Department of Molecular Biochemistry, Faculty of Chemistry, University of Gdańsk, Wita Stwosza 63, 80-308 Gdansk, Poland.
Int J Mol Sci. 2022 Mar 12;23(6):3068. doi: 10.3390/ijms23063068.
Human neurohormone vasopressin (AVP) is synthesized in overlapping regions in the hypothalamus. It is mainly known for its vasoconstricting abilities, and it is responsible for the regulation of plasma osmolality by maintaining fluid homeostasis. Over years, many attempts have been made to modify this hormone and find AVP analogues with different pharmacological profiles that could overcome its limitations. Non-peptide AVP analogues with low molecular weight presented good affinity to AVP receptors. Natural peptide counterparts, found in animals, are successfully applied as therapeutics; for instance, lypressin used in treatment of diabetes insipidus. Synthetic peptide analogues compensate for the shortcomings of AVP. Desmopressin is more resistant to proteolysis and presents mainly antidiuretic effects, while terlipressin is a long-acting AVP analogue and a drug recommended in the treatment of varicose bleeding in patients with liver cirrhosis. Recently published results on diverse applications of AVP analogues in medicinal practice, including potential lypressin, terlipressin and ornipressin in the treatment of SARS-CoV-2, are discussed.
人类神经激素血管升压素 (AVP) 在下丘脑的重叠区域合成。它主要以其血管收缩能力而闻名，负责通过维持液体平衡来调节血浆渗透压。多年来，人们一直试图修饰这种激素，并寻找具有不同药理学特征的 AVP 类似物，以克服其局限性。具有低分子量的非肽 AVP 类似物对 AVP 受体具有良好的亲和力。在动物中发现的天然肽对应物成功地用作治疗药物；例如，加压素用于治疗尿崩症。合成肽类似物弥补了 AVP 的缺点。去氨加压素更能抵抗蛋白水解，主要表现出抗利尿作用，而特利加压素是一种长效 AVP 类似物，也是推荐用于治疗肝硬化患者静脉曲张出血的药物。本文讨论了 AVP 类似物在医学实践中的不同应用，包括加压素、特利加压素和奥曲肽在 SARS-CoV-2 治疗中的潜在应用。
