tacrine

Tacrine (CS 12602) is an indirect cholinergic agonist and centrally acting anticholinesterase. It is approved for the treatment of Alzheimer's disease.

Tacrine hydrochloride hydrate (Tetrahydroaminacrine) is a cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.

Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine with potential to treat Alzheimer's disease, prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors, and is a potent GABA A receptor antagonist[1] [2] [3].

Tacrine is a indirect cholinergic agonist and centrally acting anticholinesterase. Tacrine hydrochloride hydrate is an inhibitor of acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.

Dimetacrine is a useful antidepressant.

Dimetacrine tartrate is a tricyclic antidepressant (TCA) used for the therapy of depression in Europe and formerly in Japan.

Hydroxytacrine maleate (Velnacrine maleate) is a cholinesterase (cholinesterase) inhibitor that enhances memory in rodents and may be used in the study of Alzheimer's dementia of the Alzheimer type (SDAT).

7-Bromotacrine is a biochemical.

Monometacrine, a cholesterol esterase inhibitor, exhibits antidepressant effects [1].

TA-03 (7-Meota) is a potent inhibitor of AChE in treatment of cognitive manifestation of AD.

Velnacrine (1,2,3,4-tetrahydro-9-aminoacridin-1-ol maleate) is a biochemical.

Velnacrine-d3-1 maleate (HP 029-d3-1) is the deuterium-labeled form of Velnacrine maleate. Velnacrine maleate (HP 029) is an orally active cholinesterase inhibitor utilized in Alzheimer's disease research.

AChE/BChE-IN-35, a tacrine derivative, is a dual inhibitor of AChE and BChE capable of crossing the blood-brain barrier. It exhibits an IC50 of 123.66 nM for electric eel AChE, 122.34 nM for human AChE, and 488.00 nM for equine BChE. The compound crosses cell membranes through LAT1-mediated active transport, showing increased brain exposure and a slower clearance rate from brain tissue. AChE/BChE-IN-35 is applicable in Alzheimer's disease research.

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and/or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

1. Picfeltarraenin IA (Picfeltarraenin A), IB, IV, X, XI are stronger AChE inhibitions than the known AChE inhibitor Tacrine.

ZLMT-12 (compound 35) is a tacrine derivative and a potent inhibitor of CDK2 (IC50: 0.011 μM) and CDK9 (IC50: 0.002 μM). ZLMT-12 weakly inhibits AChE (IC50: 19.023 μM) and BuChE (IC50: 2.768 μM). ZLMT-12 has anti-proliferative activity and low cytotoxicity. ZLMT-12 blocks the cell cycle in S-phase and G2/M-phase and induces apoptosis.

AChE-IN-9, a Tacrine glycoconjugate connected to acetylated β-Glucose, acts as an AChE inhibitor, demonstrating an IC 50 value of 0.4 μM and exhibiting reduced hepatotoxicity in healthy cells. This compound finds use in Alzheimer's research [1].

Octahydroaminoacridine, a Tacrine analogue, acts as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). It is applicable in Alzheimer's disease (AD) research [1].

Picfeltarraenin IA (Standard) is a reference standard for research and analysis in studies involving Picfeltarraenin IA. 1. Picfeltarraenin IA (Picfeltarraenin A), IB, IV, X, XI are stronger AChE inhibitions than the known AChE inhibitor Tacrine.

Picfeltarraenin X shows stronger AChE inhibition than the known AChE inhibitor Tacrine.

1,3,5,6-Tetrahydroxyxanthone shows moderate hepatoprotective activity with EC(50) values of 160.2 +/- 0.6 microM against tacrine-induced cytotoxicity in HepG2 cells. It can inhibit angiotensin-I-converting-enzyme activity in a dose-dependent manner.

Onitin shows super-oxide and DPPH free radical scavenging effects.It also exhibits hepatoprotective activity on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells.

Torilin and torilolone show hepatoprotective effects on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells,the EC50 values are 20.6 +/- 1.86 and 3.6 +/- 0.1 microM, respectively; and silybin as a positive control shows an EC50 value of 69.0