3-(10,11-Dihydro-5H-dibenzo(a,d)-cyclohepten-5-yliden)-N-methyl-1-propanamin-hydrochlorid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

NORTRIPTYLINE HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R36/38:Reizt die Augen und die Haut.
  R23/25:Giftig beim Einatmen und Verschlucken.
  R11:Leichtentzündlich.

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
  S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
  S24:Berührung mit der Haut vermeiden.
  S16:Von Zündquellen fernhalten - Nicht rauchen.
  S7:Behälter dicht geschlossen halten.

• Chemische Eigenschaften

  Off-White Solid

• Originator

  Aventyl,Lilly,UK,1963

• Verwenden

  Nortriptyline Hydrochloride (Amitriptyline EP Impurity C) is a tricyclic antidepressant.

• Verwenden

  Monoamine reuptake inhibitor; tricyclic antidepressant.

• Definition

  ChEBI: Nortriptyline hydrochloride is an organic tricyclic compound. It has a role as a geroprotector.

• Manufacturing Process

  A mixture of 114.5 g of 5-(3-chloropropylidene)dibenzo[a,d]cyclohepta[1,4] diene, 75 ml of benzene, and about 400 ml of methylamine is heated in an autoclave at 120°C for six hours. The excess methylamine is distilled from the reaction mixture under vacuum and the residue is stirred with 300 ml of water. Acidification of the mixture with hydrochloric acid causes the separation of the hydrochloride of 5-(3-methylaminopropylidene)dibenzo[a,d] cyclohepta[1,4]diene. The product is collected by filtration and is purified by recrystallization from a mixture of absolute ethanol and ethyl acetate. MP 210°C to 212°C.

• Trademarks

  Aventyl Hydrochloride (Lilly); Aventyl Hydrochloride (Ranbaxy); Pamelor (Tyco).

• Therapeutic Function

  Antidepressant

• Allgemeine Beschreibung

  Pertinent biological and chemical properties for nortriptyline,3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)Nmethyl-1-propanamine hydrochloride, 5-(3-methyl-aminopropylidene)-10,11-hydro-5H-dibenzo[a,d] cycloheptene hydrochloride(Aventyl, Pamelor), are given previously in thediscussion of amitriptyline. Metabolic inactivation and eliminationare like those of amitriptyline. Nortriptyline is a selectiveNE transporter (NET) inhibitor.

• Biologische Aktivität

  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.

• Biochem/physiol Actions

  Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 3.4 nM) than the serotonin transporter (Ki = 161 nM). 5-HT2 serotonin receptor antagonist.

• 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].

• Einzelnachweise

  [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.

NORTRIPTYLINE HYDROCHLORIDE Upstream-Materialien And Downstream Produkte

3-(10,11-Dihydro-5H-dibenzo(a,d)-cyclohepten-5-yliden)-N-methyl-1-propanamin-hydrochlorid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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