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Nortriptyline(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nortriptyline(hydrochloride)图片
CAS NO:894-71-3
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议

产品介绍
阿米替林的主要活性代谢物去甲米替林(Desmethylamitriptyline hydrochloride)是一种三环类抗抑郁药,用于缓解抑郁症的症状。
Cas No.894-71-3
别名盐酸去甲替林; Desmethylamitriptyline hydrochloride; Desitriptilina hydrochloride
化学名3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine, monohydrochloride
Canonical SMILESCNCC/C=C1C2=C(C=CC=C2)CCC3=C/1C=CC=C3.Cl
分子式C19H21N o HCl
分子量299.8
溶解度≥ 15mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.