Amitriptyline HCl

Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).

CAS No. 549-18-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 23500	国内在庫あり
50mg	JPY 18100	国内在庫あり
1g	JPY 101400	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（3）

製品安全説明書

現在のバッチを見る： S318301 DMSO] 63 mg/mL] false] Ethanol] 63 mg/mL] false] Water] 15 mg/mL] false 純度： 99.88%

99.88

Amitriptyline HCl 関連製品

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Serotonin Transporter阻害剤の選択性比較

生物活性

製品説明

Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).

Targets

Histamine Receptor H1 ^[9]	SERT ^[1]	Histamine receptor H4 ^[2]	NET ^[1]	5-HT2 ^[3]	もっとクリックする
0.5 nM(Ki)	3.45 nM(Ki)	7.31 nM(Ki)	13.3 nM(Ki)	235 nM(Ki)	もっとクリックする

In Vitro
In vitro	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]

In Vivo
In Vivo	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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02519400	Unknown status	Depression	Asan Medical Center	August 2015	Phase 1
NCT02101892	Completed	Migraine\|Preventive Treatment	Rambam Health Care Campus\|Migraine Research Foundation	April 2014	Not Applicable
NCT00516503	Completed	Chronic Myeloproliferative Disorders\|Leukemia\|Lymphoma\|Lymphoproliferative Disorder\|Multiple Myeloma and Plasma Cell Neoplasm\|Myelodysplastic Syndromes\|Myelodysplastic/Myeloproliferative Neoplasms\|Neurotoxicity\|Pain\|Unspecified Adult Solid Tumor Protocol Specific	Alliance for Clinical Trials in Oncology\|National Cancer Institute (NCI)	February 2008	Phase 3
NCT00471445	Completed	Neurotoxicity\|Pain\|Peripheral Neuropathy\|Unspecified Adult Solid Tumor Protocol Specific	Gary Morrow\|National Cancer Institute (NCI)\|University of Rochester	October 2007	Phase 3

参考
[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), 741-750. [9] Ola M Ghoneim, et al. Bioorg Med Chem . 2006 Oct 1;14(19):6640-58. + 展開

参考

+ 展開

化学情報

分子量	313.86	化学式	C₂₀H₂₃N.HCl
CAS No.	549-18-8	SDF	Download Amitriptyline HCl SDFをダウンロードする
Smiles	CN(C)CCC=C1C2=CC=CC=C2CCC3=CC=CC=C31.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 63 mg/mL ( (200.72 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 63 mg/mL

Water : 15 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):