For research use only.
Molecular Weight(MW): 313.86
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).
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||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).|
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 (< 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. 
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. 
-  Vaishnavi SN, et al. Biol Psychiatry, 2004, 55(3), 320-322.
-  Nguyen T, et al. Mol Pharmacol, 2001, 59(3), 427-433.
-  Rauser L, et al. J Pharmacol Exp Ther, 2001, 299(1), 83-89.
-  Werling LL, et al. Exp Neurol, 2007, 207(2), 248-257.
-  Onali P, et al. J Pharmacol Exp Ther, 2010, 332(1), 255-265.
-  Jang SW, et al. Chem Biol, 2009, 16(6), 644-656.
-  Ushijima K, et al. J Pharmacol Exp Ther, 2005, 315(2), 764-770.
-  Troelsen KB, et al. Psychopharmacology (Berl), 2005, 181(4), 741-750.
-  Ola M Ghoneim, et al. Bioorg Med Chem . 2006 Oct 1;14(19):6640-58.
|In vitro||DMSO||63 mg/mL (200.72 mM)|
|Water||15 mg/mL (47.79 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02519400||Unknown status||Drug: Amitriptyline||Depression||Asan Medical Center||August 2015||Phase 1|
|NCT02101892||Completed||Drug: Amitriptyline|Drug: placebo||Migraine|Preventive Treatment||Rambam Health Care Campus|Migraine Research Foundation||April 2014||Not Applicable|
|NCT00516503||Completed||Drug: baclofen/amitriptyline/ketamine gel|Other: placebo||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||Drug: ketamine/amitriptyline NP-H cream|Other: placebo||Neurotoxicity|Pain|Peripheral Neuropathy|Unspecified Adult Solid Tumor Protocol Specific||Gary Morrow|National Cancer Institute (NCI)|University of Rochester||October 2007||Phase 3|
|NCT00991848||Completed||Drug: Lidocaine||Fibromyalgia|Chronic Pain||Federal University of São Paulo||January 2005||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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