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帕罗西汀

帕罗西汀用途

帕罗西汀是一种苯基哌啶衍生物,是一种有效的选择性血清素再摄取抑制剂(SSRI)。帕罗西汀是一种非常弱的去甲肾上腺素(NE)摄取抑制剂,但在这个部位,它仍然比其他SSRIs更有效[1]。

帕罗西汀名称

[ CAS 号 ]:
61869-08-7

[ 中文名 ]:
帕罗西汀

[ 英文名 ]:
Paroxetine

[中文别名 ]:

帕罗昔丁

[英文别名 ]:

Paroxetine
BRL 29060A
PAROXETIN HCL
aropax
PAROXETIENE BASE
(-)-Paroxetine
FG 7051
MFCD00869588
Paroxetine (USP)
AROPAX 20

帕罗西汀生物活性

[ 描述 ]:

[ 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 >> 神经疾病

信号通路 >> 神经信号通路 >> 5-羟色胺转运蛋白

[参考文献]

[1]. M Bourin, et al. Paroxetine: a review. CNS Drug Rev. Spring 2001;7(1):25-47

帕罗西汀物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
451.7±45.0 °C at 760 mmHg

[ 熔点 ]:
114-116°C

[ 分子式 ]:
C₁₉H₂₀FNO₃

[ 分子量 ]:
329.365

[ 闪点 ]:
227.0±28.7 °C

[ 精确质量 ]:
329.142731

[ PSA ]:
39.72000

[ LogP ]:
3.89

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.561

[ 储存条件 ]:
2-8℃，避光，惰性气体

帕罗西汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM4569200

CHEMICAL NAME :: Piperidine, 3-((1,3-benzodioxol-5-yloxy)methyl)-4-(4-fluorophenyl )-, trans-(-)-

CAS REGISTRY NUMBER :: 61869-08-7

LAST UPDATED :: 199801

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C19-H20-F-N-O3

MOLECULAR WEIGHT :: 329.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 400 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - paresthesis

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 58,175,1997

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1400 ug/kg/7W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - other changes

REFERENCE :: AJPSAO American Journal of Psychiatry. (American Psychiatric Assoc., Circulation Dept., 1400 K St., NW, Washington, DC 20005) V.78- 1921- Volume(issue)/page/year: 153,134,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4200 ug/kg/3W-I

TOXIC EFFECTS :: Endocrine - hyperglycemia

REFERENCE :: AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 125,782,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 6700 ug/kg

TOXIC EFFECTS :: Behavioral - excitement

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 11,682,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2800 ug/kg/7D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - changes in sodium

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 163,390,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 946 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,37,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 286 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

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

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,37,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3150 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,37,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 700 mg/kg

SEX/DURATION :: female 2 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: ASSUA6 Acta Psychiatrica Scandinavica, Supplementum. (Munksgaard International Publishers, POB 2148, DK-1016 Copenhagen K, Denmark) No.160- 1961- Volume(issue)/page/year: 350,37,1989

帕罗西汀安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
3249

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2934999090

帕罗西汀合成路线

详细合成路线

帕罗西汀上下游产品

帕罗西汀上游产品

帕罗西汀下游产品

帕罗西汀制备

方法1：化合物(I)和化合物(Ⅱ)在二环己基碳化二亚胺(DCC)存在下，缩合得到帕罗西汀。
方法2：化合物(I)转化为甲磺酸酯后，再和化合物(Ⅱ)的钠盐反应，得到帕罗西汀。
方法3：化合物(Ⅲ)或其它N-烷基取代的化合物溶于甲苯，在5℃，于15min中，加入氯甲酸(1-氯乙基)酯。加毕，搅拌18h。加入甲醇，再搅拌12h。移出溶剂，剩余物溶入热异丙醇，用活性炭和氧化铝处理，过滤。往滤液中加入水，再过滤收集析出的沉淀，即得盐酸帕罗西汀半水合物，收率92%。

帕罗西汀海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%