894-71-3 Usage
Description
NORTRIPTYLINE HYDROCHLORIDE, also known as 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)Nmethyl-1-propanamine hydrochloride or 5-(3-methyl-aminopropylidene)-10,11-hydro-5H-dibenzo[a,d] cycloheptene hydrochloride (Aventyl, Pamelor), is a tricyclic antidepressant. It is an off-white solid with pertinent biological and chemical properties similar to those of amitriptyline, including metabolic inactivation and elimination. Nortriptyline functions as a selective NE (norepinephrine) transporter (NET) inhibitor.
Uses
Used in Pharmaceutical Industry:
NORTRIPTYLINE HYDROCHLORIDE is used as a tricyclic antidepressant for the treatment of depression and other mood disorders. It works by inhibiting the reuptake of norepinephrine, thereby increasing its levels in the brain and alleviating depressive symptoms.
Therapeutic Function
Antidepressant
Biological Activity
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].
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.
Check Digit Verification of cas no
The CAS Registry Mumber 894-71-3 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 8,9 and 4 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 894-71:
(5*8)+(4*9)+(3*4)+(2*7)+(1*1)=103
103 % 10 = 3
So 894-71-3 is a valid CAS Registry Number.
InChI:InChI=1/C19H21N.ClH/c1-20-14-6-11-19-17-9-4-2-7-15(17)12-13-16-8-3-5-10-18(16)19;/h2-5,7-11,20H,6,12-14H2,1H3;1H