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特布他林

特布他林用途

特布他林是β2-肾上腺素能受体(β2-AR)的短效激动剂。特布他林是班布特罗的活性代谢物,用作支气管扩张剂和预防早产[1][2]。

特布他林名称

[ CAS 号 ]:
23031-25-6

[ 中文名 ]:
特布他林

[ 英文名 ]:
KWD 2019

[中文别名 ]:

[英文别名 ]:

TelMisartan API
SNGP-003-04H08
MICARDIS
[3H]-Telmisartan
BIBR 277
BIBR 277SE
TIMISHATAN
Telmisaran
PRITOR
[3H]-Terbutaline

特布他林生物活性

[ 描述 ]:

特布他林是β2-肾上腺素能受体(β2-AR)的短效激动剂。特布他林是班布特罗的活性代谢物,用作支气管扩张剂和预防早产[1][2]。

[ 相关类别 ]:

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

[ 靶点 ]

Beta-2 adrenergic receptor

[参考文献]

[1]. Hoffmann C, et al. Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9.

[2]. Gaudet LM, et al. Effectiveness of terbutaline pump for the prevention of preterm birth. A systematic review and meta-analysis. PLoS One. 2012;7(2):e31679.

特布他林物理化学性质

[ 密度 ]:
1.171 g/cm3

[ 沸点 ]:
419.2ºC at 760 mmHg

[ 熔点 ]:
204-208ºC

[ 分子式 ]:
C₁₂H₁₉NO₃

[ 分子量 ]:
225.28400

[ 闪点 ]:
165.3ºC

[ 精确质量 ]:
225.13600

[ PSA ]:
72.72000

[ LogP ]:
1.91020

[ 蒸汽压 ]:
3.42E-07mmHg at 25°C

[ 折射率 ]:
1.4596 (estimate)

特布他林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DN8960000

CHEMICAL NAME :: Benzyl alcohol, alpha-((t-butylamino)methyl)-3,5-dihydroxy-

CAS REGISTRY NUMBER :: 23031-25-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C12-H19-N-O3

MOLECULAR WEIGHT :: 225.32

WISWESSER LINE NOTATION :: QR CQ EYQ1MX1&1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Multiple routes

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 380 ug/kg

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 244,692,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 714 ug/kg

TOXIC EFFECTS :: Behavioral - tremor Cardiac - arrhythmias (including changes in conduction) Cardiac - change in rate

REFERENCE :: NEJMAG New England Journal of Medicine. (Massachusetts Medical Soc., 10 Shattuck St., Boston, MA 02115) V.198- 1928- Volume(issue)/page/year: 300,143,1979 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Multiple routes

DOSE :: 5660 ug/kg

SEX/DURATION :: female 32-34 week(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - Apgar score (human only) Reproductive - Effects on Newborn - biochemical and metabolic

REFERENCE :: JOPDAB Journal of Pediatrics. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63141) V.1- 1932- Volume(issue)/page/year: 94,449,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 6 mg/kg

SEX/DURATION :: female 17-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - respiratory system Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

REFERENCE :: PEREBL Pediatric Research. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1967- Volume(issue)/page/year: 25,617,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 30 mg/kg

SEX/DURATION :: female 17-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - Central Nervous System

REFERENCE :: BRBUDU Brain Research Bulletin. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1976- Volume(issue)/page/year: 23,263,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 30 mg/kg

SEX/DURATION :: female 17-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - endocrine system

REFERENCE :: RCOCB8 Research Communications in Chemical Pathology and Pharmacology. (PJD Pub. Ltd., P.O. Box 966, Westbury, NY 11590) V.1- 1970- Volume(issue)/page/year: 76,269,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 62500 ng/kg

SEX/DURATION :: female 16-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects

REFERENCE :: BMMBES Biochemical Medicine and Metabolic Biology. (Academic Press, Inc., Journal Customer Service, POB 6250, Duluth, MN 55802-0250) V.35- 1986- Volume(issue)/page/year: 52,128,1994 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4191 No. of Facilities: 58 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1405 (estimated) No. of Female Employees: 941 (estimated)

特布他林安全信息

[ 危险品运输编码 ]:
UN 3077 9

[ 海关编码 ]:
2942000000

特布他林制备

3,5-二羟基苯甲酸和乙醇在硫酸催化下，回流反应，得到3,5-二羟基苯甲酸乙酯。在碳酸钾存在下3,5-二羟基苯甲酸乙酯和苄基氯，回流20h，用5mlo/L的盐酸或氢氧化钾水解为游离酸，和氯化亚砜一起回流1h，氯化为酰氯，和偶氮甲烷反应使成偶氮乙酰基，和溴化氢作用成为溴乙酰基，接着和叔丁胺回流20h。最后在乙酸存在下催化氢化得到特布他林。

特布他林海关

[ 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%