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PB28(一种有效的σ-2受体配体)的氚放射性标记:药代动力学和药效学特征

Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.

作者信息

Colabufo Nicola Antonio, Abate Carmen, Contino Marialessandra, Inglese Carmela, Ferorelli Savina, Berardi Francesco, Perrone Roberto

机构信息

Dipartimento Farmacochimico, Università degli Studi di Bari, via Orabona 4, 70125 Bari, Italy.

出版信息

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2183-7. doi: 10.1016/j.bmcl.2007.12.056. Epub 2007 Dec 25.

Abstract

A potent sigma-2 receptor ligand, known as PB28, was tritium radiolabelled and biologically evaluated. The results showed that [(3)H]PB28 and the corresponding unlabelled PB28 had superimposed pharmacodynamic properties. This radioligand appears as a potential candidate for receptor binding and in living cells assays.

摘要

一种名为PB28的强效σ-2受体配体被用氚进行放射性标记并进行了生物学评估。结果表明,[³H]PB28和相应的未标记PB28具有叠加的药效学特性。这种放射性配体似乎是受体结合和活细胞测定的潜在候选物。

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