后叶加压素受体拮抗剂的治疗潜力。

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阿里•F Guglin M, Vaitkevicius P Ghali JK

后叶加压素受体拮抗剂的治疗潜力。

药。2007;67 (6):847 - 58。

PubMed ID

17428103 (在PubMed

]

文摘

精氨酸加压素(AVP)是一种神经肽激素起着重要的作用在循环和体内平衡钠,和调节血清同渗重摩。几个临床条件与不当高浓度的AVP包括心力衰竭、肝硬化和抗利尿激素分泌不当综合征。三种受体亚型调解AVP的行为已确定(V(1),(2)和V (1 b))。激活V (1 a)受体位于血管平滑肌细胞和心肌导致血管收缩和后负荷增加和肥大。V(2)受体主要位于收集小管调节自由水的吸收。V (1 b)受体位于垂体前叶和调解adrenocorticotropin激素释放。AVP是介导的心血管和肾脏影响主要由V(1)和(2)受体。V (1 a)受体拮抗作用导致血管舒张和V(2)受体拮抗作用导致中,electrolyte-sparing水排泄。几个non-peptide avon拮抗剂(后叶加压素受体拮抗剂(vra))也称为“vaptans”已经开发和正在大力研究主要治疗条件的特点是hyponatraemia和液体超负荷。Conivaptan是一个结合V(1) /(2)受体拮抗剂,诱发利尿以及血液动力学的改善。 It has been shown in clinical trials to correct euvolaemic and hypervolaemic hyponatraemia, and has been approved by the US FDA for the treatment of euvolaemic hyponatraemia as an intravenous infusion. Tolvaptan, a selective V(2)-receptor antagonist, has undergone extensive clinical studies in the treatment of hyponatraemia and heart failure. It has been shown to effectively decrease fluid in volume overloaded patients with heart failure and to correct hyponatraemia. A large outcome study (n = 4133 patients) will define its role in the management of heart failure. Lixivaptan and satavaptan (SR-121463) are other selective V(2)-receptor antagonists being evaluated for the treatment of hyponatraemia. In addition, a potential role for the vaptans in attenuating polyuria in nephrogenic diabetes insipidus and cyst development in polycystic kidney disease is being explored. Ongoing clinical trials should further define the scope of the potential therapeutic role of VRAs.

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药物靶点

药物	目标	类	生物	药理作用	行动
Conivaptan	后叶加压素V1a受体	蛋白质	人类	是的	拮抗剂	细节
Conivaptan	后叶加压素V2受体	蛋白质	人类	是的	拮抗剂	细节