CB1 cannabinoid receptor ligand". Journal of Labelled Compounds and Radiopharmaceuticals. 46 (9): 799-804. doi:10.1002/jlcr. ... is a designer drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. ... AM-679 AM-1235 AM-2201 AM-2232 AM-2233 FUBIMINA JWH-018 List of AM cannabinoids List of JWH cannabinoids THJ-2201 Willis PG, ...
ZCZ-011
December 2015). "A Cannabinoid CB1 Receptor-Positive Allosteric Modulator Reduces Neuropathic Pain in the Mouse with No ... ZCZ-011 is a positive allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 PSNCBAM-1 Poklis JL, Clay DJ, ... June 2015). "HPLC-MS-MS Determination of ZCZ-011, A Novel Pharmacological Tool for Investigation of the Cannabinoid Receptor in ... Cannabinoids, Tryptamines, All stub articles, Cannabinoid stubs). ...
PTI-1
March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & ... heterocycle derivatives as agonists of the cannabinoid CB1 receptor.", issued 20 April 2010, assigned to Organon NV US 7763732 ... PTI-1 (SGT-48) is an indole-based synthetic cannabinoid. It is one of few synthetic cannabinoids containing a thiazole group ... Cannabinoids, Designer drugs, Diethylamino compounds, All stub articles, Cannabinoid stubs). ...
Heteromer
... cannabinoid CB1 / dopamine D2 heteromers, and even CB1/A2A/D2 heterotrimers where three different receptors have come together ... "Antagonistic cannabinoid CB1/dopamine D2 receptor interactions in striatal CB1/D2 heteromers. A combined neurochemical and ... A2A and cannabinoid CB1 receptors form functional heteromeric complexes that mediate the motor effects of cannabinoids". ... "Receptor-receptor interactions within receptor mosaics. Impact on neuropsychopharmacology". Brain Research Reviews. 58 (2): 415 ...
LBP-1 (drug)
It acts as a potent and selective cannabinoid receptor agonist, with high potency at both the CB1 and CB2 receptors, but low ... March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & ... April 2012). "Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain". Bioorganic & Medicinal ... heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate". Bioorganic & Medicinal Chemistry ...
2-Arachidonyl glyceryl ether
... and Raphael Mechoulam found the endogenous agonist of the cannabinoid receptor type 1 (CB1) in 2000. The discovery was 100 gram ... 3 μM at the Cannabinoid receptor type 1 and the peripheral cannabinoid receptors. The presence of 2-AGE in body tissue is ... 2-AGE binds with a Ki of 21 nM to the CB1 receptor and 480 nM to the CB2 receptor. It shows agonistic behaviour on both ... an endogenous agonist of the cannabinoid CB1 receptor". Proceedings of the National Academy of Sciences. 98 (7): 3662-3665. ...
PSNCBAM-1
Cannabinoids, CB1 receptor antagonists, Aminopyridines, All stub articles, Cannabinoid stubs). ... PSNCBAM-1 is a negative allosteric modulator of the cannabinoid CB1 receptor. GAT100 Org 27569 ZCZ-011 German N, Decker AM, ... a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats". British Journal of Pharmacology. ... "Diarylureas as Allosteric Modulators of the Cannabinoid CB1 Receptor: Structure-Activity Relationship Studies on 1-(4- ...
PTI-2
March 2011). "Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists". Bioorganic & ... heterocycle derivatives as agonists of the cannabinoid CB1 receptor.", issued 20 April 2010, assigned to Organon NV US 7763732 ... PTI-2 (SGT-49) is an indole-based synthetic cannabinoid. It is one of few synthetic cannabinoids containing a thiazole group ... Cannabinoids, Designer drugs, Isopropyl compounds, Ethers, All stub articles, Cannabinoid stubs). ...
Pregnenolone
Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... Cannabinoid receptor modulators. Receptor. .mw-parser-output .nobold{font-weight:normal}. (ligands). ... CB1 receptor antagonists. *Glycine receptor agonists. *Ketones. *Neurosteroids. *Pregnane X receptor agonists ... Nuclear receptor activity[edit]. Pregnenolone has been found to act as an agonist of the pregnane X receptor.[13] ...
Anandamid
Isolation and structure of a brain constituent that binds to the cannabinoid receptor". Science 258 (5090): 1946-9. DOI:10.1126 ... Otkriće anandamida potiče iz CB1 i CB2 istraživanja, kaja su delom bila zasnovana na stanovištu da mora da postoji prirodna ( ... Mechoulam R, Fride E (1995). „The unpaved road to the endogenous brain cannabinoid ligands, the anandamides". u: Pertwee RG. ... Ti distinktni efekti su posredovani prvenstveno CB1 kanabinoidnim receptorima u centralnom nervnom sistemu, i CB2 kanabinoidnim ...
Taranabant
... (codenamed MK-0364) is a cannabinoid receptor type 1 (CB1) inverse agonist that was investigated as a potential ... 2007). "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists". Bioorganic & Medicinal Chemistry ... Jun 2007). "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3- ... Others: 2-PG (directly potentiates activity of 2-AG at CB1 receptor) ...
Tetrahydrocannabiphorol
CB1 receptor agonists. *Phytocannabinoids. *Benzochromenes. *Cannabinoid stubs. Hidden categories: *Articles needing additional ... 8] JWH-091 has approximately double the binding affinity at the CB1 receptor (22nM ± 3.9nM) in comparison to Delta-9-THC (40.7 ... The Δ8 isomer is also known as a synthetic cannabinoid under the code name JWH-091,[6][7] It's unconfirmed whether or not Delta ... "THCp and CBDp, Newly Discovered, Extremely Potent Cannabinoids". 29 June 2020.. *^ Adams R, Loewe S, Jelinek C, Wolff H (July ...
Anandamide
... the complex is further directed to the cannabinoid receptor (CB1) and out.[36] ... These distinct effects are mediated primarily by CB1 cannabinoid receptors in the central nervous system, and CB2 cannabinoid ... it participates in the body's endocannabinoid system by binding to cannabinoid receptors, the same receptors that the ... Both the CB1 and CB2 receptors (the bonding site of anandamide) seem to play a role in the identification of positive and ...
Guineesine
In addition, the analgesic and catatonic effects were reversed by the cannabinoid receptor type 1 (CB1) inverse agonist ... "Small Molecules from Nature Targeting G-Protein Coupled Cannabinoid Receptors: Potential Leads for Drug Discovery and ... This causes an increase in the activity of the two neurotransmitters which are classified as endogenous cannabinoids. ...
N-Arachidonoyl dopamine
... (NADA) is an endocannabinoid that acts as an agonist of the CB1 receptor and the transient receptor ... cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo". The ... NADA was first described as a putative endocannabinoid (agonist for the CB1 receptor) in 2000 and was subsequently identified ... In mice, NADA was shown to induce the tetrad of physiological paradigms associated with cannabinoids: hypothermia, hypo- ...
JWH-424
JWH cannabinoids, Bromoarenes, Designer drugs, CB1 receptor agonists, All stub articles, Cannabinoid stubs). ... JWH-424 is a drug from the naphthoylindole family, which acts as a cannabinoid agonist at both the CB1 and CB2 receptors, but ... In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-424 are Schedule I Controlled ... However the 1-propyl homologues in this series showed much lower affinity at both receptors, reflecting a generally reduced ...
XLR-12
... with a Ki of 0.09 nM and 167x selectivity over the related CB1 receptor, however it still retains appreciable affinity for CB1 ... cannabinoid receptor activity". Journal of Medicinal Chemistry. 53 (1): 295-315. doi:10.1021/jm901214q. PMID 19921781. A ... "3-Cycloalkylcarbonyl indoles as cannabinoid receptor ligands", published 2006-06-29, assigned to Abbott Laboratories Frost JM, ... Cannabinoids, Designer drugs, Tetramethylcyclopropanoylindoles, All stub articles, Cannabinoid stubs). ...
GPR55
This profile as a distinct non-CB1/CB2 receptor which responds to a variety of both endogenous and exogenous cannabinoid ... "Entrez Gene: GPR55 G protein-coupled receptor 55". Brown AJ (Nov 2007). "Novel cannabinoid receptors". British Journal of ... "The orphan receptor GPR55 is a novel cannabinoid receptor". British Journal of Pharmacology. 152 (7): 1092-101. doi:10.1038/sj. ... Later it was identified by an in silico screen as a putative cannabinoid receptor because of a similar amino acid sequence in ...
JWH-015
JWH cannabinoids, Designer drugs, CB1 receptor agonists, CB2 receptor agonists). ... Its affinity for CB2 receptors is 13.8 nM, while its affinity for CB1 is 383 nM, meaning that it binds almost 28 times more ... In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-015 are Schedule I Controlled ... Ghosh S, Preet A, Groopman JE, Ganju RK (July 2006). "Cannabinoid receptor CB2 modulates the CXCL12/CXCR4-mediated chemotaxis ...
Cannabigerol
... has affinity and activity at CB1 and CB2 cannabinoid receptors in vitro. It appears to be unique among cannabinoid ... Alpha-2 adrenergic receptor agonists, Phytocannabinoids, CB1 receptor antagonists, Resorcinols, Terpeno-phenolic compounds). ... Couch DG, Maudslay H, Doleman B, Lund JN, O'Sullivan SE (March 2018). "The Use of Cannabinoids in Colitis: A Systematic Review ... Cascio MG, Gauson LA, Stevenson LA, Ross RA, Pertwee RG (January 2010). "Evidence that the plant cannabinoid cannabigerol is a ...
Parahexyl
... produces effects typical of other cannabinoid receptor agonists in animals. It has a somewhat higher oral ... Bow EW, Rimoldi JM (2016). "The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation". Perspectives ... the Δ8 and Δ9 isomers are both known to be cannabinoid receptor agonists, and Δ8-parahexyl has the code number JWH-124, while ... but as there has been no research published using parahexyl since the discovery of the CB1 receptor, this has not been ...
RCS-8
... all CB1 receptor agonists of the 3-phenylacetylindole class such as RCS-8 are Schedule I Controlled Substances. ... RCS-8 (also known as 1-(2-cyclohexylethyl)-3-(2-methoxyphenylacetyl)indole, SR-18, and BTM-8) is a synthetic cannabinoid that ...
CHM-081
CB1 receptor agonists, CB2 receptor agonists, Cyclohexyl compounds, Methoxy compounds, All stub articles, Nervous system drug ... CHM-081 (SGT-4) is a recreational designer drug which is classed as a synthetic cannabinoid. It is from the naphthoylindole ... AB-CHMINACA CHM-018 Org 28611 Edmunds R, Locos O, Brown D, Reynolds D (2013). "Identification of the synthetic cannabinoid (1-( ...
Raymond C. Stevens
2016: The marijuana receptor-human Cannabinoid receptor type 1 (CB1) and the human C-C chemokine receptor type 2 (CCR2) 2017: ... the human cannabinoid receptor CB2, the human neurokinin 1 receptor, and the melatonin receptors MT1 and MT2 2020:The human ... 2013: Serotonin receptors 5-HT1B and 5-HT2B, the second HIV co-receptor, C-C chemokine receptor type 5 (CCR5) and the first ... In 2010, the structures of the human chemokine CXCR4 receptor (HIV co-receptor), the human dopamine D3 receptor and the human ...
Cannabis use and trauma
Pertwee RG (January 2008). "The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9- ... "Distribution of CB1 cannabinoid receptors in the amygdala and their role in the control of GABAergic transmission". The Journal ... December 2019). "Cannabinoids for the treatment of mental disorders and symptoms of mental disorders: a systematic review and ... Braida D, Limonta V, Malabarba L, Zani A, Sala M (January 2007). "5-HT1A receptors are involved in the anxiolytic effect of ...
Methoxy arachidonyl fluorophosphonate
... evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptors". Br. J. Pharmacol. 140 (8): ... In addition, it binds to the CB1 receptor in rat brain membrane preparations (IC50 = 20 nM), but does not appear to agonize or ... Cannabinoid properties of methylfluorophosphonate analogs. J Pharmacol Exp Ther. 2000 Sep;294(3):1209-18. PMID 10945879 v t e v ... antagonize the receptor, though some related derivatives do show cannabinoid-like properties. DIFP - diisopropyl ...
JWH-176
... is an analgesic drug which acts as a cannabinoid receptor agonist. Its binding affinity at the CB1 receptor is 26.0 nM ... JWH cannabinoids, 1-Naphthyl compounds, Indenes, Polycyclic aromatic hydrocarbons, CB1 receptor agonists). ... In the United States, CB1 receptor agonists of the 1-(1-naphthylmethylene)indene class such as JWH-176 and JWH-171 are Schedule ... "Cannabinoids". Handbook of Experimental Pharmacology. Vol. 168. Springer. p. 269. ISBN 3-540-22565-X. Huffman JW, Padgett LW ( ...
AB-PICA
... is a potent agonist for the CB1 receptor (EC50 = 12 nM) and CB2 receptor (EC50 = 12 nM). 5F-AB-PINACA 5F-ADB 5F-AMB 5F- ... Cannabinoids, Designer drugs, Indolecarboxamides, All stub articles, Cannabinoid stubs). ... September 2015). "Pharmacology of Indole and Indazole Synthetic Cannabinoid Designer Drugs AB-FUBINACA, ADB-FUBINACA, AB-PINACA ...
JWH-133
... is a potent selective CB2 receptor agonist with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors. It was ... Additionally, cannabinoids at this receptor completely abolish neurotoxicity related to microglia activation in rat models.[ ... Bow EW, Rimoldi JM (28 June 2016). "The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation". ... binding 677nM at Cb1 and 3.4nM at CB2 while 3-(1',1'-Dimethylbutyl)-delta-8-THC itself binds 65nM at CB1. Structurally the only ...
O-823
It is described as a mixed agonist/antagonist at the cannabinoid receptor CB1, meaning that it acts as an antagonist when co- ... Griffin G, Wray EJ, Martin BR, Abood ME (October 1999). "Cannabinoid agonists and antagonists discriminated by receptor binding ... April 1999). "An investigation into the structural determinants of cannabinoid receptor ligand efficacy". British Journal of ... Cannabinoids, Benzochromenes, Phenols, Alkyne derivatives, Nitriles, All stub articles, Cannabinoid stubs). ...
Lipid signaling
The endogenous cannabinoids, or endocannabinoids, are endogenous lipids that activate cannabinoid receptors. The first such ... Anandamide activates both the CB1 receptor, found primarily in the central nervous system, and the CB2 receptor which is found ... the only identified receptors for S1P are the high-affinity G protein-coupled receptors (GPCRs), also known as S1P receptors ( ... 2-AG can also activate both cannabinoid receptors and is inactivated by monoacylglycerol lipase. It is present at approximately ...
5F-JWH-398
CB1 receptor agonists, CB2 receptor agonists, Chloroarenes, All stub articles, Nervous system drug stubs). ... is a recreational designer drug which is classed as a synthetic cannabinoid. It is from the naphthoylindole family, and ...
Apparent death
Griebel, G.; Stemmelin, J.; Scatton, B. (2005). "Effects of the cannabinoid CB1 receptor antagonist rimonabant in models of ... Donatti, A.F.; Leite-Panissi, C.R.A. (2011). "Activation of corticotropin-releasing factor receptors from the basolateral or ...
THJ-018
... acts as a full agonist with a binding affinity of 5.84 nM at CB1 and 4.57 nM at CB2 cannabinoid receptors. THJ-018 is ... Cannabinoids, Designer drugs, Naphthoylindazoles, All stub articles, Cannabinoid stubs). ... THJ-018 (SGT-17) is a synthetic cannabinoid that is the indazole analogue of JWH-018 and has been sold online as a designer ... Hess C, Schoeder CT, Pillaiyar T, Madea B, Müller CE (2016). "Pharmacological evaluation of synthetic cannabinoids identified ...
JWH-365
CB1 receptor agonists, CB2 receptor agonists, Designer drugs, Naphthoylpyrroles, All stub articles, Cannabinoid stubs). ... receptors, with a strong (~5x) selectivity for the CB2 receptor over the CB1 receptor. JWH-365 was first synthesized in 2006 by ... new high affinity ligands for the cannabinoid CB1 and CB2 receptors". Bioorganic & Medicinal Chemistry Letters. 16 (20): 5432-5 ... List of JWH cannabinoids Synthetic cannabinoid Huffman JW, Padgett LW, Isherwood ML, Wiley JL, Martin BR (October 2006). "1- ...
GW-842,166X
... is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, with a novel chemical structure ... but without cannabis-like behavioural effects due to its extremely low affinity for the CB1 receptor. GSK brought this compound ... Cannabinoids, Trifluoromethyl compounds, Aminopyrimidines, Chlorobenzenes, All stub articles, Cannabinoid stubs). ... a selective CB2 receptor agonist for the treatment of inflammatory pain". Journal of Medicinal Chemistry. 50 (11): 2597-600. ...
Exploring the Ligand Efficacy of Cannabinoid Receptor 1 (CB1) using Molecular Dynamics Simulations | Scientific Reports
Distinct efficacy profiles showed different therapeutic effects on CB1 dependent on three classes of ligands: agonists, ... method was applied to analyze the binding free energy decompositions of the CB1-ligand complexes. With these two methods, we ... simulations to identify the dynamic behaviors of inactive and active conformations of CB1 structures with the ligands. In ... CB1) is a promising therapeutic target for a variety of disorders. ...
Receptor, Cannabinoid, CB1 | Harvard Catalyst Profiles | Harvard Catalyst
Cannabinoid, CB1" by people in Harvard Catalyst Profiles by year, and whether "Receptor, Cannabinoid, CB1" was a major or minor ... "Receptor, Cannabinoid, CB1" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ... Below are the most recent publications written about "Receptor, Cannabinoid, CB1" by people in Profiles. ... Below are MeSH descriptors whose meaning is more general than "Receptor, Cannabinoid, CB1". ...
A Study of an Active-State CB1 Receptor Model and Synthetic Cannabinoid Interactions | American Academy of Forensic Sciences
Erowid.org: Erowid Reference 6199 : CB1 cannabinoid receptors and on-demand defense against excitotoxicity : Marsicano G,...
Lutz B CB1 cannabinoid receptors and on-demand defense against excitotoxicity Science 2003 302(5642):84-8 ... "CB1 cannabinoid receptors and on-demand defense against excitotoxicity" Science. 2003 Oct 3;302(5642):84-8. ... We generated conditional mutant mice that lack expression of the cannabinoid receptor type 1 in principal forebrain neurons but ... The endogenous cannabinoid system thus provides on-demand protection against acute excitotoxicity in central nervous system ...
Allosteric Interactions Between the Type 1 (CB1) and Type 2 (CB2) Cannabinoid Receptors Modify β-Arrestin2 Recruitment
Type 1 (CB1) and Type 2 (CB2) Cannabinoid receptors form heteromers with unique pharmacology compared to CB1 or CB2 alone. We ... Allosteric Interactions Between the Type 1 (CB1) and Type 2 (CB2) Cannabinoid Receptors Modify β-Arrestin2 Recruitment. ... Antagonism of CB1 or CB2 increased CP 55,940-induced β-arrestin2 recruitment to the heteromer partner. Thus, the CB1/CB2 ... CP 55,940 agonism in cells expressing CB1 and CB2 resulted in ~25% less β-arrestin2 recruitment to both CB1 and CB2, and these ...
SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition...
SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition ... SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition ... title = "SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social ... SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition ...
Plasma membrane and lysosomal localization of CB1 cannabinoid receptor are dependent on lipid rafts and regulated by anandamide...
... that the type-1 cannabinoid receptor (CB1R), which belongs to the family of G-protein-coupled receptors, is expressed on the ... also impairs DRM-association of the receptor suggesting that the membrane distribution of the receptor is dependent on rafts ... However, a substantial proportion of the receptor is present in lysosomes. We found that CB1R is associated with cholesterol- ... of sucrose density gradients suggesting that CB1 raft-association is cholesterol dependent. Interestingly binding of the ...
Cannabinoid CB1 receptor deficiency increases contextual fear memory under highly aversive conditions and long-term...
The cannabinoid receptor type 1 (CB1) is abundantly expressed in the central. nervous system where it negatively controls the ... Cannabinoid CB1 receptor deficiency increases contextual fear memory under highly. aversive conditions and long-term ... Cannabinoid CB1 receptor deficiency increases contextual fear memory under highly aversive conditions and long-term ... Cannabinoid CB1 receptor deficiency increases contextual fear memory under highly aversive conditions and long-term ...
Cannabinoid receptor CB1 mediates baseline and activity-induced survival of new neurons in adult hippocampal neurogenesis |...
In addition we used cannabinoid receptor 1 (CB1) deficient mice and treatment with CB1 antagonist AM251 in Nestin-GFP-reporter ... which could be related to CB1 receptor mediated signaling in Doublecortin (DCX)-expressing intermediate progenitor cells. CB1 ... We found the neurogenic effect of CBD to be dependent on the CB1 receptor, which is expressed over the whole dentate gyrus. ... We found that in the absence of CB1 receptors, cell proliferation was increased and neuronal differentiation reduced, ...
Efficacy and Safety of the CB1 Cannabinoid Receptor Blocker Rimonabant
One new agent in development is rimonabant, a selective cannabinoid type 1 (CB1) receptor blocker and the first member of a new ... Cite this: Efficacy and Safety of the CB1 Cannabinoid Receptor Blocker Rimonabant: Pooled Analysis of the RIO Program - ... Efficacy and Safety of the CB1 Cannabinoid Receptor Blocker Rimonabant: Pooled Analysis of the RIO Program ...
Differential expression of the neuronal CB1 cannabinoid receptor in the hippocampus of male Ts65Dn Down syndrome mouse model -...
CB1 & CB2 + GPR55? Another receptor for cannabinoids? | Marijuana Drug Facts
Is there a Third Cannabinoid Receptor?. We have long known about the two cannabinoid receptors: CB1 and CB2. Now there is ... The GPR55 receptor - the 55th in the series of G-protein-coupled receptors that also include CB1 and CB2 - is found in the ... GPR55 can explain some of the effects observed that are not mediated by the canonical cannabinoid receptors Cb1 and Cb2. To ... "orphan receptor" GPR55 - meaning its function had not yet been determined - as a "novel cannabinoid receptor." In the years ...
Minutes of the 159th Meeting of the NATIONAL ADVISORY COUNCIL ON ALCOHOL ABUSE AND ALCOHOLISM | National Institute on Alcohol...
THC produces effects via partial agonism of the cannabinoid type 1 (CB1) receptor. The CB1 receptor is activated by the ... The CB1 receptor blockade reduced the number of sleep spindles when CB1 inverse agonist AM281 was injected; the CB1 full ... There are very few CB1 receptors in the thalamus itself, but there are many in the reticular neurons. In the future, LIN plans ... There are a robust set of pharmacological tools to look at the CB1 receptor, including potent agonists and inverse agonists/ ...
Cannabinoid receptor 1 binding activity and quantitative analysis of Cannabis sativa L. smoke and vapor
Cannabis vapor and smoke was tested for cannabinoid receptor 1 (CB1) binding activity and compared to pure Delta(9)- ... Cannabinoid receptor 1 binding activity and quantitative analysis of Cannabis sativa L. smoke and vapor Chem Pharm Bull (Tokyo) ... Cannabinoids plus other components such as terpenoids and pyrolytic by-products were identified and quantified in all samples. ... There was no statistically significant difference between CB1 binding of pure Delta(9)-THC compared to cannabis smoke and vapor ...
A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models<...
A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models. ... Dive into the research topics of A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia ... A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models. / ... A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models. In ...
C&P#32: pain pain pain + where are your CB1 receptors? + your cannabinoids, your hormone cycle & you
For the orphaned GPR119 receptor (a receptor that might one day be officially designated as a cannabinoid receptor), it may be ... C&P#32: pain pain pain + where are your CB1 receptors? + your cannabinoids, your hormone cycle & you. MD & MO go legal + FDA ... Using computer modeling to analyze single-point mutations in a CB1 receptor. Evaluating Allosteric Perturbations in Cannabinoid ... CBG interacts with an adrenaline receptor (α-2 adrenoceptor) & a serotonin receptor (5-HT1A Receptor) as well as modulating the ...
Neurological Aspects of THC as a Treatment for Generalized Anxiety | Semantic Scholar
An Update on Non-CB1, Non-CB2 Cannabinoid Related G-Protein-Coupled Receptors. *P. Morales, P. Reggio ... Cannabinoid Receptors and the Endocannabinoid System: Signaling and Function in the Central Nervous System. *Shenglong Zou, U. ... Δ9-tetrahydrocannabinol is a full agonist at CB1 receptors on GABA neuron axon terminals in the hippocampus. *N. Laaris, C. ... Insight is provided into the non- CB1, non-CB2 cannabinoid-related GPCRs that have been reported thus far to consider the ...
The endocannabinoid system in migraine: from bench to pharma... : Current Opinion in Neurology
Allosteric modulators of the CB1 cannabinoid receptor: a structural update review. Cannabis Cannabinoid Res 2016; 1:22.. ... Cannabinoid (CB1) receptor activation inhibits trigeminovascular neurons. J Pharmacol Exp Ther 2007; 320:64-71.. * Cited Here ... CB1 and CB2 cannabinoid receptor agonists induce peripheral antinociception by activation of the endogenous noradrenergic ... Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor. Br J Pharmacol 2015; 172:4790-4805.. ...
Neuropathology of Drug Addictions and Substance Misuse Volume 1 - 1st Edition
Cannabis, Endocannabinoid CB1 Receptors, and the Neuropathology of Vision*Introduction. *Psychophysical Effects of Cannabinoids ... Role of Lipid Rafts and the Underlying Filamentous-Actin Cytoskeleton in Cannabinoid Receptor 1 Signaling*Cannabinoid Receptor ... Critical Role of Cannabinoid CB1 Receptors in Nicotine Reward and Addiction*Introduction ... Cannabis, Cannabinoid Receptors, and Stress-Induced Excitotoxicity*Introduction. *Endocannabinoid System and Stress: A ...
Does the cannabinoid dronabinol reduce central pain in multiple sclerosis? Randomised double blind placebo controlled crossover...
Cannabinoids reduce hyperalgesia and inflammation via interaction with peripheral CB1 receptors. Pain 1998;75: 111-9. ... Actions of cannabinoid receptor ligands on rat cultured sensory neurones: implications for antinociception. Neuropharmacology ... Analgesic effect of the cannabinoid analogue nabilone is not mediated by opioid receptors. Lancet 1999;353: 560. ... The role of central and peripheral cannabinoid1 receptors in the antihyperalgesic activity of cannabinoids in a model of ...
JCI -
Hepatic CB1 receptor is required for development of diet-induced steatosis, dyslipidemia, and insulin and leptin...
Increased mortality, hypoactivity, and hypoalgesia in cannabinoid CB1 receptor knockout mice. Proc. Natl. Acad. Sci. U. S. A. ... Effects of the cannabinoid CB1 receptor antagonist SR141716 on oxygen consumption and soleus muscle glucose uptake in Lep(ob)/ ... CB1 cannabinoid receptor knockout in mice leads to leanness, resistance to diet-induced obesity and enhanced leptin sensitivity ... The cannabinoid CB1 receptor antagonist SR141716A (Rimonabant) enhances the metabolic benefits of long-term treatment with ...
Research chemicals articles or hydrospace engineering
JWH-018 binds to both cannabinoid receptors the CB1. Posted on January 28, 2020. , By admin , No comments ... JWH-018 binds to both cannabinoid receptors the CB1. *Hexen is a psychoactive drug that was used previously for medicinal ... JWH-018 has effects like tetrahydrocannabinol (THC). Description JWH-018 binds to both cannabinoid receptors the […] ... Ethylphenidate is a synthetic cannabinoid of the class piperidine. *Cannabinoids for Chronic Pain - Igor Spigelman, PhD , UCLA ...
THC vs. CBD: What's the Difference?
THC binds with the cannabinoid 1 (CB1) receptors in the brain. It produces a high or a sense of euphoria. This high may be ... CBD binds very weakly, if at all, to CB1 receptors. CBD needs THC to bind to the CB1 receptor and, in turn, can help reduce ... This allows them to interact with your cannabinoid receptors.. The interaction affects the release of neurotransmitters in your ... Cannabis (marijuana) and cannabinoids: What you need to know. (2019). nccih.nih.gov/health/cannabis-marijuana-and-cannabinoids- ...
AM694 | C20H19FINO | ChemSpider
Models & Methods </span>
cannabis News Research Tags Articles - Page 2 of 16 - Neuroscience News
Researchers report amnesia caused by cannabinoids relies on the activation of the CB1 receptor in mitochondria in the ... People with the specific genotype of the Cannabinoid receptor 1 gene may be more prone to cannabis use disorder. Researchers ... Cannabinoid Medications Make Pain Feel Less Unpleasant and More Tolerable. A new study reveals cannabinoid medications may not ... Cannabinoids are Easier on the Brain Than Booze. A new study reveals long term alcohol use is much more damaging to the brain ...
Cannabidiol (CBD): MedlinePlus suplementos
The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: delta9-tetrahydrocannabinol, cannabidiol and delat9- ... Cannabidiol inhibitory effect on marble-burying behavior: involvement of CB1 receptors. Behav Pharmacol 2010;21:353-8. View ... Med Cannabis Cannabinoids. 2018 Jun;1:65-72. *Xu DH, Cullen BD, Tang M, Fang Y. The Effectiveness of Topical Cannabidiol Oil in ... Cannabis Cannabinoid Res 2021. View abstract.. *Kaufmann R, Aqua K, Lombardo J, Lee M. Observed Impact of Long-term Consumption ...
Endocannabinoids And Obese Diabetic Patients | 420 Magazine
... composed of G-protein-coupled cannabinoid receptors of type 1 and 2 (CB1 and CB2), of endogenous ligands for such receptors, ... 2-AG: 2-arachidonoylglycerol; AEA: anandamide; BMI: body mass index; CB1: cannabinoid receptor type 1; EC: endocannabinoid; ECS ... where they stimulate lipogenesis via cannabinoid CB1 receptors and are under the negative control of leptin and insulin. ... particularly as AEA is known to interact also with non-cannabinoid receptors, including transient receptor potential vanilloid ...
The potential benefit of the placebo effect in sham-controlled trials: implications for risk-benefit assessments and informed...
10 Best CBD Companies to Buy From in 2022: Honest Reviews & Guide | Observer
It stimulates the nervous systems CB2 receptors, which modulate inflammation. Unlike CB1 receptors, CB2 receptors do not cause ... CBD is just one of the 100+ cannabinoids found in hemp and marijuana. Other cannabinoids found in small amounts are ... It stimulates the nervous systems CB2 receptors, which modulate inflammation. Unlike CB1 receptors, CB2 receptors do not cause ... Instead, CBD acts as an inverse agonist at this receptor, making it harder for your CB1 receptors to bind with THC. As a result ...
EndocannabinoidsPsychoactiveLigandsCannabidiolAgonistBindsAntagonistsAnandamideNeuronsTherapeuticAntagonistNeuronalHuman endocannabinoid systemTetrahydrocannabinolModulateHippocampusDensity of cannabinoid receptorsDistribution of cannabinoid receptorsStimulateSynthetic cannabinoidExogenous cannabinoidsHempPotentInteractsCompoundsAnti-inflammatoryMetabolismTerpenesProteinsNeurotransmittersRimonabantSelectiveActivatesCB1RPharmacologyCannabis plantsStimulatesRegulatesTHCVBrainRegulateEndocannabinoid receptorAgonistsAbundantFoundEfficacyHigh cannabinoidRare cannabinoidMinor CannabinoidsVarious cannabinoidsDifferent cannabinoids2021ProducesCalled the endocannabinoidDronabinolGPCRsBindAnticancer drugsDopamineDelta-9-THCBody's endocannabinoidMarijuanaImmune systemEffectsDeficiencyStimulationAbstractMiceNeurotransmitter
Endocannabinoids14
- The endocannabinoid system (eCBs) encompasses the endocannabinoids, their synthetic and degradative enzymes, and cannabinoid (CB) receptors. (elsevier.com)
- Evidence is summarized that there are certain central and peripheral disorders in which increases take place in the release of endocannabinoids onto their receptors and/or in the density or coupling efficiency of these receptors and that this upregulation is protective in some disorders but can have undesirable consequences in others. (semanticscholar.org)
- The identification of its main active psychoactive ingredients led to the discovery of the cannabinoid receptors and their endogenous agonists, the endocannabinoids. (lww.com)
- The endocannabinoids, anandamide and 2-AG, are produced by adipocytes, where they stimulate lipogenesis via cannabinoid CB1 receptors and are under the negative control of leptin and insulin. (420magazine.com)
- The endocannabinoid system (ECS), composed of G-protein-coupled cannabinoid receptors of type 1 and 2 (CB1 and CB2), of endogenous ligands for such receptors, the endocannabinoids arachidonoylethanolamide (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), and of enzymes catalysing endocannabinoid biosynthesis and degradation, is a key player in the control of metabolism at both central and peripheral levels [1]. (420magazine.com)
- In the hypothalamus, endocannabinoids acting at CB1 receptors modulate the circuitries involved in food intake and are under the negative control of leptin [2]. (420magazine.com)
- Aims: Recently, the endocannabinoid system emerged as a pivotal regulator of food intake, ingestive behavior and energy metabolism, acting through CB1 and its endogenous ligands, the endocannabinoids. (endocrine-abstracts.org)
- There is a theory that cannabinoids from cannabis can fill the void left by a lack of endocannabinoids. (hightimes.com)
- Cannabinoids are typically divided into two categories: phytocannabinoids (those produced by plants) and endocannabinoids (those naturally occurring in humans). (herbaldispatch.com)
- It is composed of cannabinoid receptors and endocannabinoids, which interact with each other to regulate various physiological processes such as appetite, mood, and pain sensation. (herbaldispatch.com)
- The endocannabinoid system works through the synergistic actions of cannabinoid receptors, endocannabinoids made by the body, and enzymes. (camillacastro.us)
- Humans and animals alike naturally synthesize endocannabinoids, chemical compounds that activate the same receptors as delta-9-tetrahydrocannabinol (THC), the active component of marijuana ( Cannabis sativa ). (medscape.com)
- Once the receptors are activated, they end up being endocannabinoids and the plant cannabinoids in cannabis and hemp. (scotchcigars.com)
- In the event the outbound signs and symptoms remain, antipsychotic Your endocannabinoid routine, which commonly be inclined regarding epileptogenesis, has 2 G-proteins bundled receptors (cannabinoid model 1 CB1 not to mention cannabinoid variety 2 CB2) and a pair of endogenously synthesized, lipid-signaling endocannabinoids (anandamide N-arachidonyl ethanolamide and even 2-arachidonoyl glycerol 2-AG) that may content that will CB1 as well as CB2. (davidslandscapeconstruction.ca)
Psychoactive12
- CBD needs THC to bind to the CB1 receptor and, in turn, can help reduce some of the unwanted psychoactive effects of THC, such as euphoria or sedation. (healthline.com)
- Unlike THC, CBD and other cannabinoids do not have psychoactive properties. (laweekly.com)
- The psychoactive chemical, delta-9-tetrahydrocannabinol (THC) was isolated in the mid-1960s while other aspects of the endocannabinoid system [cannabinoid receptors (CB1 and CB2) and key endogenous cannabinoids (2-arachidonoyl glycerol and anandamide)] were identified over 20 years later. (frontiersin.org)
- Tetrahydrocannabinol (THC) is another well-known cannabinoid that produces the strong psychoactive effects of being "high. (medicalnewstoday.com)
- This may reduce the psychoactive effects of THC and may increase the number of circulating cannabinoids. (medicalnewstoday.com)
- The way the main psychoactive and non-psychoactive cannabinoids impact memory can be beneficial to PTSD patients. (hightimes.com)
- Of many classes of novel psychoactive substances, synthetic cannabinoids account for the enormous majority which are commonly encountered (Tracy et al. (springeropen.com)
- The jury's out on whether even large amounts of this cannabinoid can be considered psychoactive - but on its own, and in the low doses found in commercial cannabis products, CBN isn't likely to get you high. (wanawellness.com)
- Tetrahydrocannabivarin (THCV) is a cannabinoid that, if present in high enough doses, can interact with the body's endocannabinoid receptors to induce psychoactive effects. (sunnyskiescbd.com)
- However, when combined with four hydrogen atoms, CBD's affinity for CB1 is significantly increased, making the new cannabinoid (H4CBD) more psychoactive. (kannastar.com)
- THC is the most abundant cannabinoid found in cannabis, and it contains psychoactive properties that give users a "high. (cbdliving.com)
- When your community grounds a passing hypertensions, the first time to get the effects of same effects to the psychoactive effects is it edible is the most important thought of interacts with something like it, CBG, and CB1. (dropsmobile.com)
Ligands3
- Distinct efficacy profiles showed different therapeutic effects on CB1 dependent on three classes of ligands: agonists, antagonists, and inverse agonists. (nature.com)
- To discriminate the distinct efficacy profiles of the ligands, we carried out molecular dynamics (MD) simulations to identify the dynamic behaviors of inactive and active conformations of CB1 structures with the ligands. (nature.com)
- Our findings shed light on the understanding of different efficacy profiles of ligands by analyzing the structural behaviors of intact CB1 structures and the binding energies of ligands, thereby yielding insights that are useful for the design of new potent CB1 drugs. (nature.com)
Cannabidiol15
- Cannabidiol (CBD) is the main non-psychotropic compound of the plant cannabis sativa and belongs to the group of exogenous cannabinoids [ 15 ]. (biomedcentral.com)
- Tetrahydrocannabinol (THC) and cannabidiol (CBD) are two of the most recognized cannabinoids, but there are many others that are gaining attention for their potential therapeutic effects. (herbaldispatch.com)
- If you're reading this article, you've almost certainly heard of the cannabinoid known as CBD, or cannabidiol. (wanawellness.com)
- Cannabidiol (CBD) is a type of cannabinoid that occurs naturally in cannabis plants. (blosumcbd.com)
- Cannabidiol (CBD) - One of the four most well-known cannabinoids found in the cannabis plant. (cbdmaxonline.com)
- Based on a 2011 study titled "Safety and side effects of cannabidiol, a Cannabis sativa constituent" revealed that CBD has a better safety profile than THC and other cannabinoids. (scotchcigars.com)
- Cannabidiol and other non-habit forming cannabinoids could be used as novel therapeutic agents for the treatment of prostate cancer. (cbdepot.eu)
- Most non-THC plant cannabinoids e.g. cannabidiol and cannabigerol, seem to be devoid of psychotropic properties. (cbdepot.eu)
- Our overall findings support the concept that cannabidiol, which lacks psychotropic activity, may possess anti-inflammatory property and down regulates both cannabinoid receptors, PSA, VEGF, IL-6 and IL-8. (cbdepot.eu)
- Within this group, epilepsy is refractory in up to 40 % of patients, who have shown para el control de síntomas refractarios en a decrease in the frequency of seizures with the concomitant use of cannabidiol and conventional antiepileptics, with mild síndromes convulsivos side effects such as diarrhea and drowsiness. (bvsalud.org)
- Como parte de las terapias alternativas para el control de síntomas refractarios en enfermedades avanzadas destaca el uso de cannabidiol. (bvsalud.org)
- 40 % de los pacientes, quienes han demostrado disminución en la frecuencia de convulsiones con el uso concomitante de cannabidiol y antiepilépticos convencionales, con efectos secundarios leves, como diarrea y somnolencia. (bvsalud.org)
- de determinar el uso del cannabidiol para el control de síntomas neurológicos refractarios en pacientes con síndromes convulsivos y enfermedades neurodegenerativas, se realizó una búsqueda bibliográfica en Pubmed, Scopus y Embase. (bvsalud.org)
- Los efectos del cannabidiol lo convierten en una alternativa, of the title and research adicional a la terapéutica convencional, para el control de síntomas en trastornos neurológicos, disminuyendo de forma objectives, exhaustive sostenida el número total de episodios con un perfil de seguridad aceptable. (bvsalud.org)
- Existe limitada información respecto al uso de search of information in cannabidiol en enfermedades neurodegenerativas, por lo que no se ha evidenciado su efectividad. (bvsalud.org)
Agonist5
- Interestingly binding of the agonist, anandamide (AEA) also impairs DRM-association of the receptor suggesting that the membrane distribution of the receptor is dependent on rafts and is possibly regulated by the agonist binding. (archives-ouvertes.fr)
- When an agonist binds to CB1 a G protein is activated which, in turn, triggers a cellular response mediated by cAMP and a subsequent internalization mediated by ß-Arrestin. (innoprot.com)
- In this work, we investigated the effects of CB1 activation/blockade in mouse 3T3-L1 adypocite cells by using WIN55,212, a CB1/CB2 agonist and rimonabant, a specific CB1 antagonist, in different experimental settings such as acute treatment on pre-adipocytes and on mature adipocytes, and chronic treatment during di. (endocrine-abstracts.org)
- THCV, like Delta-9-THC, can act as an agonist of the body's CB1 endocannabinoid receptor, although the effects of THCV are much weaker than THC. (sunnyskiescbd.com)
- This chemical is a potent agonist of the CB1 receptor, but whether it is selective. (lds-chem.com)
Binds9
- THC binds with the cannabinoid 1 (CB1) receptors in the brain. (healthline.com)
- CBD binds very weakly, if at all, to CB1 receptors. (healthline.com)
- It also binds to cannabinoid 2 (CB2) receptors located in the brainstem and hippocampus, which has links to memory and emotions. (medicalnewstoday.com)
- When a ligand binds to the CB2 Receptor, it activates a G protein, which internalizes in big and high intensity vesicles. (innoprot.com)
- When a ligand binds to the CB1, it activates a G protein, which in turn, triggers a cellular response mediated by a second messenger. (innoprot.com)
- THCV binds with both CB1 and CB2 receptors, which allows it to provide a range of therapeutic benefits. (herbaldispatch.com)
- When CBD enters the body, it binds with cannabinoid receptors present in the endocannabinoid system (ECS) . (blosumcbd.com)
- Researchers found that CBD binds with CB1 receptors, 5-HT1A receptors plus other receptors in the brain that modulate anxiety. (blosumcbd.com)
- CBD works by interacting with the endocannabinoid system (ECS) in the human body in which it binds with CB2 receptors only - delivering the health benefits without any unwanted side effects. (naturecan.ie)
Antagonists4
- It was synthesized previously to develop a better understanding of the human endocannabinoid system and to determine cannabinoid receptor antagonists that would deficient the undesired powerful effects. (hs-eng.com)
- CB1 antagonists may reduce body weight and improve metabolic profiles in animals and humans by a double mechanism: at first, they target mesolimbic and hypothalamic nuclei and, thereafter, peripheral organs involved in energy storage and expenditure. (endocrine-abstracts.org)
- Cannabinoid antagonists may enhance the duration of the pattern of the scallop in mice. (dailysandiegonews.com)
- The failure of the metabotropic glutamate receptor 5 antagonists falls on the heels of the failure of Arbaclofen’s efficacy in children and adults with autism or FXS. (cdc.gov)
Anandamide4
- Plasma membrane and lysosomal localization of CB1 cannabinoid receptor are dependent on lipid rafts and regulated by anandamide in human breast cancer cells. (archives-ouvertes.fr)
- Because THC stimulates our brain's natural cannabinoid receptors (CB1) far more strongly and longer than the endogenous cannabinoid neurotransmitters anandamide and 2-AG, cannabis use throws brain chemistry out of balance temporarily, usually to people's enjoyment. (psychologytoday.com)
- The lower than normal number of available receptors left anandamide and 2-AG with fewer opportunities to have an impact. (psychologytoday.com)
- The background of depression is especially affected by the CB1 receptor and endocannabinoid anandamide (2,3). (hamppumaa.fi)
Neurons11
- A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release. (harvard.edu)
- Cannabinoid 1 receptor signaling on GABAergic neurons influences astrocytes in the ageing brain. (harvard.edu)
- We generated conditional mutant mice that lack expression of the cannabinoid receptor type 1 in principal forebrain neurons but not in adjacent inhibitory interneurons. (erowid.org)
- The endogenous cannabinoid system thus provides on-demand protection against acute excitotoxicity in central nervous system neurons. (erowid.org)
- CB1 affected the stages of adult neurogenesis that involve intermediate highly proliferative progenitor cells and the survival and maturation of new neurons. (biomedcentral.com)
- The receptor "receives the chemical and sends messages to cells such as neurons," according to Robert Sindelar, chief science officer and head of product development at BAS Research - a Berkeley, California-based licensed manufacturer of "white-label" cannabis products. (marijuanadrugfacts.com)
- Whenever neurons containing CB1 receptors are over-stimulated by THC's stronger and longer activation, a homeostatic response follows in an effort to rebalance the brain. (psychologytoday.com)
- As a result, neurons immediately react to THC's over-stimulation by reducing the number of CB1 receptors. (psychologytoday.com)
- By downregulating CB1 receptors, neurons partially regain some balance. (psychologytoday.com)
- Ethanol induces persistent potentiation of 5-HT receptor-stimulated GABA release at synapses on rat hippocampal CA1 neurons. (neurotree.org)
- Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
Therapeutic10
- Cannabinoid receptor 1 (CB1) is a promising therapeutic target for a variety of disorders. (nature.com)
- Thus, CB1 is a promising therapeutic target for a variety of disorders. (nature.com)
- This receptor, GPR55, may be key to understanding a wide spectrum of therapeutic applications for cannabinoids - and especially CBD. (marijuanadrugfacts.com)
- Most impressive was a 2015 overview published by Frontiers in Pharmacology, which found that two orphan receptors as well as the "deorphanized" GPR55 "may be promising therapeutic targets, with diverse physiological roles," ranging from gastrointestinal to bone disorders. (marijuanadrugfacts.com)
- It is believed that the therapeutic significance of cannabinoids is masked by the adverse effects and here alternative strategies are discussed to take therapeutic advantage of cannabinoids. (semanticscholar.org)
- The aim of the present study was to determine the cannabinoid chemotypes used for therapeutic purposes in Argentina and evaluate whether the cannabinoids present in home-made derivatives are comparable to those in commercially available products. (researchgate.net)
- Conclusions Our results indicate that despite their considerable variability, home-made preparations as a whole show cannabinoid levels and profiles equivalent to the commercially available products commonly used for medicinal, therapeutic and palliative purposes in Argentina. (researchgate.net)
- When we consume activated cannabinoids, we can experience the therapeutic benefits of the cannabis plant. (medicalmarijuana411.com)
- In this guide, we'll explore the different cannabinoids found in cannabis and discuss the potential therapeutic benefits that each one may offer. (herbaldispatch.com)
- Each cannabinoid has its own unique effects, and understanding how they interact with each other is key to utilizing cannabis for its therapeutic potential. (herbaldispatch.com)
Antagonist3
- The Δ 9 -tetrahydrocannabivarin (THCV) 21 is a CB1 antagonist that is structurally similar to THC. (nature.com)
- In addition we used cannabinoid receptor 1 (CB1) deficient mice and treatment with CB1 antagonist AM251 in Nestin-GFP-reporter mice to investigate the role of the CB1 receptor in adult neurogenesis in detail. (biomedcentral.com)
- It is well known that cannabinoid type 1 receptor (CB1) antagonist drugs may reduce body weight and improve metabolic profiles in obese animals and humans by a double mechanism: at first, targeting mesolimbic and hypothalamic nuclei and, thereafter, peripheral organs involved in energy storage and expenditure. (endocrine-abstracts.org)
Neuronal5
- Whereas the impact of synthetic cannabinoids on the neuronal progenitor cells has been described, there has been lack of information about the action of plant-derived extracts on neurogenesis. (biomedcentral.com)
- We found that in the absence of CB1 receptors, cell proliferation was increased and neuronal differentiation reduced, which could be related to CB1 receptor mediated signaling in Doublecortin (DCX)-expressing intermediate progenitor cells. (biomedcentral.com)
- 2010). Changes in tissue volume, morphology and composition have been reported in neuronal structures rich in cannabinoid receptors, most notably the hippocampus (Matochik et al . (medscape.com)
- Unlike neuronal tissue, fibre-enriched structures become depleted of cannabinoid (CB) receptors as the rat brain matures. (medscape.com)
- Local modulation by presynaptic receptors controls neuronal communication and behaviour. (neurotree.org)
Human endocannabinoid system2
- A scientific study published last year was the latest to focus the research community on the potential of the GPR55 receptor, which is now known to be the third identified receptor in the human endocannabinoid system. (marijuanadrugfacts.com)
- What CBG vs CBD debate, another noteworthy point is that just like CBD, CBG also attaches to the receptors in the human endocannabinoid system, however it does not have a preference when it comes to attaching to CB1 or CB2 receptors. (naturecan.ie)
Tetrahydrocannabinol5
- Cannabis vapor and smoke was tested for cannabinoid receptor 1 (CB1) binding activity and compared to pure Delta(9)-tetrahydrocannabinol (Delta(9)-THC). (nih.gov)
- 28 29 A large multicentre randomised placebo controlled study including 630 multiple sclerosis patients found an improvement in pain after 15 weeks of treatment with cannabinoids (oral δ-9-tetrahydrocannabinol or cannabis extract). (bmj.com)
- dimethylhexyl)-?8-tetrahydrocannabinol (10), exhibits 52-fold selectivity for this receptor with good (28 nM) affinity. (rti.org)
- De Giacomo V, Ruehle S, Lutz B, Häring M, Remmers F (2021) Differential glutamatergic and GABAergic contributions to the tetrad effects of Δ9-tetrahydrocannabinol revealed by cell-type-specific reconstitution of the CB1 receptor. (unimedizin-mainz.de)
- The most pharmacologically and toxicologically relevant as well as the most well-understood cannabinoid is tetrahydrocannabinol (THC), Dr. Boothe states. (wunderpetcbd.com)
Modulate3
- Cannabinoids modulate functions and activity of signaling pathways that have a key role in pain control. (lww.com)
- Innoprot Green Fluorescent CB2 Cannabinoid Receptor Cell Line allows to assay compounds, or analyze their capability to modulate CB2 activation and the following redistribution process inside the cells. (innoprot.com)
- Innoprot HiTSeeker CB1 Cell Line allows to assay compounds, or analyze their capability to modulate CB1. (innoprot.com)
Hippocampus3
- In the present study, the role of CB1 was investigated in three different hippocampus-dependent memory tasks and in in vivo hippocampal synaptic plasticity in knockout (CB1-ko) and wildtype mice. (bordeaux-neurocampus.fr)
- In conclusion, CB1 deficiency leads to enhanced contextual fear memory and altered synaptic plasticity in the hippocampus, supporting the key role of endocannabinoid signalling in learning and memory, in particular following highly aversive encounters. (bordeaux-neurocampus.fr)
- Researchers report amnesia caused by cannabinoids relies on the activation of the CB1 receptor in mitochondria in the hippocampus. (neurosciencenews.com)
Density of cannabinoid receptors2
- 1997). In adulthood, the density of cannabinoid receptors in these fibre-enriched structures has been found to diminish, eventually supplanted by the classical distribution of cannabinoid receptors (Romero et al . (medscape.com)
- However, the most important activities of the ECS may be in pain control and immunity function as evidenced by the higher density of cannabinoid receptors in those areas. (siciley.com)
Distribution of cannabinoid receptors1
- This widespread distribution of cannabinoid receptors is the reason why THC produces such powerful physical and psychological effects. (medicalnewstoday.com)
Stimulate4
- Gabet and Bab's team are building off of studies they have conducted in the past, where they discovered that the cannabinoid receptors within our bodies both stimulate bone formation and prevent bone loss. (medicaldaily.com)
- Cannabinoids like CBD, CBG, and CBN stimulate our CB1&CB2 receptors to help encourage homeostasis in our bodies In short. (pinterest.ph)
- Rather, THCV seems to stimulate your CB1 cannabinoid receptors in a way that naturally curbs cravings. (wanawellness.com)
- CBD does not stimulate the receptors, unlike THC that stimulates the CB1 and CB2 receptors. (scotchcigars.com)
Synthetic cannabinoid5
- Overview NM-2201 is an effective synthetic cannabinoid that is known as 1-pentyl-3-(1-naphthoyl) indole chemically. (hs-eng.com)
- Hexen, or Hexen (N-Ethylhexedrone), is a synthetic cannabinoid that is classified as an artificial cathinone. (hs-eng.com)
- Overview Ethylphenidate is a synthetic cannabinoid of the class piperidine and closely related to methylphenidate. (hs-eng.com)
- In 2014, the new synthetic cannabinoid, THJ-2201 [(1-(5-fluoropentyl)-1H-indazol-3-yl)(naphthalen-1-yl) methanone], had been found in the USA, Japan, and Russia. (springeropen.com)
- Indazole-based synthetic cannabinoid, 5-FADB , has been used in the manufacture of designer drugs and sold online as an active ingredient in synthetic cannabis products. (lds-chem.com)
Exogenous cannabinoids1
- Growing preclinical evidence and initial clinical findings suggest that modulation of the endocannabinoid system, via endogenous or exogenous cannabinoids may be relevant for migraine via multiple mechanisms. (lww.com)
Hemp12
- Pisupati and colleagues [4] analyzed the nuclear genomic diversity among cannabis varieties, including fiber hemp and seed oil hemp, high cannabinoid drug-types, and feral populations. (lww.com)
- They found the existence of at least three major groups of diversity with European hemp varieties, with genetic groups having different cannabinoid and terpenoid content. (lww.com)
- Contains CBD, THC (0.3% or less), other cannabinoids, natural terpenes (hemp plant compounds responsible for flavor and aroma as well as other wellness benefits), flavonoids (hemp plant compounds responsible for pigmentation). (holistapet.com)
- Cannabinoid, also known as Cannabis Oil or CBD, is a chemical compound which comes from marijuana or hemp. (cbdual.com)
- Every selection of the cannabis family members creates cannabinoids, consisting of hemp. (hempconspiracy.net)
- Are the cannabinoids derived from broad-spectrum hemp oil rather than isolate? (wanawellness.com)
- At the moment, hemp-derived CBD is still the only cannabinoid found in Wana Wellness products. (wanawellness.com)
- The flower parts of the hemp plant contain a wider variety and higher concentrations of cannabinoids and terpenes than the stalks and stems. (aarti-aunty.com)
- This broad spectrum CBD product utilizes the whole hemp plant, meaning our CBD vape pens are naturally rich in cannabinoids and, due to our unique blend, it's also rich in amino acids and fatty acids. (aarti-aunty.com)
- The marijuana, or hemp, plant contains over 450 unique chemicals, the most well-known of which are more than 70 cannabinoids. (wunderpetcbd.com)
- It is considered a major cannabinoid of hemp. (cbdliving.com)
- I have a few pounds of receptors to certainly work on our limited sources and Keoni it it reddit can't feel it it to be investigated by American-grown hemp seeds and tests. (dropsmobile.com)
Potent4
- Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists. (harvard.edu)
- While research surrounding THCV is still in its infancy, research has shown cannabinoids can have a potent effect on appetite. (sunnyskiescbd.com)
- THCV also has potent anti-inflammatory properties like many other cannabinoids, including CBD and CBG. (sunnyskiescbd.com)
- H4CBD is 100x more potent than CBD at your CB1 receptor and has greater anti-inflammatory properties than CBD. (kannastar.com)
Interacts9
- Because there is a growing body of evidence around the GPR55 receptor, including the 2017 study which discovered the GPR55 receptor's role in treating Dravet syndrome, Sindelar says there is more pressure on the academic community to continue researching the GPR55 receptor as a potential target for epilepsy treatment, especially in terms of how it interacts with CBD. (marijuanadrugfacts.com)
- The Endocannabinoid System (ECS) interacts with other non-cannabinoid systems, like the endorphin system, the immune system, and the vanilloid system responsible for changing pain from acute to chronic. (pinterest.ph)
- Learn more about your ECS, how it works inside the body, and how it interacts with cannabinoids like CBD and THC to help improve your overall health and wellbeing. (pinterest.ph)
- Serotonin interacts with 5-HT1A receptors, which play a significant role in anxiety disorders. (blosumcbd.com)
- Cannabinoid - Any chemical, natural or synthetic, that interacts with the endocannabinoid system. (cbdmaxonline.com)
- THC oil interacts with the serotonin receptors in the brain and maintains its balance. (articlesfit.com)
- CBG interacts directly with both of our CB1 and CB2 cannabinoid receptors within our brain for a more powerful effect on the endocannabinoid system vs CBD. (naturecan.ie)
- When it comes to CBD vs CBG, you will find that CBG interacts with these very same receptors, making it clear this relatively unknown cannabinoid has the potential to deliver positive impacts on the body in a similar way to CBD. (naturecan.ie)
- The intracellular (or cytoplasmic ) domain of the receptor interacts with the interior of the cell or organelle, relaying the signal. (ipfs.io)
Compounds9
- One new agent in development is rimonabant, a selective cannabinoid type 1 (CB1) receptor blocker and the first member of a new class of compounds targeting the endocannabinoid system, which has a key role in the regulation of energy balance and body composition. (medscape.com)
- All of these compounds showed selectivity for the CB2 receptor and one of them, 1-bromo-1-deoxy-3-(1? (rti.org)
- 16:46): Synthetic cannabinoids tend to be unsafe compounds that should be avoided. (bmtinfonet.org)
- Cannabinoids are a class of chemical compounds which act on the cannabinoid receptors in cells which repress neurotransmitter release in a person's brain. (cbdual.com)
- The stem contains very little THC but a high proportion of CBD and other nonpsychotropic cannabinoids as well as flavonoids, terpenoids and other potentially beneficial compounds, Dr. Boothe says. (wunderpetcbd.com)
- Cannabinoids are compounds that activate certain nerve receptors in the brain and body. (siciley.com)
- Additionally, some common edible and medicinal plants contain cannabinoids or cannabinoid-like compounds, which helps to explain their popular uses. (siciley.com)
- These chemical compounds are known as cannabinoids. (cbdliving.com)
- Cannabinoid compounds are smoked or vaporized by heating them at a temperature below the point at which combustion occurs, thereby releasing various cannabinoid vapors without burning any plant matter. (newstylereal.com)
Anti-inflammatory2
- One study in Frontiers in Pharmacology, suggested cannabinoids' anti-inflammatory effect may reduce inflammation too much. (aarti-aunty.com)
- Cannabinoids, the active components of Cannabis sativa Linnaeus , have received renewed interest in recent years due to their diverse pharmacologic activities such as cell growth inhibition, anti-inflammatory effects and tumor regression, but their use in chemotherapy is limited by their psychotropic activity. (cbdepot.eu)
Metabolism3
- In addition, CB1 receptors help regulate metabolism and appetite. (cbdmaxonline.com)
- Cannabinoids of medical significance appear to undergo first-pass metabolism and, as such, the risk of toxicity with inhalant products is much greater than with oral products, Dr. Boothe says. (wunderpetcbd.com)
- they react with the receptor to induce changes in the metabolism and activity of a cell. (ipfs.io)
Terpenes2
- Full-spectrum CBD products are as their name suggests: They contain all of the constituents of the plant, including terpenes, essential oils, flavonoids, and over 100 other cannabinoids, in addition to CBD. (peels.com)
- This is followed by what's called "winterization," which removes the other terpenes and cannabinoids from the plant. (peels.com)
Proteins3
- Guanine is associated with the G proteins because of how these receptors interact with cells. (marijuanadrugfacts.com)
- Their work focuses primarily on rhodopsin and the cannabinoid receptor CB1, studying how these proteins interact with their affiliate signaling partners (G-proteins, arrestins and kinases). (ohsu.edu)
- [2] [3] Many membrane receptors include transmembrane proteins . (ipfs.io)
Neurotransmitters2
- The cannabinoid receptor type 1 (CB1) is abundantly expressed in the central nervous system where it negatively controls the release of several neurotransmitters. (bordeaux-neurocampus.fr)
- The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES . (nih.gov)
Rimonabant1
- Cite this: Efficacy and Safety of the CB1 Cannabinoid Receptor Blocker Rimonabant: Pooled Analysis of the RIO Program - Medscape - Feb 02, 2008. (medscape.com)
Selective2
- We wanted to determine if the Tango β- arrestin2 luc reporter assay could measure heteromer-dependant allosteric modulation of β-arrestin2 recruitment to CB1 and CB2 following non-selective agonism with CP 55,940 and antagonism using AM251 or AM630. (dal.ca)
- Thus, the CB1/CB2 heteromer negatively modulates β-arrestin2 recruitment following non-selective agonism, and positively modulates β-arrestin2 recruitment following antagonism with AM251 or AM630. (dal.ca)
Activates4
- THC attaches itself to cannabin-oid receptors and activates them. (news-medical.net)
- CBD activates particular receptors like serotonin and adenosine. (scotchcigars.com)
- When CBD activates the adenosine receptors, it can help relieve anxiety since the adenosine receptors release dopamine. (scotchcigars.com)
- and kava - a calming medicinal herb with a cannabinoid-like compound that activates cannabinoid receptors in the brain[10]. (siciley.com)
CB1R2
- In this report we show, by confocal analysis of indirect immunofluorescence, that the type-1 cannabinoid receptor (CB1R), which belongs to the family of G-protein-coupled receptors, is expressed on the plasma membrane in human breast cancer MDA-MB-231 cells. (archives-ouvertes.fr)
- Here, we investigate the ability of a novel CB1 receptor (CB1R) allosteric modulator, ABM300, to ameliorate these dysregulated behaviors. (elsevier.com)
Pharmacology1
- Type 1 (CB1) and Type 2 (CB2) Cannabinoid receptors form heteromers with unique pharmacology compared to CB1 or CB2 alone. (dal.ca)
Cannabis plants5
- CBD is one of over one hundred cannabinoids that occur naturally in cannabis plants. (holistapet.com)
- Cannabinoids are produced in the flowers and leaves of cannabis plants, with each plant typically containing dozens of different cannabinoids. (herbaldispatch.com)
- Although there are more than 100 different cannabinoids found in cannabis plants, only a few have been studied in-depth. (herbaldispatch.com)
- A rare cannabinoid found in cannabis plants, THCV is a cousin of the well-known compound THC. (herbaldispatch.com)
- It's a cannabinoid, one of a family of molecules that are unique to cannabis plants. (healthmj.com)
Stimulates2
- When THC stimulates CB1 receptors in the amygdala, cannabinoid tone increases, lowering the bar for any stimulus being imbued with a sense of novelty. (psychologytoday.com)
- This receptor stimulates appetite, so blocking this can help reduce appetite and decrease hunger signals. (sunnyskiescbd.com)
Regulates1
- Treatment with Cannabis extract containing high CBD down regulates CB1, CB2, VEGF, PSA, pro-inflammatory cytokines/chemokine IL-6/IL-8. (cbdepot.eu)
THCV3
- Sometimes referred to as the "skinny cannabinoid," THCV may in fact aid with weight loss. (wanawellness.com)
- While most cannabinoids increase your appetite, recent studies have indicated that THCV could have the opposite effect. (sunnyskiescbd.com)
- While researchers are still not fully sure how this occurs, many believe THCV blocks the CB1 receptor. (sunnyskiescbd.com)
Brain22
- Bone Anabolic Response in the Calvaria Following Mild Traumatic Brain Injury is Mediated by the Cannabinoid-1 Receptor. (harvard.edu)
- The GPR55 receptor - the 55th in the series of G-protein-coupled receptors that also include CB1 and CB2 - is found in the brain and gastrointestinal tract. (marijuanadrugfacts.com)
- CBD targets the CB1 and CB2 receptors in the brain to alleviate different medical problems. (laweekly.com)
- A 2018 review in Surgical Neurology International indicates that CBD may reduce inflammation in the brain by indirectly interacting with CB2 receptors. (medicalnewstoday.com)
- Cannabis use typically begins during adolescence and early adulthood, a period when cannabinoid receptors are still abundant in white matter pathways across the brain. (medscape.com)
- In particular, cannabinoid receptors have been detected in white matter structures of the foetal and post-natal rat brain, including the corpus callosum, anterior commissure, fornix, stria terminalis and stria medullaris (Romero et al . (medscape.com)
- More generally, developing white matter may be at greater risk of damage due to its higher concentration of cannabinoid receptors relative to the mature brain, an important consideration given adolescence and young adulthood is the peak time of cannabis initiation. (medscape.com)
- Understanding THC's interaction with the brain's important natural cannabinoid chemistry and physiology will now make sense of the impact that overly frequent cannabis use has on the brain and mental functioning. (psychologytoday.com)
- CB1 receptors are found primarily in the brain, while CB2 receptors are found throughout the immune system and other bodily tissues. (herbaldispatch.com)
- The human brain has specific receptors for cannabinoids: CB1 and CB2. (healthmj.com)
- While the human brain is a complicated organ the scientific community has not fully mastered however, it has been proven to be in contact with cannabinoids. (dailysandiegonews.com)
- This is the first research to demonstrate that synthetic cannabinoids could interfere with brain dopamine release. (dailysandiegonews.com)
- Besides, the body naturally produces cannabinoids used in the brain and throughout the body. (blosumcbd.com)
- Cannabinoid 1 (CB1) Receptor - CB1 receptors are found primarily in the brain, central nervous system, lungs, liver, and kidneys, as well as on the skin. (cbdmaxonline.com)
- When CBD is used, it attaches itself to particular receptors in the brain. (scotchcigars.com)
- When someone takes CBD, it affects the endocannabinoid system composed of receptors found all over the body and brain. (scotchcigars.com)
- THC plays its role by binding with the CB1 and CB2 receptors in the brain. (articlesfit.com)
- THC is responsible for most of the psychotropic or behavioral effects of the Cannabis plant, and it acts by binding to the CB-1 receptor in the brain. (wunderpetcbd.com)
- CBD acts on your brain and body through a network of receptors called the endocannabinoid system (ECS). (siciley.com)
- Cannabinoids and their receptors throughout the brain and body form an interconnected network called the endocannabinoid system (ECS). (siciley.com)
- CB1 receptors, which are mostly concentrated in the central nervous system - your brain and spinal cord and mostly in areas of the central nervous system that have to do with processing pain messages from the body[12].CB2 receptors, which are more evenly distributed throughout the body and are especially prevalent in the immune system[12]. (siciley.com)
- When delta 9 THC is synthesized to create delta 10 THC, it affects how the delta 10 THC product reacts to the CB1 and CB2 receptors in your brain. (cbdliving.com)
Regulate4
- We'll also provide an overview of the endocannabinoid system, a network of receptors and enzymes that helps regulate many physiological processes in humans. (herbaldispatch.com)
- These cannabinoid receptors within the human body can help regulate various processes that we experience every day like mood, memory, pain sensation, and appetite. (scotchcigars.com)
- These receptors regulate important functions in the human body such as appetite, sleep and pain control, among others. (naturecan.ie)
- Rotation Model: Ligand binding to the extracellular part of the receptor induces the rotation of the receptor's transmembrane region inside the cell membrane, in doing so regulate it's activity inside the cell. (ipfs.io)
Endocannabinoid receptor1
- Endocannabinoid Receptor - These receptors reside on the surface of a variety of types of cells throughout the body, to trigger a physiological response. (cbdmaxonline.com)
Agonists2
- Antiemetic Effects of Cannabinoid Agonists in Nonhuman Primates. (harvard.edu)
- PPARγ agonists, such as the glitazones, used for the treatment of type 2 diabetes (T2D), reduce either adipocyte 2-AG concentrations or CB1 receptor expression levels, or both [3-5]. (420magazine.com)
Abundant1
- It is the most abundant cannabinoid in most cannabis strains. (herbaldispatch.com)
Found10
- We found the neurogenic effect of CBD to be dependent on the CB1 receptor, which is expressed over the whole dentate gyrus. (biomedcentral.com)
- A 2009 study published by PNAS found a role for the GPR55 receptor in regulating osteoclast function - that is to say, bone formation and healing . (marijuanadrugfacts.com)
- Results The results indicate that the medium-to-low cannabinoid concentration in a significant number of home-made oil samples is similar to that found in commercial products. (researchgate.net)
- Both CBD and THC cannabinoids, as well as the other cannabinoids found within cannabis, assist the body's Endocannabinoid System (ECS) and can contribute to greater health. (medicalmarijuana411.com)
- Scientists have found CB-1 receptors signal the deactivation of traumatic memories. (hightimes.com)
- In particular, the CB1 receptor has been found to play an important role as a mood regulator. (hamppumaa.fi)
- The body's natural system for taking in the cannabinoids found in cannabis, such as CBD or THC, is called the endocannabinoid system. (shopnaturallife.com)
- Cannabinoid 2 (CB2) Receptor - CB2 receptors are mainly found on immune cells but are also present in the central nervous system. (cbdmaxonline.com)
- Also, a 2015 study found that cannabinoids are powerful at bringing down pain levels related to cancer, neuropathy, and other intense and constant pain conditions. (compcaremd.com)
- The cannabinoids found in the plant vary with the part of the plant. (wunderpetcbd.com)
Efficacy4
- Cannabinoids have been proposed for the treatment of migraine but their efficacy and tolerability are controversial. (lww.com)
- In recent years the efficacy of cannabinoids in the treatment of multiple sclerosis symptoms, including pain and spasticity, has been discussed. (bmj.com)
- 24 - 27 Three randomised studies that evaluated the efficacy of cannabinoids on different neurogenic symptoms, including pain, have recently been published. (bmj.com)
- The other drug classes mentioned above have much more documented duration of action and efficacy without the systemic cannabinoid adverse effects. (medscape.com)
High cannabinoid1
- However, extractions from portions of the plant that do not contain high cannabinoid content often contain more than trace amounts of cannabinoids, rendering them subject to DEA regulation as a schedule 1 product. (wunderpetcbd.com)
Rare cannabinoid2
- So, if pain or stress are the main barriers between you and a good night's rest, CBN just might just be the rare cannabinoid you didn't know you needed! (wanawellness.com)
- But as the research advances, the potential for new, rare cannabinoid-infused formulations is certainly growing. (wanawellness.com)
Minor Cannabinoids2
- These letters refer to just a few of the 100+ "rare" or "minor" cannabinoids that occur within the cannabis plant. (wanawellness.com)
- Plenty is still unclear about the future of minor cannabinoids - including exactly how they should be regulated. (wanawellness.com)
Various cannabinoids2
- At the core of this research are the various cannabinoids, the active chemicals responsible for cannabis' effects. (herbaldispatch.com)
- And the best part with vaping is that you can use various cannabinoids and enhance efficiency. (articlesfit.com)
Different cannabinoids2
- There are over 100 different cannabinoids, each with its own unique effects and properties. (herbaldispatch.com)
- In simpler words, CBG does not cause a high or addiction, and difference between CBG and THC is that they are both different cannabinoids present in the weed plant. (naturecan.ie)
20211
- Kodirov SA, Bonni K, Wehrmeister M, Lutz B (2021) Depolarization-initiated endogenous cannabinoid release and underlying retrograde neurotransmission in interneurons of amygdala. (unimedizin-mainz.de)
Produces3
- Your body already has a cannabinoid system that uses the chemicals your body naturally produces. (laweekly.com)
- But why does the body have CB1 and CB2 anyway" For two decades it has been known that the human body also produces its own cannabinoids. (news-medical.net)
- The Cannabinoid Products Canada Farms it Canada try cbd gummies produces a clean, a clean mix of full-spectrum it. (canacoloscabos.com)
Called the endocannabinoid1
- After absorption into the physical body, CBD tinctures and oils connect to the endogenous cannabinoid program, called the endocannabinoid program also. (camillacastro.us)
Dronabinol1
- Does the cannabinoid dronabinol reduce central pain in multiple sclerosis? (bmj.com)
GPCRs3
- Insight is provided into the non- CB1, non-CB2 cannabinoid-related GPCRs that have been reported thus far to consider the physiological relevance of these molecular targets in modulating the ECS. (semanticscholar.org)
- HiTSeeker are cell lines stably expressing label-free GPCRs, also known as seven-(pass)-transmembrane domain receptors. (innoprot.com)
- In his laboratory at OHSU, Dr. Farrens (and colleagues) develop and use novel biochemical and physical methods to identify common structural mechanisms involved in the activation and attenuation of G-protein coupled receptors (GPCRs). (ohsu.edu)
Bind4
- CBD does not bind to either CB1 or CB2 receptors. (medicalnewstoday.com)
- According to a 2018 review article , CBD may reduce the ability of THC and other cannabinoids to bind to the CB1 receptor's. (medicalnewstoday.com)
- When contact occurs with a ligand, receptors bind together to form a dimer, a functional compound receptor composed of two structural similar monomers. (ipfs.io)
- For example, a neurotransmitter , hormone , or atomic ions may each bind to the extracellular domain as a ligand coupled to receptor. (ipfs.io)
Anticancer drugs1
- Research in animal models suggests the possible use of cannabinoids as anticancer drugs. (medscape.com)
Dopamine1
- Long-term alcohol consumption alters dorsal striatal dopamine release and regulation by D2 dopamine receptors in rhesus macaques. (neurotree.org)
Delta-9-THC1
- There was no statistically significant difference between CB1 binding of pure Delta(9)-THC compared to cannabis smoke and vapor at an equivalent concentration of Delta(9)-THC. (nih.gov)
Body's endocannabinoid1
- CBD may interact with the receptors in your body's endocannabinoid system (ECS), which helps harmonize the nervous system and create a state of homeostasis (or equilibrium) within the body. (peels.com)
Marijuana1
- The DEA has clarified its regulation of marijuana, noting the products derived from the parts of the plant that have only a trace of cannabinoids are not considered marijuana and thus are not subject to schedule 1 regulation. (wunderpetcbd.com)
Immune system1
- The ECS has two primary receptors: CB1 and CB2, located in the central nervous system and immune system respectively. (blosumcbd.com)
Effects12
- Because of the psychotropic effects of some cannabinoids, their clinical use is limited. (biomedcentral.com)
- ABM300 was characterized in vitro (receptor binding, β-arrestin2 recruitment, ERK1/2 phosphorylation, cAMP inhibition) and in vivo (anxiety-like behaviors, cannabimimetic effects, novel environment exploratory behavior, pre-pulse inhibition, conditioned avoidance response) to assess the effects of the compound in dysregulated behaviors within the transgenic models. (elsevier.com)
- There are a growing number of reports which correlate synthetic cannabinoids and acute behavioral and physiological effects including acute kidney injury, convulsions, and sudden death. (springeropen.com)
- Knowing how these cannabinoids interact with each other is key to understanding the effects of cannabis. (herbaldispatch.com)
- MDMA can block WIN's action by lowering the level of cannabinoid tone and, consequently, increasing the effects of MDMA that reward. (dailysandiegonews.com)
- CB1 receptors aren't involved in the photoresponse effects of WIN. (dailysandiegonews.com)
- CONCLUSIONS: These findings underscore the need to further evaluate use-motives as well as the interaction between dietary factors, cannabinoid pharmacokinetics, and subjective drug effects and the interactive effects of oral cannabis products and alcohol in a controlled laboratory setting. (bvsalud.org)
- To date, cannabinoids have been successfully used in the treatment of nausea and vomiting, two common side effects that accompany chemotherapy in cancer patients. (cbdepot.eu)
- This cannabinoid appears to retain many of the potentially therapeutically beneficial effects of THC but without the undesirable psychotropic effects. (wunderpetcbd.com)
- The most significant difference between the two cannabinoids is that THC has intoxicating effects while CBD is non-intoxicating. (siciley.com)
- Klotho is an enzyme which effects a receptor to recognize the ligand ( FGF23 ). (ipfs.io)
- In other receptors, the transmembrane domains undergo a conformational change upon binding, which effects intracellular conditions. (ipfs.io)
Deficiency1
- Cannabinoid CB1 receptor deficiency increases contextual fear memory under highly aversive conditions and long-term potentiation in vivo. (bordeaux-neurocampus.fr)
Stimulation2
- The phrase "over-stimulated" means only that THC's stimulation of CB1 receptors exceeds normal physiologic levels, leading to greater than normal negative feedback on the neuron 's release of transmitters with each firing. (psychologytoday.com)
- Fewer receptors reduce the amount of negative feedback produced by cannabinoid stimulation and a more physiologic balance is re-established. (psychologytoday.com)
Abstract1
- abstract = "Cannabinoid CB(1) receptor (CB(1)R) signaling has been suggested to play an important role in the regulation of memory and cognition. (maastrichtuniversity.nl)
Mice7
- There was no difference in short-term and long-term social and object recognition memory between CB1-ko and wildtype mice. (bordeaux-neurocampus.fr)
- In contrast, in background contextual fear conditioning CB1-ko mice showed enhanced freezing levels in the conditioning context and increased generalised contextual fear after a high-intensity conditioning foot shock of 1.5 mA, but not after 0.7 mA. (bordeaux-neurocampus.fr)
- In in vivo field potential recordings in the dentate gyrus, CB1-ko mice displayed a decreased paired-pulse facilitation of the populations spikes, suggesting an altered inhibitory synaptic drive onto hippocampal granule cells. (bordeaux-neurocampus.fr)
- This is the first study showing that the relative cannabinoid sensitivity of GABA and glutamate neurotransmission is species‐dependent, and it is hypothesized that WIN‐55,212 reduced anxiety in mice by affecting GABA neurotransmission whereas it increased anxiety in rats via glutamatergic mechanisms. (semanticscholar.org)
- Mice without CB1 receptors show psychological abnormalities," he explains. (news-medical.net)
- There are genetically modified strains of mice in which both cannabinoid receptors are dysfunctional. (news-medical.net)
- However, strains of mice in which the cannabinoid receptors are missing react much more intensely. (news-medical.net)
Neurotransmitter1
- When THC and CBD are ingested into the body, they activate your CB1 and CB2 receptors, which control the neurotransmitter and central nervous system, therefore regulating pain. (compcaremd.com)