CID16020046 is a compound which acts as an
inverse agonist at the former
orphan receptorGPR55,[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 CB2cannabinoid 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]
^Brown AJ, Castellano-Pellicena I, Haslam CP, Nichols PL, Dowell SJ (2018). "Structure-Activity Relationship of the GPR55 Antagonist, CID16020046". Pharmacology. 102 (5–6): 324–331.
doi:
10.1159/000493490.
PMID30296786.
S2CID52938892.
^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.
PMID23639801.
S2CID17801.
^Montecucco F, Bondarenko AI, Lenglet S, Burger F, Piscitelli F, Carbone F, et al. (October 2016). "Treatment with the GPR55 antagonist CID16020046 increases neutrophil activation in mouse atherogenesis". Thrombosis and Haemostasis. 116 (5): 987–997.
doi:
10.1160/TH16-02-0139.
PMID27465665.
^Wang Y, Pan W, Wang Y, Yin Y (March 2020). "The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs)". Archives of Biochemistry and Biophysics. 681: 108254.
doi:
10.1016/j.abb.2020.108254.
PMID31904362.
S2CID209895392.
^Marichal-Cancino BA, Sánchez-Fuentes A, Méndez-Díaz M, Ruiz-Contreras AE, Prospéro-García O (June 2016). "Blockade of GPR55 in the dorsolateral striatum impairs performance of rats in a T-maze paradigm". Behavioural Pharmacology. 27 (4): 393–6.
doi:
10.1097/FBP.0000000000000185.
PMID26292188.
S2CID3627821.