AL 8810 isopropyl ester

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Background

EC50: 430 nMAL 8810 is a a FP receptor antagonist.Prostaglandin F receptor (FP), a receptor belonging to the prostaglandin (PG) group of receptors, binds to and mediates the biological actions of Prostaglandin F2α (PGF2α).In vitro: Previous study found that AL-8810 had weak agonist potency in A7r5 cells and 3T3 fibroblasts. AL-8810 exhibited properties of an apparent competitive antagonist, which was demonstrated by producing parallel dextral shifts of the agonist concentration-response curves and no significant suppression of the maximal agonist-induced response. In addition, AL-8810 could dose-dependently antagonize the response to 100 nM fluprostenol in A7r5 cells, but however, AL-8810 could not significantly inhibit functional responses of DP, TP, EP(2), EP(4), receptor subtypes even at 10 μM concentration [1]. In vivo: In a previous study, the effect of acute intraperitoneal post-treatment with AL-8810 was studied in FP receptor knockout (FP-/-) mice after controlled cortical impact (CCI). Results showed that post-treatment with AL-8810 had no significant effect on cortical lesions, suggesting the irreversible effect of primary CCI injury, but significantly reduced hippocampal swelling. In addition, AL-8810 treatment at a dose of 10 mg/kg could significantly improve NDS after CCI, and in the AL-8810 group, CCI-induced decrease in grip strength was three-fold less [2]. Clinical trial: Up to now, AL 8810 is still in the preclinical development stage.

[1] B. W. Griffen, P. Klimko, J. Y. Crider, et al. AL-8810: A novel prostaglandin F2α analog with selective antagonist effects at the prostaglandin F2α (FP) receptor. Journal of Pharmacology and Experimental Therapeutics 290(3), 1278-1284 (1999).
[2] Glushakov AV, Robbins SW, Bracy CL, Narumiya S, Doré S. Prostaglandin F2α FP receptor antagonist improves outcomes after experimental traumatic brain injury. J Neuroinflammation. 2013 Oct 30;10:132. doi: 10.1186/1742-2094-10-132.