普罗替林

普罗替林用途

普罗替林是一种有效的抗抑郁剂。普罗替林抑制乙酰胆碱酯酶活性,IC50值为0.06 mM,并抑制Aβ自组装。普罗替林可用于治疗抑郁症和阿尔茨海默病[1][2][3]。
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普罗替林名称

[ CAS 号 ]:
438-60-8

[ 中文名 ]:
普罗替林

[ 英文名 ]:
protriptyline

[英文别名 ]:

普罗替林生物活性

[ 描述 ]:

普罗替林是一种有效的抗抑郁剂。普罗替林抑制乙酰胆碱酯酶活性,IC50值为0.06 mM,并抑制Aβ自组装。普罗替林可用于治疗抑郁症和阿尔茨海默病[1][2][3]。

[ 相关类别 ]:

研究领域 >> 神经疾病
信号通路 >> 神经信号通路 >> 疼痛

[体外研究]

普罗替林(0-70μM；24小时；PC3细胞)对PC3细胞产生细胞毒性[2]。细胞毒性试验[2]细胞系：PC3细胞浓度：50、60和70μM孵育时间：24小时结果：细胞活力呈浓度依赖性下降。

[体内研究]

普罗替林(10 mg/kg；静脉注射；持续21天；AD大鼠模型)改善STZ治疗大鼠的空间学习和保留记忆[3]。动物模型：AD大鼠模型[3]剂量：10mg/kg给药：腹腔注射；21天。结果：pTau、Aβ42和BACE-1水平降低,神经退行性变、氧化应激和胶质细胞活化减少。通过减少NFκB和GFAP的表达,提高p-ERK/ERK比率,增强BDNF和CREB水平。

[参考文献]

[1]. Bansode SB, et, al. Molecular investigations of protriptyline as a multi-target directed ligand in Alzheimer's disease. PLoS One. 2014 Aug 20;9(8):e105196.

[2]. Chang HT, et, al. The mechanism of protriptyline-induced Ca2+ movement and non-Ca2+-triggered cell death in PC3 human prostate cancer cells. J Recept Signal Transduct Res. 2015;35(5):429-34.

[3]. Tiwari V, et, al. Protriptyline improves spatial memory and reduces oxidative damage by regulating NFκB-BDNF/CREB signaling axis in streptozotocin-induced rat model of Alzheimer's disease. Brain Res. 2021 Mar 1;1754:147261.

普罗替林物理化学性质

[ 密度 ]:
1.026 g/cm3

[ 沸点 ]:
407.7ºC at 760 mmHg

[ 分子式 ]:
C19H21N

[ 分子量 ]:
263.37700

[ 闪点 ]:
198.3ºC

[ 精确质量 ]:
263.16700

[ PSA ]:
12.03000

[ LogP ]:
4.69280

[ 储存条件 ]:
室温

普罗替林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
HP1050000
CHEMICAL NAME :
5H-Dibenzo(a,d)cycloheptene-5-propylamine, N-methyl-
CAS REGISTRY NUMBER :
438-60-8
LAST UPDATED :
199612
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C19-H21-N
MOLECULAR WEIGHT :
263.41
WISWESSER LINE NOTATION :
L C676 BHJ B3M1

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 :
240 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
42 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
269 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
67 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
192 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
30 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay)
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 17,65,1974
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
310 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
8200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPPAO Farmaco, Edizione Pratica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 25,519,1970 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
630 mg/kg/6W-I
TOXIC EFFECTS :
Cardiac - EKG changes not diagnostic of specified effects Cardiac - pulse rate increase, without fall in BP
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,1709,1980 *** REVIEWS *** TOXICOLOGY REVIEW IDPYAK Industrial Pharmacology. (Mount Kisco, NY) V.1-3, 1974-79. Discontinued. Volume(issue)/page/year: 2,209,1975
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普罗替林安全信息

[ 海关编码 ]:
2921499090

普罗替林合成路线

详细合成路线

普罗替林上下游产品

普罗替林上游产品

普罗替林下游产品

普罗替林海关

[ 海关编码 ]: 2921499090

[ 中文概述 ]:
2921499090 其他芳香单胺及衍生物及它们的盐. 增值税率:17.0% 退税率:9.0% 监管条件:无 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

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

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