盐酸苯氧丙酚胺

盐酸苯氧丙酚胺用途

Isoxsuprine hydrochloride 是 β 肾上腺素受体激动剂,对于子宫肌层和胎盘的 β 肾上腺素受体的 Ki 值分别为 13.65 μM 和 3.48 μM。Isoxsuprine hydrochloride 也是一种 NMDA 受体拮抗剂。

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盐酸苯氧丙酚胺名称

[ CAS 号 ]:
579-56-6

[ 中文名 ]:
异舒普林盐酸盐

[ 英文名 ]:
Isoxsuprine hydrochloride

[中文别名 ]:

异舒普林盐酸盐

[英文别名 ]:

Dilavase
suprilent
vasoplex
Vadosilan
Vasotran
Divadilan
EINECS 209-443-6
Isoxsuprin-hydrochlorid
vasodilan
isoxsuprine*HCl

盐酸苯氧丙酚胺生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 内分泌

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 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[ 靶点 ]

Ki: 13.65 μΜ (myometrial beta-adrenergic receptor), 3.48 μΜ (placcntal beta-adrenergic receptor)[1] NMDA receptor[3]

[体外研究]

结果表明,盐酸异苏平对环状化学排斥诱导缺陷(CCID)的形成具有剂量依赖性抑制作用(5～60μM),对12(S)-HETE的合成也有抑制作用。此外,盐酸异苏平是唯一一种抑制所有三种迁移标记物(MLC2、MYPT和paxillin)诱导的药物[2]。

[体内研究]

经载体治疗的动物的总梗死体积为279±25 mm3,而经盐酸异苏平治疗的动物的总梗死体积为137±18 mm3[3]。

[细胞实验]

将MCF-7ALOX12细胞接种于3.5厘米的培养皿中，在2.5 mL无选择压力的完全MEM培养基中培养。第二天，将培养基换成无血清培养基，细胞在37℃下保持24小时，然后用10μM花生四烯酸处理细胞，同时用不同浓度的盐酸异苏平处理细胞4小时，当上清液被吸出，在2000年离心，在4℃下r.p.M.离心5分钟，收集在冷冻管中，闪蒸冷冻并在-80°C下保存，直到分析[2]。

[动物实验]

本研究选用体重290～300g的雄性自发性高血压大鼠（SHR）。再灌注时，动物通过尾侧静脉静脉注射0.5ml载体（生理盐水中含0.6%二甲基亚砜）或1 mg/kg盐酸异苏平。所有动物在手术后接受3毫升的皮下盐水以防止脱水。再灌注24小时后处死动物，将脑组织切成4 mm厚的四分体，用2,3,5-三苯基四唑（TTC）染色鉴定梗死组织。水肿校正的梗死体积是通过从对侧半球的总体积中减去同侧半球的非梗死组织面积来计算的。梗死体积使用图像J软件进行量化[3]。

[参考文献]

[1]. Falkay G, et al. Affinity of tocolytic agents on human placental and myometrial beta-adrenergic receptors. J Perinat Med. 1986;14(2):109-13.

[2]. Kretschy N, et al. In vitro inhibition of breast cancer spheroid-induced lymphendothelial defects resembling intravasation into the lymphatic vasculature by acetohexamide, isoxsuprine, nifedipin and proadifen. Br J Cancer. 2013 Feb 19;108(3):570-8.

[3]. Hill JW, et al. Identification of isoxsuprine hydrochloride as a neuroprotectant in ischemic stroke through cell-based high-throughput screening. PLoS One. 2014 May 7;9(5):e96761.

盐酸苯氧丙酚胺物理化学性质

[ 密度 ]:
1.146g/cm3

[ 沸点 ]:
484.2ºC at 760mmHg

[ 熔点 ]:
203-204°

[ 分子式 ]:
C₁₈H₂₄ClNO₃

[ 分子量 ]:
337.84100

[ 闪点 ]:
246.6ºC

[ 精确质量 ]:
337.14400

[ PSA ]:
61.72000

[ LogP ]:
4.06410

[ 储存条件 ]:
2-8°C

盐酸苯氧丙酚胺MSDS

详细MSDS(安全技术说明书)

盐酸苯氧丙酚胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DO8225000

CHEMICAL NAME :: Benzyl alcohol, p-hydroxy-alpha-(1-((1-methyl-2-phenoxyethyl)amino)et hyl)-, hydrochloride

CAS REGISTRY NUMBER :: 579-56-6

LAST UPDATED :: 199601

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C18-H23-N-O3.Cl-H

MOLECULAR WEIGHT :: 337.88

WISWESSER LINE NOTATION :: QR DYQY1&MY1&1OR &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1750 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 164 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1100 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 185 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 61 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >1200 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 143 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 57 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Cardiac - change in rate Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 1,579,1959 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9300 mg/kg/31D-I

TOXIC EFFECTS :: Cardiac - other changes Cardiac - changes in heart weight Gastrointestinal - changes in structure or function of salivary glands

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: 19,1334,1985 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 4400 ug/kg/3H

SEX/DURATION :: female 21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - hepatobiliary system Reproductive - Specific Developmental Abnormalities - endocrine system

REFERENCE :: JPEMAO Journal of Perinatal Medicine. (Walter de Gruyter, Inc., 200 Saw Mill River Rd., Hawthorne, NY 10532) V.1- 1973- Volume(issue)/page/year: 9,293,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5237 No. of Facilities: 74 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 2349 (estimated) No. of Female Employees: 1218 (estimated)

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盐酸苯氧丙酚胺安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H410

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
UN 3077 9 / PGIII

[ WGK德国 ]:
3

[ RTECS号 ]:
DO8225000