BIS(7)-TACRINE Struktur

BIS(7)-TACRINE

Bezeichnung:BIS(7)-TACRINE

CAS-Nr224445-12-9

Englisch Name:BIS(7)-TACRINE

CBNumberCB7428931

SummenformelC33H42Cl2N4

Molgewicht565.62

MOL-Datei224445-12-9.mol

BIS(7)-TACRINE physikalisch-chemischer Eigenschaften

storage temp.	2-8°C
Löslichkeit	H2O: soluble10mg/mL, clear
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25-36/37/38
S-Sätze:	26-36-45
RIDADR	UN 2811 6.1/PG 3

BIS(7)-TACRINE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R25:Giftig beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
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).
Biologische Aktivität
bis(7)-tacrine is an ache inhibitor.acetylcholinesterase ( ache), the primary cholinesterase in the body, is an enzyme catalyzing the breakdown of acetylcholine and of some other choline esters that function as neurotransmitters.
in vitro
bis(7)-tacrine, the 9-amino-1,2,3,4-tetrahydroacridine (tha) dimer, was identified as a promising drug candidate for the palliative treatment of alzheimer's disease, due to its significant enhancement in acetylcholinesterase (ache) inhibition potency and ache/butyrylcholinesterase (bche) selectivity relative to tha itself. enzyme kinetic studies performed in rat cortex found that both bis(7)-tacrine and tha exhibited mixed inhibition, and the rat cortex ki values were consistent with the previously determined human cerebellum ki values [1].
in vivo
previous study evaluated the neuropharmacological effects of tha on memory impairment caused by scopolamine injection. balb/c mice were orally treated with tha at 10 mg/kg for 10 days. results showed that tha significantly could reduce the total number of entry error and reference memory errors. in addition, tha also inhibited the ache activity in the hippocampus significantly [2].
IC 50
0.40 nm
Einzelnachweise
[1] carlier, p. r.,han, y.f.,chow, e.s.h., et al. evaluation of short-tether bis-tha ache inhibitors. a further test of the dual binding site hypothesis. bioorganic & medicinal chemistry 7, 351-357 (1999).
[2] lee js, hong ss, kim hg, lee hw, kim wy, lee sk, son cg. gongjin-dan enhances hippocampal memory in a mouse model of scopolamine-induced amnesia. plos one. 2016 aug 2;11(8):e0159823.

BIS(7)-TACRINE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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