CID16020046

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]

CID16020046
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ECHA InfoCard100.233.214
Chemical and physical data
FormulaC25H19N3O4
Molar mass425.435 g·mol−1
3D model (JSmol)

See also

References
  1. Brown AJ, Castellano-Pellicena I, Haslam CP, Nichols PL, Dowell SJ. Structure-Activity Relationship of the GPR55 Antagonist, CID16020046. Pharmacology. 2018;102(5-6):324-331. doi:10.1159/000493490 PMID 30296786
  2. Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M, Heinemann A (July 2013). "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. doi:10.1124/jpet.113.204180. PMID 23639801.
  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. Neurogastroenterol Motil. 2015 Oct;27(10):1432-45. doi:10.1111/nmo.12639 PMID 26227635
  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. Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis. Thromb Haemost. 2016 Oct 28;116(5):987-997. PMID 27465665
  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). Arch Biochem Biophys. 2020 Mar 15;681:108254. doi:10.1016/j.abb.2020.108254 PMID 31904362
  6. Wang XF, Galaj E, Bi GH, Zhang C, He Y, Zhan J, Bauman MH, Gardner EL, Xi ZX. Different receptor mechanisms underlying phytocannabinoid- versus synthetic cannabinoid-induced tetrad effects: Opposite roles of CB1 /CB2 versus GPR55 receptors. Br J Pharmacol. 2020 Apr;177(8):1865-1880. doi:10.1111/bph.14958 PMID 31877572
  7. Marichal-Cancino BA, Sánchez-Fuentes A, Méndez-Díaz M, Ruiz-Contreras AE, Prospéro-García O. Blockade of GPR55 in the dorsolateral striatum impairs performance of rats in a T-maze paradigm. Behav Pharmacol. 2016 Jun;27(4):393-6. doi:10.1097/FBP.0000000000000185 {{pmid|26292188}
  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. 2017 Sep;27(9):985-998. doi:10.1002/hipo.22747 PMID 28653801


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