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血管紧张素II

血管紧张素II用途

Angiotensin II human 是由 Angiotensin I 经过血管紧张素转换酶 (ACE) 催化移除 C 末端残基而得到。Angiotensin II 由 AT₁ 和 AT₂ 受体调节。

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血管紧张素II名称

[ CAS 号 ]:
4474-91-3

[ 中文名 ]:
人血管紧张素II

[ 英文名 ]:
Angiotensin II acetate salt

[中文别名 ]:

[英文别名 ]:

Angiotensin II
ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE
Angiotensin II human

血管紧张素II生物活性

[ 描述 ]:

Angiotensin II human是作用于 AT1 和 AT2 受体的血管收缩剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管紧张素受体

研究领域 >> 心血管疾病

天然产物 >> 其他

多肽产品

[ 靶点 ]

Angiotensin receptor (AT receptor)[1]

[体外研究]

血管紧张素II(Ang II)的大多数已知作用是由AT1受体介导的,AT2受体有助于调节血压和肾功能[1]。血管紧张素II通过许多作用引起血压(BP),最重要的是血管收缩,交感神经刺激,醛固酮生物合成增加和肾脏作用。其他血管紧张素II作用包括诱导生长,细胞迁移和血管平滑肌细胞的有丝分裂,成纤维细胞中I型和III型胶原的合成增加,导致血管壁和心肌增厚,以及纤维化。这些作用由1型Ang II受体(AT1)介导[2]。在细胞水平上,两种血管紧张素受体(AT1和AT2)的表达赋予对血管紧张素II的反应。血管紧张素II对血压升高的影响是由AT1受体介导的[3]。

[体内研究]

为了区分对于高血压发病机制至关重要的AT1受体群体,将渗透性微型泵皮下植入每只动物中以连续输注血管紧张素II(1,000ng/kg/min)持续4周。血管紧张素II通过激活肾脏中的AT1受体促进钠重吸收而引起高血压[3]。

[动物实验]

使用缺乏血管紧张素II的AT1A受体的小鼠[3]（129×C57BL / 6）F1小鼠。给小鼠喂食含有所有营养素和水的10克/天凝胶0.25％NaCl饮食。在基线收集1周后，给动物植入注入血管紧张素II的渗透性微型泵，并再次返回代谢笼5天。通过使用IL943自动火焰光度计测定尿钠含量。在输注血管紧张素II 28天后，收获心脏，称重，在福尔马林中固定，切片，并用Masson三色染色。所有组织都由病理学家（PR）检查，不知道基因型。

[参考文献]

[1]. de Gasparo M, et al. International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev. 2000 Sep;52(3):415-72.

[2]. Fyhrquist F, et al. Role of angiotensin II in blood pressure regulation and in the pathophysiology of cardiovascular disorders. J Hum Hypertens. 1995 Nov;9 Suppl 5:S19-24.

[3]. Crowley SD, et al. Angiotensin II causes hypertension and cardiac hypertrophy through its receptors in the kidney. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17985-90.

[相关活性小分子]

血管紧张素II物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
809.08°C (rough estimate)

[ 分子式 ]:
C₅₀H₇₁N₁₃O₁₂

[ 分子量 ]:
1046.179

[ 精确质量 ]:
1045.534546

[ PSA ]:
406.34000

[ LogP ]:
2.34

[ 外观性状 ]:
白色至浅黄色粉末

[ 折射率 ]:
1.664

[ 储存条件 ]:
-20°C

血管紧张素II毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BW2165000

CHEMICAL NAME :: Angiotensin II, 5-L-isoleucine-

CAS REGISTRY NUMBER :: 4474-91-3

LAST UPDATED :: 199712

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C50-H71-N13-O12

MOLECULAR WEIGHT :: 1046.34

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17400 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6079,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 30800 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6079,1990 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 119 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6109,1990

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血管紧张素II安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
BW2165000

血管紧张素II合成路线

详细合成路线

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血管紧张素II文献

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IGF-1 deficiency impairs cerebral myogenic autoregulation in hypertensive mice.

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Effects of a domain-selective ACE inhibitor in a mouse model of chronic angiotensin II-dependent hypertension.

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The somatic isozyme of ACE (angiotensin I-converting enzyme) comprises two distinct zinc-dependent catalytic domains with different substrate specificities for angiotensin I (cleaved selectively by th...

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