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去氧肾上腺素

去氧肾上腺素用途

(R)-(-)-Phenylephrine是选择性的α1-肾上腺素受体激动剂,主要用作减充血剂。

去氧肾上腺素名称

[ CAS 号 ]:
59-42-7

[ 中文名 ]:
去氧肾上腺素碱

[ 英文名 ]:
(R)-(-)-Phenylephrine

[中文别名 ]:

[英文别名 ]:

Neophryn
Mydfrin
Mesatone
Mesaton
Phenylephrine
Nostril
EINECS 200-424-8
MFCD00044749
Mezaton
Adrianol

去氧肾上腺素生物活性

[ 描述 ]:

(R)-(-)-Phenylephrine是选择性的α1-肾上腺素受体激动剂,主要用作减充血剂。

[ 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 >> 代谢疾病

[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]

去氧肾上腺素物理化学性质

[ 密度 ]:
1.159 g/cm3

[ 沸点 ]:
341.1ºC at 760 mmHg

[ 熔点 ]:
171°C

[ 分子式 ]:
C₉H₁₃NO₂

[ 分子量 ]:
167.20500

[ 闪点 ]:
163.4ºC

[ 精确质量 ]:
167.09500

[ PSA ]:
52.49000

[ LogP ]:
1.03590

[ 折射率 ]:
-55.5 ° (C=5, 1mol/L HCl)

[ 储存条件 ]:
室温

去氧肾上腺素MSDS

去氧肾上腺素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO7175000

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

CAS REGISTRY NUMBER :: 59-42-7

LAST UPDATED :: 199706

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C9-H13-N-O2

MOLECULAR WEIGHT :: 167.23

WISWESSER LINE NOTATION :: QR CYQ1M1 -L

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 188 ug/kg

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section

REFERENCE :: ANESAV Anesthesiology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1940- Volume(issue)/page/year: 36,187,1972

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Ocular

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 5500 ug/kg

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section

REFERENCE :: ANESAV Anesthesiology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1940- Volume(issue)/page/year: 36,187,1972

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 28 mg/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 85,119,1945

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

ROUTE OF EXPOSURE :: Intraduodenal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 65 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 180,155,1969

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 160,22,1968

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 875 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 28,46,1965

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 38 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Cardiac - pulse rate increase, without fall in BP Skin and Appendages - hair

REFERENCE :: APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 38,474,1976 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 20 ug/kg

SEX/DURATION :: female 16 week(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

REFERENCE :: AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 143,170,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 40 ug/kg

SEX/DURATION :: female 16 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow)

REFERENCE :: AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 143,170,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80598 No. of Facilities: 97 (estimated) No. of Industries: 2 No. of Occupations: 3 No. of Employees: 183 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80598 No. of Facilities: 147 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 6641 (estimated) No. of Female Employees: 5606 (estimated)

去氧肾上腺素安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S26-S36-S45

[ RTECS号 ]:
DO7175000

去氧肾上腺素合成路线

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