An antagonist of CCR3
GW 766994 is an antagonist of chemokine (C-C motif) receptor 3 (CCR3) with a Ki value of 13.8 nM in an assay of eosinophil chemotaxis induced by chemokine (C-C motif) ligand 11 (CCL11).1 It decreases CCL11-induced cyclin-dependent kinase 5 (Cdk5) and tau phosphorylation and production of amyloid β (1-42) (Aβ42) in isolated mouse hippocampal neurons when used at a concentration of 10 ?M.2
1.Neighbour, H., Boulet, L.-P., Lemiere, C., et al.Safety and efficacy of an oral CCR3 antagonist in patients with asthma and eosinophilic bronchitis: A randomized, placebo-controlled clinical trialClin. Exp. Allergy44(4)508-516(2014) 2.Zhu, C., Xu, B., Sun, X., et al.Targeting CCR3 to reduce amyloid-β production, tau hyperphosphorylation, and synaptic loss in a mouse model of Alzheimer's diseaseMol. Neurobiol.54(10)7964-7978(2017)
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