Type |
Details |
Score |
Genotype |
Symbol: |
Gpr55/Gpr55 |
Background: |
involves: 129S5/SvEvBrd * C57BL/6 |
Zygosity: |
hm |
Has Mutant Allele: |
true |
|
•
•
•
•
•
|
Genotype |
Symbol: |
Gpr55/Gpr55 |
Background: |
involves: 129S5/SvEvBrd |
Zygosity: |
hm |
Has Mutant Allele: |
true |
|
•
•
•
•
•
|
Publication |
First Author: |
Kohno M |
Year: |
2006 |
Journal: |
Biochem Biophys Res Commun |
Title: |
Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18. |
Volume: |
347 |
Issue: |
3 |
Pages: |
827-32 |
|
•
•
•
•
•
|
Publication |
First Author: |
Burstein S |
Year: |
2008 |
Journal: |
Neuropharmacology |
Title: |
The elmiric acids: biologically active anandamide analogs. |
Volume: |
55 |
Issue: |
8 |
Pages: |
1259-64 |
|
•
•
•
•
•
|
Publication |
First Author: |
Bradshaw HB |
Year: |
2009 |
Journal: |
Prostaglandins Other Lipid Mediat |
Title: |
Orphan endogenous lipids and orphan GPCRs: a good match. |
Volume: |
89 |
Issue: |
3-4 |
Pages: |
131-4 |
|
•
•
•
•
•
|
Publication |
First Author: |
Southern C |
Year: |
2013 |
Journal: |
J Biomol Screen |
Title: |
Screening β-arrestin recruitment for the identification of natural ligands for orphan G-protein-coupled receptors. |
Volume: |
18 |
Issue: |
5 |
Pages: |
599-609 |
|
•
•
•
•
•
|
Publication |
First Author: |
Yin H |
Year: |
2009 |
Journal: |
J Biol Chem |
Title: |
Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. |
Volume: |
284 |
Issue: |
18 |
Pages: |
12328-38 |
|
•
•
•
•
•
|
Publication |
First Author: |
Alexander SP |
Year: |
2012 |
Journal: |
Br J Pharmacol |
Title: |
So what do we call GPR18 now? |
Volume: |
165 |
Issue: |
8 |
Pages: |
2411-3 |
|
•
•
•
•
•
|
Publication |
First Author: |
Davenport AP |
Year: |
2013 |
Journal: |
Pharmacol Rev |
Title: |
International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. |
Volume: |
65 |
Issue: |
3 |
Pages: |
967-86 |
|
•
•
•
•
•
|
Protein Domain |
Type: |
Family |
Description: |
Several 7TM receptors have been cloned but their endogenous ligands are unknown; these have been termed orphan receptors. However, recent research has identified certain pharmacological targets that could be investigated to find, for example, new potential cannabinoid receptors or channels [, , ]. GPR18 [, ], GPR55 [, ], GPR119 []show little structural similarity to CB1 and CB2 receptors, but they respond to endogenous agents analogous to the endogenous cannabinoid ligands, as well as some natural/synthetic cannabinoid receptor ligands []. However, because they do not fulfill all of the cannabinoid receptor criteria defined by IUPHAR, the classification of these proteins remains a contentious issue due to conflicting pharmacological results. As a result, they remain classified as putative endogenous agonists by IUPHAR [].This entry represents G protein-coupled receptor 18, also known as N-arachidonyl glycine receptor. It has been found to be a receptor for endogenous lipid neurotransmitters, several of which also bind to cannabinoid receptors [, , , ]. Recent research also 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 []. However, the pairing of GPR18 with N-arachidonoylglycine (NAGly) and tetrahydrocannabinol (THC) was not reproduced in two studies based on beta-arrestin assays [, ]. So, until further research allows a more definitive decision the function and nomenclature GPR18 is still being debated [, ]. |
|
•
•
•
•
•
|
Publication |
First Author: |
Briand-Mésange F |
Year: |
2020 |
Journal: |
J Biol Chem |
Title: |
Glycerophosphodiesterase 3 (GDE3) is a lysophosphatidylinositol-specific ectophospholipase C acting as an endocannabinoid signaling switch. |
Volume: |
295 |
Issue: |
46 |
Pages: |
15767-15781 |
|
•
•
•
•
•
|
Publication |
First Author: |
Kaplan JS |
Year: |
2017 |
Journal: |
Proc Natl Acad Sci U S A |
Title: |
Cannabidiol attenuates seizures and social deficits in a mouse model of Dravet syndrome. |
Volume: |
114 |
Issue: |
42 |
Pages: |
11229-11234 |
|
•
•
•
•
•
|
Publication |
First Author: |
Taylor L |
Year: |
2015 |
Journal: |
Sci Rep |
Title: |
Primary Macrophage Chemotaxis Induced by Cannabinoid Receptor 2 Agonists Occurs Independently of the CB2 Receptor. |
Volume: |
5 |
|
Pages: |
10682 |
|
•
•
•
•
•
|
Publication |
First Author: |
Arifin SA |
Year: |
2018 |
Journal: |
Biochim Biophys Acta Mol Cell Biol Lipids |
Title: |
Oleoyl-lysophosphatidylinositol enhances glucagon-like peptide-1 secretion from enteroendocrine L-cells through GPR119. |
Volume: |
1863 |
Issue: |
9 |
Pages: |
1132-1141 |
|
•
•
•
•
•
|
Publication |
First Author: |
Soga T |
Year: |
2005 |
Journal: |
Biochem Biophys Res Commun |
Title: |
Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. |
Volume: |
326 |
Issue: |
4 |
Pages: |
744-51 |
|
•
•
•
•
•
|
Publication |
First Author: |
Chu ZL |
Year: |
2007 |
Journal: |
Endocrinology |
Title: |
A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. |
Volume: |
148 |
Issue: |
6 |
Pages: |
2601-9 |
|
•
•
•
•
•
|
Publication |
First Author: |
Overton HA |
Year: |
2006 |
Journal: |
Cell Metab |
Title: |
Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. |
Volume: |
3 |
Issue: |
3 |
Pages: |
167-75 |
|
•
•
•
•
•
|
Publication |
First Author: |
Ning Y |
Year: |
2008 |
Journal: |
Br J Pharmacol |
Title: |
Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells. |
Volume: |
155 |
Issue: |
7 |
Pages: |
1056-65 |
|
•
•
•
•
•
|
Publication |
First Author: |
Swaminath G |
Year: |
2008 |
Journal: |
Arch Pharm (Weinheim) |
Title: |
Fatty acid binding receptors and their physiological role in type 2 diabetes. |
Volume: |
341 |
Issue: |
12 |
Pages: |
753-61 |
|
•
•
•
•
•
|
Publication |
First Author: |
Lan H |
Year: |
2009 |
Journal: |
J Endocrinol |
Title: |
GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis. |
Volume: |
201 |
Issue: |
2 |
Pages: |
219-30 |
|
•
•
•
•
•
|
Publication |
First Author: |
Overton HA |
Year: |
2008 |
Journal: |
Br J Pharmacol |
Title: |
GPR119, a novel G protein-coupled receptor target for the treatment of type 2 diabetes and obesity. |
Volume: |
153 Suppl 1 |
|
Pages: |
S76-81 |
|
•
•
•
•
•
|
Publication |
First Author: |
Chu ZL |
Year: |
2010 |
Journal: |
Mol Endocrinol |
Title: |
N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119. |
Volume: |
24 |
Issue: |
1 |
Pages: |
161-70 |
|
•
•
•
•
•
|
Protein Domain |
Type: |
Family |
Description: |
Several 7TM receptors have been cloned but their endogenous ligands are unknown; these have been termed orphan receptors. However, recent research has identified certain pharmacological targets that could be investigated to find, for example, new potential cannabinoid receptors or channels [, , ]. GPR18 [, ], GPR55 [, ], GPR119 []show little structural similarity to CB1 and CB2 receptors, but they respond to endogenous agents analogous to the endogenous cannabinoid ligands, as well as some natural/synthetic cannabinoid receptor ligands []. However, because they do not fulfill all of the cannabinoid receptor criteria defined by IUPHAR, the classification of these proteins remains a contentious issue due to conflicting pharmacological results. As a result, they remain classified as putative endogenous agonists by IUPHAR [].This entry represents glucose-dependent insulinotropic receptor, also known as G protein-coupled receptor 119. It is expressed predominantly in the pancreas and gastrointestinal tract in rodents and humans, as well as in the brain in rodents []. It has been shown to be involved in the control of glucose-dependent insulin release and glucagon-like peptide 1 release, respectively [, ], which caused a reduction in food intake and body weight gain in rats []. GPR119 has also been shown to regulate incretin and insulin hormone secretion [, , ], behaving as a glucose-dependent insulinotropic receptor. As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity and diabetes [, , ]. Although GPR119 is phylogenetically related to cannabinoid receptors, only fatty acid amides interact with GPR119 [, , , ]. The potency order is N-oleoyl dopamine >oleoyl ethanolamide >palmitoyl ethanolamide >anandamide [, ]. However, because only N-oleoyl dopamine and oleoyl ethanolamide have reasonably high (low micromolar) affinity for GPR119, and because neither of these lipids interacts with CB1 or CB2 receptors, GPR119 cannot currently be viewed as a cannabinoid receptor []. |
|
•
•
•
•
•
|
Publication |
First Author: |
Harada K |
Year: |
2017 |
Journal: |
J Biol Chem |
Title: |
Lysophosphatidylinositol-induced activation of the cation channel TRPV2 triggers glucagon-like peptide-1 secretion in enteroendocrine L cells. |
Volume: |
292 |
Issue: |
26 |
Pages: |
10855-10864 |
|
•
•
•
•
•
|
Protein |
Organism: |
Mus musculus/domesticus |
Length: |
331
 |
Fragment?: |
false |
|
•
•
•
•
•
|
Protein |
Organism: |
Mus musculus/domesticus |
Length: |
335
 |
Fragment?: |
false |
|
•
•
•
•
•
|