Home Neuronal Signaling Serotonin Transporter inhibitor - Histamine Receptor inhibitor - 5-HT Receptor inhibitor Amitriptyline HCl

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Amitriptyline HCl Serotonin Transporter inhibitor

Cat.No.S3183

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. This compound 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. It is a tricyclic antidepressant (TCA).
Amitriptyline HCl Serotonin Transporter inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 313.86

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S318301 DMSO]63 mg/mL]false]Ethanol]63 mg/mL]false]Water]15 mg/mL]false Purity: 99.88%
99.88

Chemical Information, Storage & Stability

Molecular Weight 313.86 Formula

C20H23N.HCl

 Storage (From the date of receipt)
CAS No. 549-18-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)CCC=C1C2=CC=CC=C2CCC3=CC=CC=C31.Cl

Solubility

In vitro
Batch:

DMSO : 63 mg/mL ( (200.72 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 63 mg/mL

Water : 15 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
Histamine Receptor H1 [9]
0.5 nM(Ki)
SERT [1]
3.45 nM(Ki)
Histamine receptor H4 [2]
7.31 nM(Ki)
NET [1]
13.3 nM(Ki)
5-HT2 [3]
235 nM(Ki)
Sigma 1 receptor [4]
287 nM(Ki)
In vitro

Amitriptyline inhibits Forskolin-stimulated cyclic AMP accumulation with EC50 values of 16.2 μM in intact CHO/DOR cells. This compound causes a concentration-dependent stimulation of ERK1/2 and GSK-3β phosphorylation with EC50 values of 9.0 μM in CHO/DOR cells. It (15 μM) causes a stimulation of ERK1/2 phosphorylation in C6 cells. This chemical (30 μM) inhibits Forskolin-stimulated adenylyl cyclase activity and antagonizes (−)-U50,488 inhibitory effect in rat nucleus accumbens. [5] It binds the extracellular domain of both TrkA and TrkB and promotes TrkA-TrkB receptor heterodimerization. This compound (< 500 nM) promotes TrkA autophosphorylation in primary neurons and induces neurite outgrowth in PC12 cells. It selectively protects T17 cells from apoptosis with EC50 of 50 nM. [6]
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] This compound (15 mg/kg and 30 mg/kg, i.p.) dose-dependently decreases the immobility time in the forced swimming test (FST) of mice. This chemical (15 mg/kg, i.p.) shows a significant 24-h rhythm in the immobility time in the forced swimming test (FST) of mice. [7] It (1 mg/kg and 3 mg/kg) significantly increases the total distance travelled of mice in novel cages. This compound (10 mg/kg p.o., twice daily) considerably attenuates the hypothermic response to 8-OHDPAT and mCPP in mice. It (10 mg/kg p.o., twice daily) significantly reduces serotonin transporter density by approximately 20% in cortex of mice. [8]
References
  • https://pubmed.ncbi.nlm.nih.gov/17689532/
  • https://pubmed.ncbi.nlm.nih.gov/19828880/
  • https://pubmed.ncbi.nlm.nih.gov/19549602/
  • https://pubmed.ncbi.nlm.nih.gov/16079297/
  • https://pubmed.ncbi.nlm.nih.gov/16032412/
  • https://pubmed.ncbi.nlm.nih.gov/16782354

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06312813 Recruiting
Rosacea
Wright State University
 February 27 2024 Phase 2
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

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