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血管加压素受体拮抗剂:潜在适应症及临床结果

Vasopressin receptor antagonists: potential indications and clinical results.

作者信息

Arai Yukinori, Fujimori Akira, Sudoh Katsumi, Sasamata Masao

机构信息

Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc, 21 Miyukigaoka, Tsukuba-Shi, Ibaraki, Japan.

出版信息

Curr Opin Pharmacol. 2007 Apr;7(2):124-9. doi: 10.1016/j.coph.2006.09.009. Epub 2007 Feb 9.

Abstract

Hyponatremia is a common electrolyte disorder with the potential to cause serious neurological complications. Conventional therapies for hyponatremia have been found to be inconsistently effective. Arginine vasopressin (AVP) is etiologically critical for hyponatremia, and it has been proven that AVP receptor (AVP-R) antagonists normalize serum sodium levels in hyponatremic patients. Additionally, one of these drugs showed potential for reducing mortality in patients with decompensated heart failure and for suppressing the progression of genetic renal disease in animals. The first non-peptide AVP-R antagonist has recently been approved in the United States. It is expected that this approval will accelerate the development of future clinical applications of AVP-R antagonists and open the door to a new era in the treatment of these intractable diseases.

摘要

低钠血症是一种常见的电解质紊乱,有可能导致严重的神经并发症。传统的低钠血症治疗方法已被发现效果不一。精氨酸加压素(AVP)在低钠血症的病因学中至关重要,并且已经证明AVP受体(AVP-R)拮抗剂可使低钠血症患者的血清钠水平恢复正常。此外,其中一种药物显示出降低失代偿性心力衰竭患者死亡率以及抑制动物遗传性肾病进展的潜力。第一种非肽类AVP-R拮抗剂最近已在美国获得批准。预计这一批准将加速AVP-R拮抗剂未来临床应用的开发,并为治疗这些难治性疾病开启一个新时代。

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