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Argipressin (acetate) Sale

(Synonyms: 精氨酸加压素) 目录号 : GC48997

A peptide hormone with vasoconstrictive and antidiuretic activities

Argipressin (acetate) Chemical Structure

Cas No.:129979-57-3

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1 mg
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产品描述

Argipressin is a peptide hormone with vasoconstrictive and antidiuretic activities that binds to the vascular arginine vasopressin receptor, V1, with Kd values of 1.31 and 1.44 nM in A7r5 rat aortic smooth muscle cells and neonatal rat cardiomyocytes, respectively.1,2 It also stimulates the intracellular release of calcium in A7r5 cells (EC50 = 5 nM).3 In rat models, argipressin induces hypertension and tachycardia when injected into the lateral septal nuclei at a dose of 100-400 ng and increases heart rate and mean arterial pressure (MAP) when injected into the medial amygdaloid body at a dose of 150-600 ng.4,5

1.Thibonnier, M., Bayer, A.L., Simonson, M.S., et al.Multiple signaling pathways of V1-vascular vasopressin receptors of A7r5 cellsEndocrinology129(6)2845-2856(1991) 2.Xu, Y.J., and Gopalakrishnan, V.Vasopressin increases cytosolic free [Ca2+] in the neonatal rat cardiomyocyte. Evidence for V1 subtype receptorsCirc. Res.69(1)239-245(1991) 3.Byron, K.L.Vasopressin stimulates Ca2+ spiking activity in A7r5 vascular smooth muscle cells via activation of phospholipase A2Circ. Res.78(5)813-820(1996) 4.Gao, L., Jiang, N.-C., Luo, Q.-H., et al.Cardiovascular effects of injection of argipressin into lateral septal nuclei in ratsZhongguo Yao Li Xue Bao.17(1)49-52(1996) 5.Jiang, N.-C., Gao, L., Chen, C., et al.Effects of argipressin injected into medial amygdaloid body on blood pressure and heart rate in ratsZhongguo Yao Li Xue Bao.14(2)118-120(1993)

Chemical Properties

Cas No. 129979-57-3 SDF
别名 精氨酸加压素
Canonical SMILES N[C@@H](CSSC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(NCC(N)=O)=O)CCCNC(N)=N)=O)=O)NC([C@H](CC(N)=O)N2)=O)C(N[C@@H](CC3=CC=C(O)C=C3)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](CCC(N)=O)C2=O)=O)=O)=O.CC(O)=O
分子式 C46H65N15O12S2·XC2H4O2 分子量 1084.2
溶解度 Water: 1 mg/ml 储存条件 -20°C
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1 mM 0.9223 mL 4.6117 mL 9.2234 mL
5 mM 0.1845 mL 0.9223 mL 1.8447 mL
10 mM 0.0922 mL 0.4612 mL 0.9223 mL
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Research Update

Desmopressin acetate nasal spray for adults with nocturia

Expert Rev Clin Pharmacol 2017 Dec;10(12):1281-1293.PMID:29048257DOI:10.1080/17512433.2017.1394185.

Nocturia impacts 70% of individuals over age 70 years. Nocturnal polyuria is present in up to 88% of adults with nocturia, however, treatment options for reducing nighttime urine production have historically been limited to behavioral modification and off label use of timed diuretics and desmopressin. NoctivaTM (desmopressin acetate nasal spray, DANS, Serenity Pharmaceuticals, LLC) is a novel formulation of desmopressin approved by the Food and Drug Administration for the treatment of nocturia due to nocturnal polyuria in March 2017. Areas covered: Incidence and etiology of nocturia, currently available therapies (approved and off label), and pharmacokinetic, efficacy, and safety data associated with DANS. Expert commentary: DANS has been studied for the treatment of nocturia in adults over age 50 without contraindications to the use of desmopressin. 49% receiving the higher clinical dose experienced ≥50% reduction in nocturnal voids in clinical trials vs. 30% with placebo. Although nadir serum sodium <135 mmol/L was not uncommon (14%), the incidence of sodium ≤125 mmol/L was rare (1%). DANS therefore appears to benefit a significant subset of patients with nocturia while maintaining an acceptable risk profile. Given the risks of hyponatremia, education of patients and prescribers in contraindications and the importance of monitoring are paramount.

Desmopressin acetate (DDAVP) for preventing and treating acute bleeds during pregnancy in women with congenital bleeding disorders

Cochrane Database Syst Rev 2015 Sep 9;(9):CD009824.PMID:26350784DOI:10.1002/14651858.CD009824.pub3.

Background: Congenital bleeding disorders can cause obstetric haemorrhage during pregnancy, labour and following delivery. Desmopressin acetate is found to be an effective drug which can reduce the risk of haemorrhage and can also stop bleeding in certain congenital bleeding disorders. Its use in pregnancy has been controversial. Hence beneficial and adverse effects of desmopressin acetate in these groups of pregnant women should be evaluated.This is an update of a Cochrane review first published in 2013. Objectives: To determine the efficacy of desmopressin acetate in preventing and treating acute bleeds during pregnancy in women with congenital bleeding disorders. Search methods: We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group's Coaguopathies Trials Register comprising references identified from comprehensive electronic database searches and handsearches of relevant and abstract books of conferences proceedings. We also searched for any randomised controlled trials in a registry of ongoing trials and the reference lists of relevant articles and reviews.Date of most recent search: 18 June 2015. Selection criteria: Randomised and quasi-randomised controlled trials investigating the efficacy of desmopressin acetate versus tranexamic acid or factor VIII or rFactor VII or fresh frozen plasma in preventing and treating congenital bleeding disorders during pregnancy were eligible. Data collection and analysis: No trials matching the selection criteria were eligible for inclusion. Main results: No trials matching the selection criteria were eligible for inclusion. Authors' conclusions: The review did not identify any randomised controlled trials investigating the relative effectiveness of desmopressin acetate for bleeding during pregnancy in women with congenital bleeding disorders. In the absence of high quality evidence, clinicians need to use their clinical judgement and lower level evidence (e.g. from observational trials) to decide whether or not to treat women with congenital bleeding disorders with desmopressin acetate.Given the ethical considerations, future randomised controlled trials are unlikely. However, other high quality controlled studies (such as risk allocation designs, sequential design, parallel cohort design) to investigate the risks and benefits of using desmopressin acetate in this population are needed.

Desmopressin acetate (DDAVP) for preventing and treating acute bleeds during pregnancy in women with congenital bleeding disorders

Cochrane Database Syst Rev 2013 Apr 30;(4):CD009824.PMID:23633378DOI:10.1002/14651858.CD009824.pub2.

Background: Congenital bleeding disorders can cause obstetric haemorrhage during pregnancy, labour and following delivery. Desmopressin acetate is found to be an effective drug which can reduce the risk of haemorrhage and can also stop bleeding in certain congenital bleeding disorders. Its use in pregnancy has been controversial. Hence beneficial and adverse effects of desmopressin acetate in these groups of pregnant women should be evaluated. Objectives: To determine the efficacy of desmopressin acetate in preventing and treating acute bleeds during pregnancy in women with congenital bleeding disorders. Search methods: We searched the Cochrane Cystic Fibrosis and Genetic Disorders Group's Coaguopathies Trials Register comprising references identified from comprehensive electronic database searches and handsearches of relevant and abstract books of conferences proceedings. We also searched for any randomised controlled trials in a registry of ongoing trials and the reference lists of relevant articles and reviews.Date of most recent search: 28 February 2013. Selection criteria: Randomised and quasi-randomised controlled trials investigating the efficacy of desmopressin acetate versus tranexamic acid or factor VIII or rFactor VII or fresh frozen plasma in preventing and treating congenital bleeding disorders during pregnancy were eligible. Data collection and analysis: No trials matching the selection criteria were eligible for inclusion. Main results: No trials matching the selection criteria were eligible for inclusion. Authors' conclusions: The review did not identify any randomised controlled trials investigating the relative effectiveness of desmopressin acetate for bleeding during pregnancy in women with congenital bleeding disorders. In the absence of high quality evidence, clinicians need to use their clinical judgement and lower level evidence (e.g. from observational trials) to decide whether or not to treat women with congenital bleeding disorders with desmopressin acetate.Given the ethical considerations, future randomised controlled trials are unlikely. However, other high quality controlled studies (such as risk allocation designs, sequential design, parallel cohort design) to investigate the risks and benefits of using desmopressin acetate in this population are needed.

Desmopressin acetate the first sublingual tablet to treat nocturia due to nocturnal polyuria

Expert Rev Clin Pharmacol 2021 Aug;14(8):939-954.PMID:33993824DOI:10.1080/17512433.2021.1931122.

Introduction: Desmopressin was widely used to treat nocturnal polyuria in adults under the age of 65 due to the well-established risk of hyponatremia. Since the prevalence of nocturia increases with age, and with an aging population, those most affected were excluded from treatment. Recently, a new lower dose sublingual tablet formulation that optimizes the balance between efficacy and tolerability has been licensed for symptomatic treatment of nocturia due to idiopathic nocturnal polyuria in adults of any age, with the caveat of regular serum monitoring for those over 65. This newer formulation aims to achieve the same clinical outcomes as previous formulations while reducing the risk of hyponatremia.Areas covered: This review will look at the pharmacology of the newly formulated desmopressin and examine the results of the clinical trials that would support its treatment of adult nocturia with idiopathic nocturnal polyuria.Expert opinion: When reporting on the clinical efficacy of desmopressin on nocturia, it is important for clinical trials to publish their complete data on nocturnal and 24-hour urine voided volumes. Further research examining the physiological reasoning behind this gender-specific dosing for desmopressin and the optimal recommended treatment duration of desmopressin for those over 65 is needed.

Cardiopulmonary bypass

Curr Opin Cardiol 1991 Apr;6(2):227-34.PMID:10171173DOI:10.1097/00001573-199104000-00009.

There has been a recent renewed interest in certain aspects of cardiopulmonary bypass employing extracorporeal circulation. Several areas have received special attention. Among these is the institution of extracorporeal circulation using a percutaneous technique for circulatory assistance during high-risk percutaneous transluminal coronary angioplasty. A national registry has been established to review and monitor results using this percutaneous technique. Several recent developments in the delivery of cardioplegia during ischemic arrest have stimulated investigative efforts. In particular, the delivery of cardioplegia in a retrograde manner through the coronary sinus has proved an effective and useful adjunct to myocardial protection during cardiopulmonary bypass with extracorporeal circulation. A newer investigative technique employing only warm cardioplegia delivered primarily through the retrograde coronary sinus route seems to offer some promise in providing optimal myocardial protection while minimizing hemorrhagic complications and other cold-induced myocardial injury. Because of concerns regarding blood transfusion-related communicable disease (eg, acquired immune deficiency syndrome and non-A, non-B hepatitis), there has been increasing research effort into postoperative hemorrhage related to cardiopulmonary bypass with extracorporeal circulation. Specifically, various drugs that may serve as hemostatic adjuncts have been investigated extensively. These drugs include aprotinin and desmopressin acetate. Likewise, several studies have evaluated other drugs (mainly aspirin) that have a negative influence on postoperative hemostasis. Additionally, there has been continued research interest in the activation of the inflammatory system during cardiopulmonary bypass.(ABSTRACT TRUNCATED AT 250 WORDS)