Amitriptyline hydrochloride

Amitriptyline hydrochlorideCAS号: 549-18-8分子式: C20H24ClN分子量: 313.86描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述
Amitriptyline Hydrochloride is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.
纯度
99%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
盐酸阿米替林
外观
白色结晶性粉末
可溶性/溶解性
DMSO : 59 mg/mL (188 mM)

Ethanol : 59 mg/mL (188 mM)

Water : 12 mg/mL (38.2 mM)

生物活性
靶点
Serotonin receptor,5-HT4,Norepinephrine receptor,5-HT2,Sigma 1 receptor
In vitro(体外研究)
Amitriptyline inhibits Forskolin-stimulated cyclic AMP accumulation with EC50 values of 16.2 μM in intact CHO/DOR cells. Amitriptyline causes a concentration-dependent stimulation of ERK1/2 and GSK-3β phosphorylation with EC50 values of 9.0 μM in CHO/DOR cells. Amitriptyline (15 μM) causes a stimulation of ERK1/2 phosphorylation in C6 cells. Amitriptyline (30 μM) inhibits Forskolin-stimulated adenylyl cyclase activity and antagonizes (−)-U50,488 inhibitory effect in rat nucleus accumbens. Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization. Amitriptyline (
In vivo(体内研究)
Amitriptyline (15 mg/kg, i.p.) activates TrkA and TrkB receptors and significantly reduces kainic acid-triggered neuronal cell death in mice. Amitriptyline (15 mg/kg and 30 mg/kg, i.p.) dose-dependently decreases the immobility time in the forced swimming test (FST) of mice. Amitriptyline (15 mg/kg, i.p.) shows a significant 24-h rhythm in the immobility time in the forced swimming test (FST) of mice. Amitriptyline (1 mg/kg and 3 mg/kg) significantly increases the total distance travelled of mice in novel cages. Amitriptyline (10 mg/kg p.o., twice daily) considerably attenuates the hypothermic response to 8-OHDPAT and mCPP in mice. Amitriptyline (10 mg/kg p.o., twice daily) significantly reduces serotonin transporter density by approximately 20% in cortex of mice.
参考文献
参考文献
  • 1. Vaishnavi SN, et al. Biol Psychiatry. 2004 Feb 1;55(3):320-2.
  • 2. Gould GG, et al. Biol Psychiatry. 2006 Mar 1;59(5):408-14.
  • 3. Cusack B, et al. 1994 May;114(4):559-65.
  • 4. Onali P, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):255-65.
  • 5. Jang SW, et al. Chem Biol. 2009 Jun 26;16(6):644-56.
  • 分子结构图

    Amitriptyline hydrochloride