Home Neuronal Signaling AChR inhibitor - HNMT inhibitor Tacrine hydrochloride hydrate For research use only.

Tacrine hydrochloride hydrate

Synonyms: Tacrine, Tetrahydroaminacrine, Tetrahydroaminoacridine

Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that 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. It also acts as a histamine N-methyltransferase inhibitor.

Tacrine hydrochloride hydrate Chemical Structure

Tacrine hydrochloride hydrate Chemical Structure

CAS: 206658-92-6

Purity & Quality Control

Batch: S363901 DMSO] 50 mg/mL] false] Water] 50 mg/mL] false] Ethanol] 50 mg/mL] false Purity: >97%
97

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Biological Activity

Description Tacrine (Tetrahydroaminacrine, Tetrahydroaminoacridine) is a centerally active cholinesterase inhibitor that 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. It also acts as a histamine N-methyltransferase inhibitor.
Targets
HNMT [3] cholinesterase [1]
In vitro
In vitro Tacirne is an active cholinesterase inhibitor that blocks the degradation of cholinergic nerves in the cerebral cortex and hippocampus to increase cholinergic transmission. Tacrine induces hepatic damages in vitro. It can also induce oxidative stress and mitochondrial dysfunction. Tacrine treatment in HepG2 cells markedly inhibits the phosphorylation of GSK3β[1].
Cell Research Cell lines HepG2 cells
Concentrations 300 μM
Incubation Time 5 h
Method

The level of H2O2 generation was monitored in HepG2 cells by adding the DCFH-DA. After treatment of 10–100 µM LQ for 12 h prior to the addition of 300 µM tacrine for 5h, cells were stained with 50 µM DCFH-DA for 1 h. DCFH oxidation was determined at excitation and emission wavelengths of 485 and 530 nm using a microplate reader.
In Vivo
In vivo In rats, tacrine increased markers of liver damages (ALT and AST), degenerative region areas, and numbers of infiltrating inflammatory cells. Tacrine is known to induce hepatocyte necrosis and degeneration[1]. In the past, tacrine was used for the treatment of cognitive dysfunction during vascular dementia and Alzheimer disease. It is found to abolish lipopolysaccharide induced inflammation including IL-6 secretion in the central nervous system. Tacrine can aggravate the progress of tularemia in a mouse model--the effect would be beneficial in several pathologies such as neurodegenerative disorders; e.g. the positive effect of tacrine when used in therapy for Alzheimer's disease would be attributed to its anti-inflammatory action in addition to any improvement in cognitive functions[2].
Animal Research Animal Models Sprague-Dawley rats
Dosages 30 mg/kg
Administration p.o.

Chemical lnformation & Solubility

Molecular Weight 198.26(free bases) Formula

C13H14N2.xHCl.xH2O
CAS No. 206658-92-6 SDF Download Tacrine hydrochloride hydrate SDF
Smiles C1CCC2=NC3=CC=CC=C3C(=C2C1)N.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( ； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : 50 mg/mL


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