CID16020046 explained

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

Notes and References

  1. Brown AJ, Castellano-Pellicena I, Haslam CP, Nichols PL, Dowell SJ . 52938892 . Structure-Activity Relationship of the GPR55 Antagonist, CID16020046 . Pharmacology . 2018 . 102 . 5–6 . 324–331 . 30296786 . 10.1159/000493490 .
  2. Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M, Heinemann A . 17801 . 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 . 23639801 . 10.1124/jpet.113.204180 .
  3. Stančić A, Jandl K, Hasenöhrl C, Reichmann F, Marsche G, Schuligoi R, Heinemann A, Storr M, Schicho R . The GPR55 antagonist CID16020046 protects against intestinal inflammation . Neurogastroenterology and Motility . 27 . 10 . 1432–45 . October 2015 . 26227635 . 4587547 . 10.1111/nmo.12639 .
  4. Montecucco F, Bondarenko AI, Lenglet S, Burger F, Piscitelli F, Carbone F, Roth A, Liberale L, Dallegri F, Brandt KJ, Fraga-Silva RA, Stergiopulos N, Di Marzo V, Mach F . 6 . Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis . Thrombosis and Haemostasis . 116 . 5 . 987–997 . October 2016 . 27465665 . 10.1160/TH16-02-0139 .
  5. Wang Y, Pan W, Wang Y, Yin Y . 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 . 31904362 . 10.1016/j.abb.2020.108254 . 209895392 .
  6. Wang XF, Galaj E, Bi GH, Zhang C, He Y, Zhan J, Bauman MH, Gardner EL, Xi ZX . 6 . 2 versus GPR55 receptors . British Journal of Pharmacology . 177 . 8 . 1865–1880 . April 2020 . 31877572 . 10.1111/bph.14958 . 7070166 .
  7. Marichal-Cancino BA, Sánchez-Fuentes A, Méndez-Díaz M, Ruiz-Contreras AE, Prospéro-García O . 3627821 . Blockade of GPR55 in the dorsolateral striatum impairs performance of rats in a T-maze paradigm . Behavioural Pharmacology . 27 . 4 . 393–6 . June 2016 . 26292188 . 10.1097/FBP.0000000000000185 .
  8. Hurst K, Badgley C, Ellsworth T, Bell S, Friend L, Prince B, Welch J, Cowan Z, Williamson R, Lyon C, Anderson B, Poole B, Christensen M, McNeil M, Call J, Edwards JG . A putative lysophosphatidylinositol receptor GPR55 modulates hippocampal synaptic plasticity . Hippocampus . 27 . 9 . 985–998 . September 2017 . 28653801 . 5568947 . 10.1002/hipo.22747 .

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