从进化角度揭示枸橼酸岑沙喹在低血容量休克中的复苏治疗潜力

IF 2.7 4区 医学 Q3 NEUROSCIENCES CNS & neurological disorders drug targets Pub Date : 2024-01-01 DOI:10.2174/1871527322666230623113013
Ravinder Singh, Varinder Singh, Pratima Kumari, Namita Aggarwal, Muskaan Oberoi, Heena Khan, Thakur Gurjeet Singh
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引用次数: 0

摘要

低血容量性休克(HS)是一种身体组织血液灌注和氧合不足的临床症状,与巨大的发病率和死亡率相关。治疗方法包括补充液体和手术修复可逆的出血原因,但这些方法会导致不可逆的血液灌注损失、全身炎症、多器官衰竭和死亡。枸橼酸噻喹酯(CC)是一种创新的中枢作用型心血管活性药物,最初被用作降压药。它作用于α2B-肾上腺素能受体,产生静脉收缩,继而增加回流到心脏的静脉。据推测,这些作用可通过增加心输出量和组织灌注,使枸橼酸仙噻喹发挥复苏作用。在动物和人体中进行的药代动力学研究表明,枸橼酸仙哈喹的耐受性良好,副作用也不明显。因此,枸橼酸 centhaquin 似乎是一种很有前景的药物,研究人员对将其开发为 HS 复苏药物越来越感兴趣。本综述深入探讨了枸橼酸 centhaquin 作为复苏剂的发展情况,并深入探讨了相关的作用机制和分子信号传导,以促进今后对 CC 的研究,从而将其用于 HS 的临床治疗。
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Evolutionary Unmasking Resuscitative Therapeutics Potential of Centhaquin Citrate in Hypovolemic Shock.

Hypovolemic shock (HS), a clinical condition of insufficient blood perfusion and oxygenation in body tissues, is associated with immense morbidity and mortality. Treatment approaches include fluid replacement and surgical repair of reversible causes of hemorrhage; however, they cause irreversible blood perfusion loss, systemic inflammation, multiple organ failure, and death. Centhaquin citrate (CC) is an innovative centrally acting cardiovascular active agent that is initially intended as an antihypertensive drug. However, due to its positive ionotropic effect, Centhaquin citrate is being tested clinically as a resuscitative agent for the management of hypovolemic shock It acts at the α2B-adrenergic receptor to produce venous constriction followed by an increase in venous return to the heart. These actions are assumed to be capable of resuscitative activity observed by centhaquin citrate, through an increase in cardiac output and tissue perfusion. Pharmacokinetics investigations in animals and humans have shown that centhaquin citrate is well tolerated and has insignificant side effects. Therefore, centhaquin citrate seems to be a promising entity and gaining the interest of researchers to develop it as a resuscitative agent in HS. The review gives insight into the development of centhaquin citrate as a resuscitative agent and provides insight into the associated mechanism of action and molecular signalling to foster future research on CC for its clinical use in HS.

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来源期刊
CiteScore
5.10
自引率
3.30%
发文量
158
审稿时长
6-12 weeks
期刊介绍: Aims & Scope CNS & Neurological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes. CNS & Neurological Disorders - Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of CNS & neurological drug targets. The journal also accepts for publication original research articles, letters, reviews and drug clinical trial studies. As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.
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