1,2,3,4-Tetrahydroacridin-9-aminmonohydrochlorid

Bezeichnung:1,2,3,4-Tetrahydroacridin-9-aminmonohydrochlorid

CAS-Nr1684-40-8

Englisch Name:TACRINE HYDROCHLORIDE

CBNumberCB5402661

SummenformelC13H15ClN2

Molgewicht234.72

MOL-Datei1684-40-8.mol

Synonyma

1,2,3,4-Tetrahydroacridin-9-aminmonohydrochlorid

1,2,3,4-Tetrahydroacridin-9-aminmonohydrochlorid physikalisch-chemischer Eigenschaften

Schmelzpunkt	280-284 °C(lit.)
storage temp.	Inert atmosphere,2-8°C
Löslichkeit	Soluble in aqueous buffers
pka	pKa 9.8 (Uncertain)
Aggregatzustand	Crystalline solid
Farbe	White to light yellow
CAS Datenbank	1684-40-8(CAS DataBase Reference)
EPA chemische Informationen	Tacrine hydrochloride (1684-40-8)

Sicherheit

Kennzeichnung gefährlicher	T,Xn
R-Sätze:	25-36/37/38-20/22
S-Sätze:	26-36-45
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	AR9532500
HazardClass	6.1(a)
PackingGroup	II
Toxizität	LD50 intravenous in mouse: 5600ug/kg

Gefahreninformationscode (GHS)

TACRINE HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R20/22:Gesundheitsschädlich beim Einatmen und Verschlucken.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Beschreibung
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.
Beschreibung
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.
Chemische Eigenschaften
Pale Yellow Solid
Originator
NIH (U.S.A.)
Verwenden
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
Verwenden
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.
Verwenden
anticholinesterase, cognitive adjuvant, K channel blocker
Trademarks
Cognex (Sciele).
Allgemeine Beschreibung
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.
Allgemeine Beschreibung
Yellow needles (from concentrated hydrochloric acid); white powder. pH of 1.5% solution: 4.5-6. Bitter taste.
Air & Water Reaktionen
Water soluble.
Reaktivität anzeigen
TACRINE HYDROCHLORIDE is incompatible with strong oxidizing agents, acid chlorides and acid anhydrides . Neutralize bases in slightly exothermic reactions.
Brandgefahr
Flash point data for TACRINE HYDROCHLORIDE are not available; however, TACRINE HYDROCHLORIDE is probably combustible.
Biologische Aktivität
Potent cholinesterase inhibitor, a cognition enhancer in vivo .
Stoffwechsel
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.

1,2,3,4-Tetrahydroacridin-9-aminmonohydrochlorid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

1684-40-8, TACRINE HYDROCHLORIDE Verwandte Suche:

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