For research use only.
CAS No. 549-18-8
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).
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|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)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04899206||Active not recruiting||Drug: Antihypertensive Agents||ACE Inhibitors|ARB|Hypertension|Depression||Sebastian Videla|Institut d''Investigació Biomèdica de Bellvitge|Institut Català de la Salut|Hospital Universitari de Bellvitge||March 30 2021||--|
|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|
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