| Identification | Back Directory | [Name]
BIS(7)-TACRINE | [CAS]
224445-12-9 | [Synonyms]
BIS(7)-TACRINE
Bis(heptyl)-cognitin dihydrochloride
Bis(heptyl)-cognitin dihydrochloride >=98% (HPLC)
N,N'-BIS(1,2,3,4-TETRAHYDRO-9-ACRIDINYL)-1,7-HEPTANEDIAMINE, DIHYDROCHLORIDE
heptylene-bis(tacrine) dihydrochloride, heptylene-bis(THA) dihydrochloride | [Molecular Formula]
C33H42Cl2N4 | [MDL Number]
MFCD08062163 | [MOL File]
224445-12-9.mol | [Molecular Weight]
565.62 |
| Hazard Information | Back Directory | [Uses]
Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease [1][2][3]. | [Biological Activity]
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 | [References]
[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. |
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Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
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