Preladenant
Adenosine A2A receptor antagonist / Preladenant is a potent (Ki = 1.1nM) and selective (>1000-fold over other adenosine receptors) adenosine A2A antagonist.1 It has shown efficacy in rodent and primate models of Parkinsons disease without inducing dyskinesias and displays antidepressant effects.1-3 It has been shown that activation of the adenosine A2A receptor blocks the activation of immune cells and increases the number of regulatory T-cells.4-6 Currently in clinical trials as combination therapy with pembrolizumab.7
Biochemicals & reagents
377727-87-2
SCH 420814
1) Hodgson et al. (2009), Characterization of the potent and selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimodin-5-amine] in rat models of movement disorders and depression; J.Pharmacol.Exp.Ther. 330 294 2) Hodgson et al. (2010), Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders; Exp.Neurol. 225 384 3) Pinna et al. (2016), Antidyskinetic effect of A2A and 5HT1A/B receptor ligands in two animal models of Parkinson's disease; Mov.Disord. 31 501 4) Beavis et al. (2013), Blockade of A2A receptors potently suppresses the metastasis of CD73+ tumors; Proc.Natl.Acad.Sci USA. 110 14711 5) Hatfield and Sitkovsky (2016), A2A adenosine receptor antagonist to weaken the hypoxia-HIF-1a driven immunosuppression and improve immunotherapies of cancer; Curr.Opin.Pharmacol. 29 90 6) Ohta et al. (2016), A metabolic immune checkpoint: adenosine in the tumor microenvironment; Front.Immunol. 7 1 7) NCT03099161
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TARGET: GPCR -- PATHWAY: cAMP / cGMP signaling -- RESEARCH AREA: Immunology; Neuroscience -- DISEASE AREA: Neurodegeneration; Mood disordersCancer