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Argipressin (Vasopressin) Sale

(Synonyms: 精氨加压素; Arg8-vasopressin; AVP) 目录号 : GC30764

精氨酸加压素作为调节血浆渗透压和血容量/血压的重要激素,一直被用于治疗感染性休克和失代偿性肝硬化。

Argipressin (Vasopressin) Chemical Structure

Cas No.:113-79-1

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10mM (in 1mL Water)
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Sample solution is provided at 25 µL, 10mM.

Description

Arginine-vasopressin, as an important hormone in the regulation of plasma osmolality and blood volume/pressure, always is used in the treatment of septic shock and decompensated cirrhosis.[1]

In vitro experiment it shown that treatment with 5-10 μM argipressin (vasopressin) in RN46A cells decreased RN46A proliferation, while 10 μM argipressin (vasopressin) decreased the number of cells extending neurites. [2] In vitro, treatment with 0.1 μM and 1 μM. argipressin (vasopressin)in PV cardiomyocytes, there had a faster dose dependent beating rate than control PV cardiomyocytes by 4 and 37% respectively. [3] In vitro, Arginine vasopressin (10-12M-10-6M) can induce markedly concentration-dependent increases of insulin release from both rodent and human beta-cells, as well as mouse islets.[4] Moreover, treatment with 100 pM to 1 μM Arginine-vasopressin in the non-neuronal cells evoked [Ca2+](i) responses and had concentration-dependent responses increased with days in vitro in culture, reaching a maximum amplitude after 4-5 day. [5]

In vivo efficacy test it exhibited that argipressin (vasopressin) shown antinociception in the hot-plate test after intracerebroventricular injection (0.5 ug) and in the acetic acid abdominal constriction test after intraperitoneal injection (0.1 mg/kg).[6] In vivo experiment it demonstrated that treatment with 0.5 u/kg arginine vasopressin intravenously significantly increased the levels of IL-6 mRNA in rat hearts with the maximum level occurred at 6 h.[7]

References:

[1] Wagener G, Bakker J. Vasopressin in cirrhosis and sepsis: physiology and clinical implications. Minerva Anestesiol. 2015 Dec;81(12):1377-83. Epub 2014 Nov 11.

[2] Marinova Z, et al. Effects of oxytocin and Argipressin (Vasopressin) on the proliferation and differentiation of a serotonergic cell line. J Neural Transm (Vienna). 2018 Jan;125(1):103-106.

[3] Huang JH, et al. Argipressin (Vasopressin) modulates electrical activity and calcium homeostasis in pulmonary vein cardiomyocytes. J Biomed Sci. 2019 Sep 17;26(1):71.

[4] Mohan S, et al. Vasopressin receptors in islets enhance glucose tolerance, pancreatic beta-cell secretory function, proliferation and survival. Biochimie. 2019 Mar;158:191-198.

[5] Moriya T, et al. Vasopressin-induced intracellular Ca2? concentration responses in non-neuronal cells of the rat dorsal root ganglion. Brain Res. 2012 Nov 5;1483:1-12.

[6] Hart SL, Oluyomi AO. Vasopressin and stress-induced antinociception in the mouse. Br J Pharmacol. 1990 Feb;99(2):243-6.

[7] Sun SZ, et al. β-Arrestin 2 mediates Argipressin (Vasopressin)-induced IL-6 induction via the ERK1/2-NF-κB signal pathway in murine hearts. Acta Pharmacol Sin. 2020 Feb;41(2):198-207.

精氨酸加压素作为调节血浆渗透压和血容量/血压的重要激素,一直被用于治疗感染性休克和失代偿性肝硬化。[1]

体外实验表明,用 5-10 μM argipressin(血管加压素)处理 RN46A 细胞会降低 RN46A 的增殖,而 10 μM argipressin(血管加压素)会减少延伸轴突的细胞数量。 [2] 在体外,用 0.1 μM 和 1 μM 处理。 PV 心肌细胞中的 argipressin(血管加压素),其剂量依赖性搏动率比对照 PV 心肌细胞分别快 4% 和 37%。 [3] 在体外,精氨酸加压素 (10-12M-10-6M) 可显着增加胰岛素释放的浓度依赖性来自啮齿动物和人类 β 细胞以及小鼠胰岛。[4] 此外,在非神经元细胞中用 100 pM 至 1 μM 精氨酸加压素处理可诱发 [Ca2+ ](i) 反应和浓度依赖性反应随着体外培养天数的增加而增加,在 4-5 天后达到最大幅度。 [5]

体内药效试验表明,argipressin(血管加压素)在侧脑室注射(0.5 ug)后的热板试验和腹腔注射(0.1 mg/kg)后的醋酸缩腹试验中均表现出镇痛作用。 [6] 体内实验表明,静脉注射0.5 u/kg精氨酸加压素可显着提高大鼠心脏IL-6 mRNA水平,并在6 h时达到最大值。[7]

实验参考方法

Cell experiment [1]:

Cell lines

PV cardiomyocytes

Preparation Method

For the measurement of SR Ca2+ leak, PV cardiomyocytes were incubated with argipressin (vasopressin)(1 µM) or Argipressin (Vasopressin)(1 µM) plus KN-93 (a Ca2+/calmodulin-dependent protein kinase II, CaMKII inhibitor, 1 µM) for 4~6 h before experiments.

Reaction Conditions

1 µM; 4~6 h

Applications

Spontaneous Ca2+ transients in argipressin (vasopressin) (1 µM)-treated PV cardiomyocytes were smaller than those in the control by 67%. Argipressin (Vasopressin)(1 µM)-treated PV cardiomyocytes had greater Ca2+ leak than the control, which was attenuated by the presence of KN-93 (1 µM).

Animal experiment [2]:

Animal models

Rats

Dosage form

1.0 or 5.0 ug/kg; s.c.

Preparation method

Rats were injected with a single subcutaneous dose of either saline, argipressin (vasopressin) (1.0 or 5.0 ug/kg), or an argipressin (vasopressin) analog with only weak endocrinological activity, des-gly-argipressin vasopressin ( 1.0, 5.0 or 10.0 ug/kg). Additional extinction trials were conducted at 2, 4, 6 and 8 h post-injection.

Applications

Argipressin (Vasopressin) potentiated this radial maze extinction behavior while DG-AVP produced behavioral results directionally opposite to those predicted by a memory facilitation hypothesis. In a subsequent experiment, vasopressin had no effects on unconditioned locomotor activity measured 2 and 4 h post-injection.

References:

[1] Huang JH, et al. Argipressin (Vasopressin) modulates electrical activity and calcium homeostasis in pulmonary vein cardiomyocytes. J Biomed Sci. 2019 Sep 17;26(1):71.

[2] Packard MG, et al. Effects of peripherally injected vasopressin and des-glycinamide vasopressin on the extinction of a spatial learning task in rats. Regul Pept. 1985 May;11(1):51-63.

化学性质

Cas No. 113-79-1 SDF
别名 精氨加压素; Arg8-vasopressin; AVP
Canonical SMILES Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH2 (Disulfide bridge: Cys1-Cys6)
分子式 C46H65N15O12S2 分子量 1084.23
溶解度 Water : ≥ 360 mg/mL (332.03 mM) 储存条件 Store at -20°C
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1 mM 0.9223 mL 4.6116 mL 9.2231 mL
5 mM 0.1845 mL 0.9223 mL 1.8446 mL
10 mM 0.0922 mL 0.4612 mL 0.9223 mL
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