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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monoamine Transporter-Amitriptyline
Amitriptyline

Chemical Structure : Amitriptyline

CAS No.: 50-48-6

Amitriptyline

货号: PC-28021Not For Human Use, Lab Use Only.

Amitriptyline is a tricyclic antidepressant by blocking SERT (Ki=3.45 nM) and NET (Ki=13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft, is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Amitriptyline is a tricyclic antidepressant by blocking SERT (Ki=3.45 nM) and NET (Ki=13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft, is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities.
Amitriptyline binds to DAT (with Ki = 2.58 μM).
Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki=11-24 nM), H1 receptors (Ki=0.5-1.1 nM), adrenergic α1 receptors (Ki=4.4 nM).
Amitriptyline blocks sodium channels and hERG potassium channel (IC50=4.78 μM) and has cardiotoxicity

物理化学性质&存储条件

分子量 277.41
分子式 C20H23N
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(10,11-Dihydro-5H-dibenzo[a,d][7]annulen-5-ylidene)-N,N-dimethyl-1-propanamine

参考文献

1. Kim Lawson. Biomedicines. 2017 Jun; 5(2): 24.

2. Jang, S.W., et al. Chem Biol, 2009. 16(6): p. 644-56.

3. S Neil Vaishnavi, et al. Biol Psychiatry. 2004 Feb 1;55(3):320-2.

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