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Nortriptyline (hydrochloride) (Synonyms: Acetexa,Pamelor®)

Catalog No.GC11989

norepinephrine and serotonin transporters blocker

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Nortriptyline (hydrochloride) Chemical Structure

Cas No.: 894-71-3

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10mg
$18.00
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50mg
$45.00
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100mg
$71.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Ki: 3.4 nM: blocks the norepinephrine transporter.

Ki: 161 nM: inhibits the serotonin transporter.

Nortriptyline, a dibenzocycloheptene-derivative tricyclic antidepressant, inhibits norepinephrine and serotonin transporters, which is used for short-term treatment of various forms of depression, including major depression, dysthymia, and atypical depressions. Nortriptyline suppresses the norepinephrine presynaptic receptors, thus inhibiting the reuptake of this neurotransmitter and increasing the concentration in the synaptic cleft in the central nervous system.

Norepinephrine transporter is responsible for the sodium-chloride (Na+/Cl-) -dependent reuptake of extracellular norepinephrine. Serotonin transporter transports serotonin from the synaptic cleft to the presynaptic neuron.

In vitro: Nortriptyline dose-dependently dampened the spontaneous migration of human polymorphonuclear cells (PMN) at the highest concentrations (10-4 and 10-5 M). Nortriptyline decreased the motility of the cells at 10-4M. Chemotaxis of PMN triggered by 10-10M N-formyl-L-methionil-L-leucyl-L-phenylalanine (FMLP) was blocked by nortriptyline in a dose-dependent fashion [1].

In vivo: Rats and mice were injected intraperitoneally with nortriptyline at the dose of 50, 25, 12.5 mg/kg. After 2 hours of the last injection, nortriptyline inducted little or no inhibition of the 4, α-dimethyl-meta-tyramine (H 77/77) induced depletion in a dose of 25 + 12.5 mg/kg. However, there was a partial blockade, evoked by nortriptyline in a dose of 50 + 25 mg/kg, of the H 77/77 elicited depletion in the noradrenaline nerve terminals in all the rats studied. Additionally, nortriptyline also proved to be active in the brain, however, its activity was low [2].

References:
[1].  Sacerdote, P., Bianchi, M., & Panerai, A. Chlorimipramine and nortriptyline but not fluoxetine and fluvoxamine inhibit human polymorphonuclear cell chemotaxis In vitro. General Pharmacology: The Vascular System. 1994; 25(3): 409-412.
[2].  Carlsson, A., Corrodi, H., Fuxe, K., & Hkfelt, T. Effects of some antidepressant drugs on the depletion of intraneuronal brain catecholamine stores caused by 4, α-dimethyl-meta-tyramine. European Journal of Pharmacology.1969; 5(4): 367-373.

Chemical Properties

Cas No. 894-71-3 SDF
Synonyms Acetexa,Pamelor®
Chemical Name 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine, monohydrochloride
Canonical SMILES CNCC/C=C1C2=C(C=CC=C2)CCC3=C/1C=CC=C3.Cl
Formula C19H21N • HCl M.Wt 299.8
Solubility ≥ 15mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.3356 mL 16.6778 mL 33.3556 mL
5 mM 0.6671 mL 3.3356 mL 6.6711 mL
10 mM 0.3336 mL 1.6678 mL 3.3356 mL
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Reviews

Review for Nortriptyline (hydrochloride)

Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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