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盐酸去氧肾上腺素

盐酸去氧肾上腺素用途

(R)-(-)-Phenylephrine hydrochloride是一种选择性的α1-肾上腺素能受体激动剂,对α1D,α1B 和α1A 受体的pKis 分为5.86,4.87和4.70。

盐酸去氧肾上腺素名称

[ CAS 号 ]:
61-76-7

[ 中文名 ]:
盐酸去氧肾上腺素

[ 英文名 ]:
Phenylephrine hydrochloride

[中文别名 ]:

[英文别名 ]:

consdrin
(R)-(-)-Phenylephrine (hydrochloride)
almefrin
synasal
phenylephrine HCl
emagrin
fenilfar
AK-Dilate
rhinall
AK-Nefrin

盐酸去氧肾上腺素生物活性

[ 描述 ]:

(R)-(-)-Phenylephrine hydrochloride是一种选择性的α1-肾上腺素能受体激动剂,对α1D,α1B 和α1A 受体的pKis 分为5.86,4.87和4.70。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 心血管疾病

[ 靶点 ]

pKi: 5.86 (α1D), 5.86 (α1B), 5.86 (α1A)[1]

[体外研究]

(R)-(-)-去氧肾上腺素是一种选择性α1-肾上腺素能受体激动剂,α1D,α1B和α1A受体的pKi值分别为5.86,4.87和4.70 [1] [2]。去氧肾上腺素促进心脏成纤维细胞增殖。去氧肾上腺素激活CaN并引起NFAT3核转位。这表明Ca(2 +)/ CaN/NFAT途径介导苯肾上腺素诱导的心脏成纤维细胞增殖,这种途径可能是心脏纤维化的可能治疗靶点[3]。

[体内研究]

用100μM去氧肾上腺素灌注心脏导致两种p38-MAPK同种型的快速(最大10分钟)12倍活化。 α1-肾上腺素受体激动剂如去氧肾上腺素增加心脏的收缩性。去氧肾上腺素还可激活新生儿心室肌细胞中的SAPKs/JNKs [4]。去氧肾上腺素可以增加高潮气量通气大鼠的肺泡液清除率,加速肺水肿的吸收[5]。

[动物实验]

大鼠：使用随机数表将170只雄性Wistar大鼠随机分成17组（n = 10）。进行具有高潮气量的短期（40分钟）机械通气以诱导肺损伤，损害大鼠中的活性Na +转运和肺液清除。不通风的大鼠用作对照。为了证明去氧肾上腺素对肺泡液清除率的影响，将不同浓度（10,1,0.1,0.01和0.001μM）的去氧肾上腺素注入HVT通气大鼠的肺泡腔[5]。

[参考文献]

[1]. Ford AP, et al. Pharmacological pleiotropism of the human recombinant alpha1A-adrenoceptor: implications foralpha1-adrenoceptor classification. Br J Pharmacol. 1997 Jul;121(6):1127-35.

[2]. Minneman KP, et al. Selectivity of agonists for cloned alpha 1-adrenergic receptor subtypes. Mol Pharmacol. 1994 Nov;46(5):929-36.

[3]. Wang J, et al. Phenylephrine promotes cardiac fibroblast proliferation through calcineurin-NFAT pathway. Front Biosci (Landmark Ed). 2016 Jan 1;21:502-13.

[4]. Lazou A, et al. Activation of mitogen-activated protein kinases (p38-MAPKs, SAPKs/JNKs and ERKs) by the G-protein-coupled receptor agonist phenylephrine in the perfused rat heart. Biochem J. 1998 Jun 1;332 ( Pt 2):459-65.

[5]. Li NJ, et al. Effect of phenylephrine on alveolar fluid clearance in ventilator-induced lung injury. Chin Med Sci J. 2013 Mar;28(1):1-6.

[相关活性小分子]

盐酸去氧肾上腺素物理化学性质

[ 沸点 ]:
341.1ºC at 760 mmHg

[ 熔点 ]:
143-145 °C(lit.)

[ 分子式 ]:
C₉H₁₄ClNO₂

[ 分子量 ]:
203.666

[ 闪点 ]:
163.4ºC

[ 精确质量 ]:
203.071304

[ PSA ]:
52.49000

[ LogP ]:
1.83790

[ 外观性状 ]:
白色至近乎于白色结晶粉末

[ 折射率 ]:
-45.5 ° (C=1, H2O)

[ 储存条件 ]:
室温

[ 水溶解性 ]:
>=10 g/100 mL at 21 ºC

盐酸去氧肾上腺素MSDS

盐酸去氧肾上腺素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO7525000

CHEMICAL NAME :: Benzyl alcohol, m-hydroxy-alpha-((methylamino)methyl)-, hydrochloride, (-)-

CAS REGISTRY NUMBER :: 61-76-7

LAST UPDATED :: 199706

DATA ITEMS CITED :: 23

MOLECULAR FORMULA :: C9-H13-N-O2.Cl-H

MOLECULAR WEIGHT :: 203.69

WISWESSER LINE NOTATION :: QR CYQ1M1 &GH -L

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 120 mg/kg

TOXIC EFFECTS :: Brain and Coverings - changes in circulation (hemorrhage, thrombosis, etc.) Behavioral - muscle weakness

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 27 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 440 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 89 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 22 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1120 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - other changes

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 16 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 22 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 500 ug/kg

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

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 7200 ug/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 84 gm/kg/12W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - miosis (pupillary constriction) Cardiac - changes in heart weight Endocrine - changes in adrenal weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 202 gm/kg/12W-I

TOXIC EFFECTS :: Cardiac - changes in heart weight Endocrine - changes in adrenal weight Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 15 mg/kg

SEX/DURATION :: female 22-31 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 1500 mg/L

REFERENCE :: NTPTR* National Toxicology Program Technical Report Series. (Research Triangle Park, NC 27709) No.206- Volume(issue)/page/year: NTP-TR-322,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - M0845 No. of Facilities: 169 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 4376 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - M0845 No. of Facilities: 360 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 14244 (estimated) No. of Female Employees: 10911 (estimated)

盐酸去氧肾上腺素安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36-S37/39

[ 危险品运输编码 ]:
3249

[ WGK德国 ]:
3

[ RTECS号 ]:
DO7525000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2937229000

盐酸去氧肾上腺素合成路线

盐酸去氧肾上腺素上下游产品

盐酸去氧肾上腺素上游产品

盐酸去氧肾上腺素下游产品

盐酸去氧肾上腺素制备

间羟基乙酮经苯甲酰化、溴化、胺化、水解、催化氢化，得到间羟基-α-甲氨基甲基苯甲醇（消旋体），再用d-酒石酸拆分，获得左旋游离碱。将游离碱悬浮于无水乙醇中，加氯化氢-乙醇液至pH=4，加热溶解，加活性炭脱色过滤，滤液中加入无水乙醚，冷冻析出结晶。甩滤，结晶用少量丙酮洗涤，干燥，得苯肾上腺素盐酸盐。

盐酸去氧肾上腺素海关

[ 海关编码 ]: 2922509090

[ 中文概述 ]:
2922509090. 其他氨基醇酚、氨基酸酚及其他含氧基氨基化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件：AB. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

盐酸去氧肾上腺素文献

Receptor mediated disruption of retinal pigment epithelium function in acute glycated-albumin exposure.

Exp. Eye Res. 137 , 50-6, (2015)

Diabetic macular edema (DME) is a major cause of visual impairment. Although DME is generally believed to be a microvascular disease, dysfunction of the retinal pigment epithelium (RPE) can also contr...

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Formulation and stability study of a pediatric 2% phenylephrine hydrochloride eye drop solution.

Ann. Pharm. Fr. 73(1) , 31-6, (2015)

We present formulation and stability evaluation of a 2% (w/v) phenylephrine hydrochloride biocompatible eye drop solution, routinely prepared in hospital pharmacy under aseptic conditions, for retinal...

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