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Preladenant

CAS No. : 377727-87-2

產品活性：Preladenant is a potent and competitive antagonist of the human adenosine A2A receptor with a K_i of 1.1 nM and has over 1000-fold selectivity over other adenosine receptors.

研究領域：GPCR/G Protein

作用靶點：Adenosine Receptor

In Vitro: Preladenant also completely antagonizes cAMP in cells expressing the recombinant human A_2A receptor. Preladenant is determined to has K_B values of 1.3 nM at the A_2A receptor; the value is in good agreement with the K_i value determined in the radioligand binding assay. A similar functional assay with A_2B receptor-expressing cells is used to demonstrate selectivity over A_2B receptors. In this assay, the K_B value for Preladenant is 1.2 μM, indicating that Preladenant is 923-fold selective for the A_2A receptor over the A_2B receptor.

In Vivo: Preladenant (1 mg/kg) inhibits L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Preladenant exhibits antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test. Preladenant produces a dose-dependent reduction in parkinsonian scores at doses of 1 mg/kg (min score: 9.0) and 3 mg/kg (min score: 6.5). A subthreshold dose of Preladenant reduces minimum and mean parkinsonian scores in animals treated with 3 mg kg of L-Dopa to 5.25 and 6.88 respectively. A Wilcoxin test is used to compare individual treatments against vehicle. Preladenant (3 mg/kg), L-Dopa (3, 6, and 12 mg/kg), and the combination of Preladenant and L-Dopa (1 or 3 mg/kg+3 mg/kg) are all significantly improved on the minimum parkinsonian score. In addition, both the 12 mg/kg L-Dopa and L-Dopa+Preladenant groups are significantly improved on both minimum and mean parkinsonian scores relative to the 3 mg/kg L-Dopa group.

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