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CAS: 549-18-8
分子式: C20H24ClN
分子量: 313.86
中文名称: 
阿米替林盐酸盐
阿密替林
英文名称: 
1-propanamine, 3-(10,11-dihydro-5h-dibenzo[a,d]cyclohepten-5-ylidene)-n,n-dimet
10,11-dihydro-n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-delta(sup 5,gamma)-pro
pylamine hcl
5-(3-dimethylaminopropylidene)dibenzo(a,d)(1,4)cycloheptadiene hydrochloride
amitriptyline chloride
amitriptyline hydrochloride
damilen hydrochloride
deprex
domical
elavil hydrochloride
endep
etrafon
limbitrol ds
miketorin
proheptadien monohydrochloride
rantoron
saroten
sk-amitriptyline
triavil
yamanouchi
amitriptylinehydrochloride
amitriptyline hcl
3-(10,11dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidine)-N,N-dimethyl-1-propanamine hydrochloride
展开更多英文名
性质描述: 本品为白色结晶性粉末。溶点196-197℃,易溶于水、乙醇、甲醇、氯仿,不溶于乙醚。无臭,味苦。
生产方法: 由二苯并[α,d]环庚二烯酮-(5)经加成、消除、成盐而得。将干燥镁片及乙醚投入反应罐,加热回流。先滴加二甲胺基氯丙烷的乙醚溶液,再滴加二苯并环庚二烯酮的乙醚溶液。回流蒸出乙醚,加甲苯,冷却后加饱和氯化铵水溶液。停止搅拌,分出甲苯液,再用甲苯对水层提取5次。合并甲苯液,用温水洗3次,用无水硫酸钠干燥,过滤。滤液回收甲苯后得羟基阿米替林粗品。将粗品用甲苯和活性炭重结晶精制后,搅拌加热下溶解于浓盐酸,回流2-3小时后,减压蒸出稀盐酸至干。加异丙醇及活性炭,升温搅拌回流1小时。趁热过滤,在搅拌下滤液缓缓冷却,结晶,过滤,烘干,得阿米替林盐酸盐。收率约为75%。
用途: 本品为抗抑郁药,具有抗抑郁作用和较强的镇静作用。主要用于内源性外源性抑郁症状、更年期忧郁症、神经性抑郁症及器质性精神病的抑郁症状,也可用于儿童和少年的遗尿症。
推荐供应商
货号品牌产品名称规格包装、参考价格详情
A0908TCIAmitriptyline Hydrochloride>98.0%(T)(HPLC)750元/25G;   展开

基本信息

纯度/分析方法>98.0%(T)(HPLC)
分子式/分子量C20H23N・HCl = 313.87
外观与形状(20℃)固体
应避免的情况
相关CAS RN50-48-6
Reaxys-RN4164595
PubChem物质ID87562417
Merck Index (14)487
MDL编号MFCD00012537

技术规格

AppearanceWhite to Almost white powder to crystal
Purity(HPLC)min. 98.0 area%
Purity(Nonaqueous Titration)min. 98.0 %
Melting point195.0 to 199.0 ℃
Solubility in Wateralmost transparency

物性(参考值)

熔点195 ℃
水溶性可溶

安全信息

图形或危害标志
信号词危险
危险性说明H301 : 吞咽会中毒。
H315 : 造成皮肤刺激。
H319 : 造成严重眼刺激。
防范说明P501 : 将内装物/容器送到批准的废物处理厂处理。
P270 : 使用本产品时不要进食、饮水或吸烟。
P264 : 作业后彻底清洗皮肤。
P280 : 戴防护手套/戴防护眼罩/戴防护面具。
P302 + P352 : 如皮肤沾染:用水充分清洗。
P337 + P313 : 如仍觉眼刺激:求医/就诊。
P305 + P351 + P338 : 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。
P362+P364 : 脱掉沾污的衣服,清洗后方可重新使用。
P332 + P313 : 如发生皮肤刺激:求医/就诊。
P301 + P310 + P330 : 如误吞咽:立即呼叫急救中心/医生。漱口。
P405 : 存放处须加锁。

相关法规

RTECS#HO9450000

运输信息

UN编号UN2811
类别6.1
包装类别 III
监管条件代码(*)
296982J&KAmitriptyline Hydrochloride98%, 一种二苯并环庚烯衍生物, 三环抗抑郁剂(TCA)898元/25G;   展开

基本信息

分子式C20H23N·HCl
分子量313.86
熔点195-199
MDL编码MFCD00012537
Beilstein4164595
Merck14,487
EINECS 编号208-964-6
存储条件Store at 2-8℃

产品描述

Amitriptyline HCl 是一种三环抗抑郁药,抑制5-羟色胺受体,去甲肾上腺素受体, 5-HT4, 5-HT2和sigma 1受体, IC50分别为3.45 nM, 13.3 nM, 7.31 nM, 235 nM和287 nM。

靶点(IC50 & Targe)

5-HT,3.45nM

5-HT2,235nM

5-HT4,7.31nM

Norepinephrine receptor,13.3nM

σ1,287nM

体外研究

Amitriptyline抑制毛喉素刺激的环AMP聚集,在完整CHO/DOR细胞中EC50值为16.2 μM。Amitriptyline浓度依赖性刺激ERK1/2和GSK-3β磷酸化作用,CHO/DOR细胞中EC50值为9.0 μM。Amitriptyline (15 μM)刺激C6细胞中ERK1/2磷酸化。Amitriptyline (30 μM)抑制毛喉素刺激的腺苷酸环化酶活性,并拮抗大鼠伏核中(−)-U50,488的抑制作用。[5] Amitriptyline结合到TrkA和TrkB的胞外结构域,并促进TrkA-TrkB受体异源二聚化。Amitriptyline (< 500 nM)促进初级神经元中TrkA自身磷酸化,并诱导PC12细胞中神经突增生。Amitriptyline选择性保护T17细胞免于细胞凋亡,EC50为50 nM。[6]

体内研究

在小鼠中,Amitriptyline (15 mg/kg, i.p.)激活TrkA和TrkB受体,并显著减少红藻氨酸引起的神经元细胞死亡。[6] Amitriptyline (15 mg/kg 和30 mg/kg, i.p.)剂量依赖性减少小鼠强迫性游泳测试(FST)中的不动时间。小鼠强迫性游泳测试(FST)中,Amitriptyline (15 mg/kg, i.p.)使小鼠不动时间现出显著的24-h节律性。[7] Amitriptyline (1 mg/kg和3 mg/kg)显著增加小鼠在新笼子实验中总的行走距离。Amitriptyline (10 mg/kg p.o.,每天两次)大大减弱小鼠体内对8-OHDPAT和mCPP的低体温响应。Amitriptyline (10 mg/kg p.o.,每天两次)显著降低小鼠大脑皮层中大约20%的血清素转运体密度。[8]

参考文献

[1] Vaishnavi SN, et al. Biol Psychiatry, 2004, 55(3), 320-322.

[2] Nguyen T, et al. Mol Pharmacol, 2001, 59(3), 427-433.

[3] Rauser L, et al. J Pharmacol Exp Ther, 2001, 299(1), 83-89.

[4] Werling LL, et al. Exp Neurol, 2007, 207(2), 248-257.

[5] Onali P, et al. J Pharmacol Exp Ther, 2010, 332(1), 255-265.

[6] Jang SW, et al. Chem Biol, 2009, 16(6), 644-656.

[7] Ushijima K, et al. J Pharmacol Exp Ther, 2005, 315(2), 764-770.

[8] Troelsen KB, et al. Psychopharmacology (Berl), 2005, 181(4

安全信息

图形或危害标志
提示语Danger
危险说明H301
H319
H410
防范说明P273
P301+P310
P305+P351+P338
P501
UN号码2811
危险分类6.1
包装等级III
WGK3
RTECSHO9450000
PHR1384SupelcoAmitriptyline HydrochloridePharmaceutical Secondary Standard; Certified Reference Material1359.83元/1 G;   展开

产品说明

一般描述

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards. Amitriptyline hydrochloride is a drug, and a tricyclic antidepressant with anticholinergic activity. It is widely used in combination with chlordiazepoxide 7-chloro-2-(methyl-amino)-5-phenyl-3H-1,4-benzodiazepine-4-oxide for the treatment of patients with moderate to severe depression associated with moderate to severe anxiety.

应用

These Secondary Standards are qualified as Certified Reference Materials. These are suitable for use in several analytical applications including but not limited to pharma release testing, pharma method development for qualitative and quantitative analyses, food and beverage quality control testing, and other calibration requirements.
Amitriptyline hydrochloride may be used as a pharmaceutical reference standard for the quantification of the analyte in pharmaceutical formulations using spectrophotometric technique and reversed-phase high-performance liquid chromatography.

生化/生理作用

三环抗抑郁剂;抑制分别具有 100nM 和 14.7nM Kis 的去甲肾上腺素和 5-羟色胺转运蛋白;对 α1-肾上腺素受体、5-羟色胺和毒蕈碱型乙酰胆碱受体具有高度的体外亲和力。

分析说明

These secondary standards offer multi-traceability to the USP, EP (PhEur) and BP primary standards, where they are available.

其他说明

This Certified Reference Material (CRM) is produced and certified in accordance with ISO 17034 and ISO/IEC 17025. All information regarding the use of this CRM can be found on the certificate of analysis.

附注

To see an example of a Certificate of Analysis for this material enter LRAA1640 in the slot below. This is an example certificate only and may not be the lot that you receive.

基本信息

经验(实验)分子式C20H23N · HCl
分子量313.86
EC 号208-964-6
MDL编号MFCD00012537
PubChem化学物质编号329823361
NACRESNA.24

产品性质

质量水平300
等级certified reference material
pharmaceutical secondary standard
CofAcurrent certificate can be downloaded
technique(s)HPLC: suitable
gas chromatography (GC): suitable
application(s)pharmaceutical (small molecule)
格式neat
药典可追溯性traceable to BP 16
traceable to PhEur Y0000563
traceable to USP 1029002
储存温度2-30℃
SMILES stringCl[H].CN(C)CC\C=C1\c2ccccc2CCc3ccccc13
InChI1S/C20H23N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-12H,7,13-15H2,1-2H3;1H
InChI keyKFYRPLNVJVHZGT-UHFFFAOYSA-N
Gene Informationhuman ... SLC6A2(6530), SLC6A4(6532)

安全信息

象形图GHS06GHS08GHS09
警示用语:Danger
危险声明H301 - H319 - H361d - H410
预防措施声明P201 - P273 - P301 + P310 + P330 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Repr. 2
储存分类代码6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
Y0000563Amitriptyline HydrochlorideEuropean Pharmacopoeia (EP) Reference Standard1259.15元/ ;   展开

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

三环抗抑郁剂;抑制分别具有 100nM 和 14.7nM Kis 的去甲肾上腺素和 5-羟色胺转运蛋白;对 α1-肾上腺素受体、5-羟色胺和毒蕈碱型乙酰胆碱受体具有高度的体外亲和力。

包装

Unit quantity: 10 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式C20H23N · HCl
分子量313.86
MDL编号MFCD00012537
PubChem化学物质编号329831024
NACRESNA.24

产品性质

等级pharmaceutical primary standard
manufacturer/tradenameEDQM
application(s)pharmaceutical (small molecule)
格式neat
储存温度2-8℃
SMILES stringCl[H].CN(C)CC\C=C1\c2ccccc2CCc3ccccc13
InChI1S/C20H23N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-12H,7,13-15H2,1-2H3;1H
InChI keyKFYRPLNVJVHZGT-UHFFFAOYSA-N
Gene Informationhuman ... SLC6A2(6530), SLC6A4(6532)

安全信息

象形图GHS06GHS08GHS09
警示用语:Danger
危险声明H301 - H319 - H361d - H410
预防措施声明P201 - P273 - P301 + P310 + P330 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Repr. 2
储存分类代码6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
A8404Sigma-AldrichAmitriptyline Hydrochloride≥98% (TLC), powder552.83元/10 G;   1215.53元/25 G;   3340.11元/100 G;   5883.36元/250 G;   展开

产品说明

应用

盐酸阿密曲替林已用于:

  • 研究其作为抗抑郁药对酸性鞘磷脂酶转基因(t-ASM)小鼠社会行为和记忆的影响
  • 分析其作为三环类抗抑郁药物对人全血中糖皮质受体功能的影响
  • 研究其作为抗抑郁药对氯喹诱导小鼠搔抓和运动行为的影响

生化/生理作用

三环抗抑郁剂;抑制分别具有 100nM 和 14.7nM Kis 的去甲肾上腺素和 5-羟色胺转运蛋白;对 α1-肾上腺素受体、5-羟色胺和毒蕈碱型乙酰胆碱受体具有高度的体外亲和力。
盐酸阿密曲替林(Amitriptyline)可用于治疗焦虑、躁郁和更年期抑郁症。它具有抗组胺、抗胆碱和抗血清素特性。盐酸阿密曲替林是两亲性药物,具有神经抑制活性。

特点和优势

粉末的保质期至少为三年。

基本信息

经验(实验)分子式C20H23N · HCl
分子量313.86
EC 号208-964-6
MDL编号MFCD00012537
PubChem化学物质编号24278073
NACRESNA.77

产品性质

质量水平200
测定≥98% (TLC)
形式powder
颜色 white to off-white
溶解性H2O: soluble
ethanol: soluble
创始人Bristol-Myers Squibb
储存温度2-8℃
SMILES stringCl[H].CN(C)CC\C=C1\c2ccccc2CCc3ccccc13
InChI1S/C20H23N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-12H,7,13-15H2,1-2H3;1H
InChI keyKFYRPLNVJVHZGT-UHFFFAOYSA-N
Gene Informationhuman ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133), SLC6A2(6530), SLC6A4(6532)

安全信息

象形图GHS06GHS08GHS09
警示用语:Danger
危险声明H301 - H319 - H361d - H410
预防措施声明P201 - P273 - P301 + P310 + P330 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Repr. 2
储存分类代码6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
个人防护装备Eyeshields, Faceshields, Gloves, type P1 (EN143) respirator filter, type P3 (EN 143) respirator cartridges
1029002USPAmitriptyline HydrochlorideUnited States Pharmacopeia (USP) Reference Standard3231.47元/200 MG;   展开

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

三环抗抑郁剂;抑制分别具有 100nM 和 14.7nM Kis 的去甲肾上腺素和 5-羟色胺转运蛋白;对 α1-肾上腺素受体、5-羟色胺和毒蕈碱型乙酰胆碱受体具有高度的体外亲和力。

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

USP issued SDS can be found here.
Sales restrictions may apply.

基本信息

经验(实验)分子式C20H23N · HCl
分子量313.86
MDL编号MFCD00012537
PubChem化学物质编号329749005
NACRESNA.24

产品性质

等级pharmaceutical primary standard
manufacturer/tradenameUSP
application(s)pharmaceutical (small molecule)
格式neat
SMILES stringCl[H].CN(C)CC\C=C1\c2ccccc2CCc3ccccc13
InChI1S/C20H23N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-12H,7,13-15H2,1-2H3;1H
InChI keyKFYRPLNVJVHZGT-UHFFFAOYSA-N
Gene Informationhuman ... SLC6A2(6530), SLC6A4(6532)

安全信息

象形图GHS06GHS08GHS09
警示用语:Danger
危险声明H301 - H319 - H361d - H410
预防措施声明P201 - P273 - P301 + P310 + P330 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2 - Repr. 2
储存分类代码6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
BP016Amitriptyline HydrochlorideBritish Pharmacopoeia (BP) Reference Standard1916.08元/150 MG;   展开

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia. For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

三环抗抑郁剂;抑制分别具有 100nM 和 14.7nM Kis 的去甲肾上腺素和 5-羟色胺转运蛋白;对 α1-肾上腺素受体、5-羟色胺和毒蕈碱型乙酰胆碱受体具有高度的体外亲和力。

包装

Unit quantity: 150 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity please visit British Pharmacopoeia

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式C20H23N · HCl
分子量313.86
MDL编号MFCD00012537
NACRESNA.24

产品性质

等级pharmaceutical primary standard
manufacturer/tradenameBP
格式neat
储存温度2-8℃
SMILES stringCl[H].CN(C)CC\C=C1\c2ccccc2CCc3ccccc13
InChI1S/C20H23N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-12H,7,13-15H2,1-2H3;1H
InChI keyKFYRPLNVJVHZGT-UHFFFAOYSA-N
Gene Informationhuman ... SLC6A2(6530), SLC6A4(6532)

安全信息

象形图GHS06GHS09
警示用语:Danger
危险声明H301 - H319 - H410
预防措施声明P301 + P330 + P331 + P310 - P305 + P351 + P338
危险分类Acute Tox. 3 Oral - Aquatic Acute 1 - Aquatic Chronic 1 - Eye Irrit. 2
储存分类代码6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable
463103FluorochemAmitriptyline Hydrochloride95%220元/1g;   242元/5g;   418元/10g;   968元/25g;   展开

基本信息

CAS Number549-18-8
MDL NumberMFCD00012537
Melting Point195℃

安全信息

图形或危害标志
危险性说明 H301: Toxic if swallowed.
H315: Causes skin irritation.
H319: Causes serious eye irritation.
H335: May cause respiratory irritation.
防范说明 P233: Keep container tightly closed.
P260: Do not breathe .
P261: Avoid breathing
P264: Wash hands thoroughly after handling.
P270: Do not eat, drink or smoke when using this product.
P271: Use only outdoors or in a well-ventilated area.
P280: Wear .
P301 + P310: IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P302 + P352: IF ON SKIN: Wash with plenty of soap and water.
P304: IF INHALED: .
P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P312: Call a POISON CENTER or doctor/physician if you feel unwell.
P321: Specific treatment (see . on this label).
P330: Rinse mouth.
P332 + P313: If skin irritation occurs: Get medical advice/ attention.
P337 + P313: If eye irritation persists: Get medical advice/attention.
P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P362: Take off contaminated clothing and wash before reuse.
P403: Store in a well-ventilated place.
P403 + P233: Store in a well-ventilated place. Keep container tightly closed.
P405: Store locked up.
P501: Dispose of contents/container to local regulations.
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