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 recep
Storage Temp
Store at -80°C
Shipped In
Dry ice packs + Cold packs
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Action Type
INHIBITOR
Mechanism of action
Norepinephrine transporter inhibitor
Product Description
Information
Amitriptyline HCl is an inhibitor of bothserotonin transporter (SERT)andnorepinephrine transporter (NET)with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibitshistamine receptor H1,histamine receptor H4,5-HT2andsigma 1 receptorwith K 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. 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
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. Cell Data
cell lines：Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30)
