Amitriptyline hydrochloride

产品编号 T0678   CAS 549-18-8
别名: Amitriptyline HCl, Annoyltin, Tryptizol, Domical

Amitriptyline Hydrochloride is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Amitriptyline hydrochloride结构式
Amitriptyline hydrochloride , CAS 549-18-8
规格 库存 价格/RMB 数量
500 mg 上海现货 479.00
1 g 上海现货 575.00
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产品描述 Amitriptyline Hydrochloride is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.
靶点活性 5-HT : ic50 3.45nM,   5-HT2 : ic50 235nM,   5-HT4 : ic50 7.31nM,   Norepinephrine receptor : ic50 13.3nM,   σ1 : ic50 287nM,  
体外活性 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. [5] Amitriptyline binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization. Amitriptyline (< 500 nM) promotes TrkA autophosphorylation in primary neurons and induces neurite outgrowth in PC12 cells. Amitriptyline selectively protects T17 cells from apoptosis with EC50 of 50 nM. [6]
体内活性 Amitriptyline (15 mg/kg, i.p.) activates TrkA and TrkB receptors and significantly reduces kainic acid-triggered neuronal cell death in mice. [6] 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. [7] 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. [8]
别名 Amitriptyline HCl, Annoyltin, Tryptizol, Domical
纯度 99.87%
分子量 313.86
分子式 C20H24ClN
CAS No. 549-18-8

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

DMSO: 59 mg/mL (188 mM)

Ethanol: 59 mg/mL (188 mM)

Water: 12 mg/mL (38.2 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

文献引用

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.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Adrenergic Receptor Compound Library Neuronal Signaling Compound Library Histamine & Melatonin Library Ion Channel Inhibitor Library Serotonin Compound Library FDA-approved Drug Library Cytokine Inhibitor Library GPCR Compound Library Cardiotoxicity Compound Library Anti-Cardiovascular Disease Compound Library Killers Collection

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