タクリン·塩酸塩 化学特性,用途語,生産方法
効能
認知症治療薬, アセチルコリンエステラーゼ阻害薬
説明
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.
化学的特性
Pale Yellow Solid
使用
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
一般的な説明
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.
空気と水の反応
Water soluble.
反応プロフィール
TACRINE HYDROCHLORIDE is incompatible with strong oxidizing agents, acid chlorides and acid anhydrides . Neutralize bases in slightly exothermic reactions.
火災危険
Flash point data for TACRINE HYDROCHLORIDE are not available; however, TACRINE HYDROCHLORIDE is probably combustible.
生物活性
Potent cholinesterase inhibitor, a cognition enhancer in vivo .
代謝
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.
タクリン·塩酸塩 上流と下流の製品情報
原材料
準備製品