| CAS: | 549-18-8 | |||||||||||||||||||||||
| 分子式: | C20H24ClN | |||||||||||||||||||||||
| 分子量: | 313.86 | |||||||||||||||||||||||
| 中文名称: |
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| 英文名称: |
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| 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。 |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | 详情 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| A0908 | TCI | Amitriptyline Hydrochloride | >98.0%(T)(HPLC) | 750元/25G; | 展开 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
基本信息
技术规格
物性(参考值)
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| 296982 | J&K | Amitriptyline Hydrochloride | 98%, 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
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
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| PHR1384 | Supelco | Amitriptyline Hydrochloride | Pharmaceutical Secondary Standard; Certified Reference Material | 1359.83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. 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
产品性质
安全信息
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| Y0000563 | Amitriptyline Hydrochloride | European Pharmacopoeia (EP) Reference Standard | 1259.15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
产品性质
安全信息
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| A8404 | Sigma-Aldrich | Amitriptyline Hydrochloride | ≥98% (TLC), powder | 552.83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:
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。 特点和优势 粉末的保质期至少为三年。 基本信息
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| 1029002 | USP | Amitriptyline Hydrochloride | United States Pharmacopeia (USP) Reference Standard | 3231.47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. 基本信息
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| BP016 | Amitriptyline Hydrochloride | British Pharmacopoeia (BP) Reference Standard | 1916.08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
产品性质
安全信息
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| 463103 | Fluorochem | Amitriptyline Hydrochloride | 95% | 220元/1g; 242元/5g; 418元/10g; 968元/25g; | 展开 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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