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GPR18
''N''-Arachidonyl glycine receptor (NAGly receptor), also known as G protein-coupled receptor 18 (GPR18), is a protein that in humans is encoded by the ''GPR18'' gene. Along with the other previously "orphan" receptors GPR55 and GPR119, GPR18 has been found to be a receptor for endogenous lipid neurotransmitters, several of which also bind to cannabinoid receptors. It has been found to be involved in the regulation of intraocular pressure. Research supports the hypothesis that GPR18 is the abnormal cannabidiol receptor and N-arachidonoyl glycine, the endogenous lipid metabolite of anandamide, initiates directed microglial migration in the CNS through activation of GPR18, though recent evidence demonstrates that NAGly was not shown to be a GPR18 agonist in rat sympathetic neurons. Resolvin D2 (RvD2), a member of the specialized proresolving mediators (SPM) class of polyunsaturated fatty acid metabolites, is an activating ligand for GPR18; RvD2 and its activation of GPR18 cont ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-arachidonoyl Glycine
''N''-Arachidonylglycine (NAGly) is a carboxylic metabolite of the endocannabinoid anandamide (AEA). Since it was first synthesized in 1996, NAGly has been a primary focus of the relatively contemporary field of lipidomics due to its wide range of signaling targets in the brain, the immune system and throughout various other bodily systems. In combination with 2‐arachidonoyl glycerol (2‐AG), NAGly has enabled the identification of a family of lipids often referred to as endocannabinoids. Recently, NAGly has been found to bind to G-protein coupled receptor 18 (GPR18), the putative abnormal cannabidiol receptor. NaGly is an endogenous inhibitor of fatty acid amide hydrolase (FAAH) and thereby increases the ethanolamide endocannabinoids AEA, oleoylethanolamide (OEA) and palmitoylethanolamide (PEA) levels. NaGly is found throughout the body and research on its explicit functions is ongoing. Biosynthesis and degradation The biosynthesis and degradation of NaGly is not complet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-Arachidonylglycine
''N''-Arachidonylglycine (NAGly) is a carboxylic metabolite of the endocannabinoid anandamide (AEA). Since it was first synthesized in 1996, NAGly has been a primary focus of the relatively contemporary field of lipidomics due to its wide range of signaling targets in the brain, the immune system and throughout various other bodily systems. In combination with 2‐arachidonoyl glycerol (2‐AG), NAGly has enabled the identification of a family of lipids often referred to as endocannabinoids. Recently, NAGly has been found to bind to G-protein coupled receptor 18 (GPR18), the putative abnormal cannabidiol receptor. NaGly is an endogenous inhibitor of fatty acid amide hydrolase (FAAH) and thereby increases the ethanolamide endocannabinoids AEA, oleoylethanolamide (OEA) and palmitoylethanolamide (PEA) levels. NaGly is found throughout the body and research on its explicit functions is ongoing. Biosynthesis and degradation The biosynthesis and degradation of NaGly is not com ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CID-85469571
PSB-CB5 (CID-85469571) is a compound which acts as an antagonist at the former orphan receptor GPR18, and is the first selective antagonist characterised for this receptor, with an IC50 of 279nM, and good selectivity over related receptors (over 36x selectivity vs CB1 and GPR55, and 14x vs CB2.) As all previously known antagonists for GPR18 also antagonise GPR55, it has been difficult to separate the effects of these two receptor targets, so the discovery of a selective GPR18 antagonist is expected to be useful in research into the actions of this receptor. See also * CID-16020046 * O-1918 O-1918 is a synthetic compound related to cannabidiol, which is an antagonist at two former orphan receptors GPR18 and GPR55, that appear to be related to the cannabinoid receptors. O-1918 is used in the study of these receptors, which have been ... References {{Cannabinoidergics Cannabinoids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor
Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids; plant cannabinoids (such as Tetrahydrocannabinol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic. There are two known subtypes of cannabinoid receptors, termed CB1 and CB2. The CB1 receptor is expressed mainly in the brain (central nervous system or "CNS"), but also in the lungs, liver and kidneys. The CB2 receptor is expressed mainly in the immune system, in hematopoietic cells, and in parts of the brain. The protein sequences of CB1 and CB2 receptors are about 44% simi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O-1602
O-1602 is a synthetic compound most closely related to abnormal cannabidiol, and more distantly related in structure to cannabinoid drugs such as THC. O-1602 does not bind to the classical cannabinoid receptors CB1 or CB2 with any significant affinity, but instead is an agonist at several other receptors which appear to be related to the cannabinoid receptors, particularly GPR18 and GPR55. These previously orphan receptors have been found to be targets for a number of endogenous and synthetic cannabinoid compounds, and are thought to be responsible for most of the non-CB1, non-CB2 mediated effects that have become evident in the course of cannabinoid research. O-1602 produces some effects shared with classical cannabinoid compounds such as analgesic and antiinflammatory effects and appetite stimulation, but it does not produce sedation or psychoactive effects, and has several actions in the gut and brain that are not shared with typical cannabinoid agonists. See also * Cannabidi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abnormal Cannabidiol
Abnormal cannabidiol (Abn-CBD) is a synthetic regioisomer of cannabidiol, which unlike most other cannabinoids produces vasodilator effects, lowers blood pressure, and induces cell migration, cell proliferation and mitogen-activated protein kinase activation in microglia, but without producing any psychoactive effects. Receptor activity It has been shown that the actions of abnormal cannabidiol are mediated through a site separate from the CB1 and CB2 receptors, which responds to abnormal cannabidiol, O-1602, and the endogenous ligands: anandamide (AEA), N-arachidonoyl glycine (NAGly) and N-arachidonoyl L-serine. Multiple lines of evidence support the proposed identification of this novel target in microglia as the previously "orphan" receptor GPR18. Another possible target of abnormal cannabidiol is GPR55, which has also received much attention as a putative cannabinoid receptor, although a growing body of evidence points to lysophosphatidylinositol (LPI) as the endogenous ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GPR55
G protein-coupled receptor 55 also known as GPR55 is a G protein-coupled receptor that in humans is encoded by the ''GPR55'' gene. GPR55, along with GPR119 and GPR18, have been implicated as novel cannabinoid receptors. History GPR55 was identified and cloned for the first time in 1999. Later it was identified by an in silico screen as a putative cannabinoid receptor because of a similar amino acid sequence in the binding region. Research groups from Glaxo Smith Kline and Astra Zeneca characterized the receptor extensively because it was hoped to be responsible for the blood pressure lowering properties of cannabinoids. GPR55 is indeed activated by endogenous and exogenous cannabinoids such as plant and synthetic cannabinoids but GPR-55 knockout mice generated by a research group from Glaxo Smith Kline showed no altered blood pressure regulation after administration of the cannabidiol-derivative abnormal cannabidiol. Signal cascade GPR55 is coupled to the G-protein G1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GPR119
G protein-coupled receptor 119 also known as GPR119 is a G protein-coupled receptor that in humans is encoded by the ''GPR119'' gene. GPR119, along with GPR55 and GPR18, have been implicated as novel cannabinoid receptors. Pharmacology GPR119 is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents. Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. GPR119 has also been shown to regulate incretin and insulin hormone secretion. As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity and diabetes. Ligands A number of endogenous and synthetic ligands for this receptor have been identified: * 2-Oleoylglycerol * Anandamide * AR-231,453 * MBX-2982 * Oleoylethanolamide Oleoylethanolamide (OEA) is an endogenous peroxisome proliferator-activated receptor alpha ( PPAR-α) agonist. It is a naturally occurring ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abnormal Cannabidiol
Abnormal cannabidiol (Abn-CBD) is a synthetic regioisomer of cannabidiol, which unlike most other cannabinoids produces vasodilator effects, lowers blood pressure, and induces cell migration, cell proliferation and mitogen-activated protein kinase activation in microglia, but without producing any psychoactive effects. Receptor activity It has been shown that the actions of abnormal cannabidiol are mediated through a site separate from the CB1 and CB2 receptors, which responds to abnormal cannabidiol, O-1602, and the endogenous ligands: anandamide (AEA), N-arachidonoyl glycine (NAGly) and N-arachidonoyl L-serine. Multiple lines of evidence support the proposed identification of this novel target in microglia as the previously "orphan" receptor GPR18. Another possible target of abnormal cannabidiol is GPR55, which has also received much attention as a putative cannabinoid receptor, although a growing body of evidence points to lysophosphatidylinositol (LPI) as the endogenous ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
O-1918
O-1918 is a synthetic compound related to cannabidiol, which is an antagonist at two former orphan receptors GPR18 and GPR55, that appear to be related to the cannabinoid receptors. O-1918 is used in the study of these receptors, which have been found to be targets for a number of endogenous and synthetic cannabinoid compounds, and are thought to be responsible for most of the non-CB1, non-CB2 mediated effects that have become evident in the course of cannabinoid research. See also * Abnormal cannabidiol * Cannabidiol dimethyl ether * CID-16020046 CID16020046 is a compound which acts as an inverse agonist at the former orphan receptor GPR55, and may be the first selective inverse agonist characterised for this receptor. It was found to block a number of GPR55 mediated responses such as wou ... * CID-85469571 * O-1602 * Tetrahydrocannabiorcol References {{Cannabinoidergics Cannabinoids Cyclohexenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Resolvin D2
Resolvins are specialized pro-resolving mediators (SPMs) derived from omega-3 fatty acids, primarily eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), as well as docosapentaenoic acid (DPA) and clupanodonic acid. As autacoids similar to hormones acting on local tissues, resolvins are under preliminary research for their involvement in promoting restoration of normal cellular function following the inflammation that occurs after tissue injury. Resolvins belong to a class of polyunsaturated fatty acid (PUFA) metabolites termed specialized proresolving mediators (SPMs). Biochemistry and production Resolvins (Rvs) fall into several sub-classes based on the straight chain PUFA from which they are formed and/or a unique aspect of their structure. The Resolvin Ds (RvDs) are metabolites of the 22-carbon PUFA, DHA (i.e. 4''Z'',7''Z'',10''Z'',13''Z'',16''Z'',19''Z'')-docosahexaenoic acid); the resolvin Es (RvEs) are metabolites of the 20-carbon PUFA, EPA (i.e. 5''Z'',8''Z'',11' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Specialized Proresolving Mediators
Specialized pro-resolving mediators (SPM, also termed specialized proresolving mediators) are a large and growing class of cell signaling molecules formed in cells by the metabolism of polyunsaturated fatty acids (PUFA) by one or a combination of lipoxygenase, cyclooxygenase, and cytochrome P450 monooxygenase enzymes. Pre-clinical studies, primarily in animal models and human tissues, implicate SPM in orchestrating the resolution of inflammation. Prominent members include the resolvins and protectins. SPM join the long list of other physiological agents which tend to limit inflammation (see ) including glucocorticoids, interleukin 10 (an anti-inflammatory cytokine), interleukin 1 receptor antagonist (an inhibitor of the action of pro-inflammatory cytokine, interleukin 1), annexin A1 (an inhibitor of formation of pro-inflammatory metabolites of polyunsaturated fatty acids), and the gaseous resolvins, carbon monoxide (see ), nitric oxide (see ), and hydrogen sulfide (see and ). ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
