首页> 外国专利> Method of screening for a drug candidate that increases ATP release from RBCs stimulated via the Gs or Gi pathway

Method of screening for a drug candidate that increases ATP release from RBCs stimulated via the Gs or Gi pathway

机译:筛选增加通过Gs或Gi途径刺激的RBC中ATP释放的候选药物的方法

摘要

The invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCs treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCs. Likewise, RBCs of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCs. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release by RBCs. Thus the invention is directed to compositions and methods for improving ATP release by RBCs, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.
机译:本发明基于以下发现:红细胞含有磷酸二酯酶3B(PDE3B),并且对该磷酸二酯酶的抑制允许cAMP的积累增加和随后的ATP释放。进一步发现,与正常的RBC相比,用胰岛素处理的RBC累积的cAMP明显减少,而释放的ATP则明显减少。同样,患有2型糖尿病(高胰岛素血症)的患者的RBC累积的cAMP明显少于正常RBC,释放的ATP明显少。进一步发现,前列腺素类似物与磷酸二酯酶3B抑制剂协同作用,以改善或增加红细胞的cAMP积累和ATP释放。因此,本发明涉及通过施用PDE3B抑制剂或PDE3B抑制剂和前列腺素类似物的组合改善RBCs释放ATP的组合物和方法。

著录项

  • 公开/公告号US8084221B2

    专利类型

  • 公开/公告日2011-12-27

    原文格式PDF

  • 申请/专利权人 RANDY S SPRAGUE;MADELYN STUMPF;

    申请/专利号US20070695102

  • 发明设计人 RANDY S SPRAGUE;MADELYN STUMPF;

    申请日2007-04-02

  • 分类号G01N33/53;

  • 国家 US

  • 入库时间 2022-08-21 17:26:13

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