Chemistry:CID16020046
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| Formula | C25H19N3O4 |
| Molar mass | 425.435 g·mol−1 |
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CID16020046 is a compound which acts as an inverse agonist at the former orphan receptor GPR55,[1] 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 wound healing and activation of immune system T-cells and B-cells, as well as showing inverse agonist activity in the absence of GPR55 agonist stimulation. However while it was found to have good selectivity over the related CB1 and CB2 cannabinoid receptors as well as a number of other targets, CID16020046 has not yet been tested against another related receptor GPR18, so its selectivity for GPR55 over this target has not been established.[2] It has antiinflammatory actions,[3][4][5] has been used to study the interaction between GPR55 mediated and CB1 mediated activity,[6] and research using this compound has revealed a role for GPR55 in learning and memory.[7][8]
See also
References
- ↑ "Structure-Activity Relationship of the GPR55 Antagonist, CID16020046". Pharmacology 102 (5–6): 324–331. 2018. doi:10.1159/000493490. PMID 30296786.
- ↑ "A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function". The Journal of Pharmacology and Experimental Therapeutics 346 (1): 54–66. July 2013. doi:10.1124/jpet.113.204180. PMID 23639801.
- ↑ "The GPR55 antagonist CID16020046 protects against intestinal inflammation". Neurogastroenterology and Motility 27 (10): 1432–45. October 2015. doi:10.1111/nmo.12639. PMID 26227635.
- ↑ "Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis". Thrombosis and Haemostasis 116 (5): 987–997. October 2016. doi:10.1160/TH16-02-0139. PMID 27465665.
- ↑ "The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs)". Archives of Biochemistry and Biophysics 681: 108254. March 2020. doi:10.1016/j.abb.2020.108254. PMID 31904362.
- ↑ "2 versus GPR55 receptors". British Journal of Pharmacology 177 (8): 1865–1880. April 2020. doi:10.1111/bph.14958. PMID 31877572.
- ↑ "Blockade of GPR55 in the dorsolateral striatum impairs performance of rats in a T-maze paradigm". Behavioural Pharmacology 27 (4): 393–6. June 2016. doi:10.1097/FBP.0000000000000185. PMID 26292188.
- ↑ "A putative lysophosphatidylinositol receptor GPR55 modulates hippocampal synaptic plasticity". Hippocampus 27 (9): 985–998. September 2017. doi:10.1002/hipo.22747. PMID 28653801.
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