| CAS |
549-18-8 |
| Chinese Name |
盐酸阿米替林 |
| English Name |
Amitriptyline Hydrochloride |
| Synonyms |
Annoyltin;Tryptizol;Domical |
| Molecular Formula |
C20H23N·HCl |
| Molecular Weight |
313.87 |
| Solubility |
Soluble in Water/DMSO |
| Purity |
HPLC≥98% |
| Appearance |
White to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 208-964-6 |
| MDL |
MFCD00012537 |
| SMILES |
CN(C)CC/C=C1C2=CC=CC=C2CCC3=C\1C=CC=C3.Cl |
| InChIKey |
KFYRPLNVJVHZGT-UHFFFAOYSA-N |
| InChI |
InChI=1S/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 |
| PubChem CID |
11065 |
| Target Point |
SERT;NET;DAT;Adrenergic receptor;mAChR;Histamine receptor;5-HT receptor;TrkA |
| Passage |
Neuronal Signaling;Membrane Transporter&Ion Channel;Endocrinology & Hormones;GPCR & G Protein；Immunology & Inflammation |
| Background |
It is a SERT and NET inhibitor. It also binds to DAT and also inhibits Adrenergic receptor, mAChR, Histamine receptor and 5-HT receptor. In addition, it is a TrkA and TrkA receptor agonist with strong neurotrophic activity. |
| Biological Activity |
Amitriptyline HCl 是一种 serotonin transporter (SERT) 和 norepinephrine transporter (NET) 的抑制剂，其Ki值分别为3.45 nM和13.3 nM。Amitriptyline HCl 还可抑制histamine receptor H1、histamine receptor H4、5-HT2 和 sigma 1 receptor，对应的Ki值分别是0.5 nM、7.31 nM、235 nM和287 nM。Amitriptyline 是一种三环抗抑郁药物。[1-8] |
| In Vitro |
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] |
| In Vivo |
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] |
| Data Literature Source |
[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)，2005，1 |
| Unit |
Bottle |
| Specification |
50mg 10mM*1mL in DMSO 500mg |
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