1684-40-8 Usage
Description
Different sources of media describe the Description of 1684-40-8 differently. You can refer to the following data:
1. Tacrine is the first therapeutic launched specifically for the treatment of Alzheimer's
disease which affects four million people in the US alone. Clinically significant improvement in
cognition has been demonstrated in the patients with Alzheimer's disease. Although the
cause of Alzheimer's disease is not understood, degeneration of cholinergic neurons is
thought to be a primary factor in the development and progression of the disease. Tacrine is a
reversible acetylcholinesterase inhibitor that presumably acts centrally by elevating the
acetylcholine level in the cerebral cortex and by slowing degradation of acetylcholine from
intact cholinergic neurons. While tacrine improves the symptoms of Alzheimer's disease, the
underlining cause of the dementing process is not altered. It has also been suggested that the
beneficial effects of tacrine may be due to its multiple effects on several neurotransmitter
systems.
2. Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively). Tacrine also inhibits the uptake of serotonin and norepinephrine in rat cerebral cortex and decreases depolarization-induced calcium influx through L-type calcium channels in SN56 neuronal cells. Formulations containing tacrine have been used clinically in the treatment of Alzheimer’s disease.
Chemical Properties
Pale Yellow Solid
Originator
NIH (U.S.A.)
Uses
Different sources of media describe the Uses of 1684-40-8 differently. You can refer to the following data:
1. anticholinesterase, cognitive adjuvant, K channel blocker
2. A potent centrally acting anticholinesterase, for therapy of memory deficits in patients with Alzheimers disease. THA also selectively blocks potassium channels in the central nervous system, which results in an increased release of acetylcholi
3. A potent centrally acting anticholinesterase for therapy of memory deficits in patients with Alzheimer's disease. THA also selectively blocks potassium channels in the central nervous system, which results in an increased release of acetylcholine and a prolongation of the action potential of the presynaptic cholinergic neurons.
Brand name
Cognex (Sciele).
General Description
Different sources of media describe the General Description of 1684-40-8 differently. You can refer to the following data:
1. Tacrine hydrochloride,1,2,3,4-tetrahydro-9-aminoacridine hydrochloride (THA,Cognex), is a reversible cholinesterase inhibitor that hasbeen used in the treatment of Alzheimer disease for severalyears. The drug has been used to increase the levels of AChin these patients on the basis of observations from autopsiesthat concentrations of ChAT and AChE are markedly reducedin the brain, whereas the number of muscarinic receptorsis almost normal. The use of the drug is not withoutcontroversy, as conflicting results on efficacy have been reported.The drug has been used in mild-to-moderateAlzheimer dementia.
2. Yellow needles (from concentrated hydrochloric acid); white powder. pH of 1.5% solution: 4.5-6. Bitter taste.
Air & Water Reactions
Water soluble.
Reactivity Profile
TACRINE HYDROCHLORIDE is incompatible with strong oxidizing agents, acid chlorides and acid anhydrides . Neutralize bases in slightly exothermic reactions.
Fire Hazard
Flash point data for TACRINE HYDROCHLORIDE are not available; however, TACRINE HYDROCHLORIDE is probably combustible.
Biological Activity
Potent cholinesterase inhibitor, a cognition enhancer in vivo .
Metabolism
Tacrine is
extensively metabolized by CYP450 to at least three metabolites. The major metabolite, 1-hydroxy-tacrine, is active. Its elimination half-life is
between 1.5 and 4 hours, with metabolites being are excreted via the urine.
Check Digit Verification of cas no
The CAS Registry Mumber 1684-40-8 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 1,6,8 and 4 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1684-40:
(6*1)+(5*6)+(4*8)+(3*4)+(2*4)+(1*0)=88
88 % 10 = 8
So 1684-40-8 is a valid CAS Registry Number.
InChI:InChI=1/C13H14N2.ClH/c14-13-9-5-1-3-7-11(9)15-12-8-4-2-6-10(12)13;/h1,3,5,7H,2,4,6,8H2,(H2,14,15);1H
