Name | Donepezil |
Synonyms | n-1-one DONEPEZIL Donepezil Donepesil AKOS 226-23 Donepezil base 5,6-Dimethoxy-2,3-dihydro-1H-inden-1-one 1-Benzyl-4-[(5,6-dimethoxy-1-indanone)-2-yl]methylpiperidine N-Benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl] piperidine 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL) METHYL] PIPERIDINE 2-[(1-benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one 2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-1-one 2,3-dihydro-5,6-dimethoxy-2-((1-(phenylmethyl)-4-piperidinyl)methyl)-1h-inde |
CAS | 120014-06-4 |
EINECS | 601-651-9 |
InChI | InChI=1/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3 |
Molecular Formula | C24H29NO3 |
Molar Mass | 379.49 |
Density | 1.141±0.06 g/cm3(Predicted) |
Melting Point | 207°C |
Boling Point | 527.9±50.0 °C(Predicted) |
Flash Point | 273.1°C |
Water Solubility | 2.931 mg/L |
Solubility | Acetone (Slightly), Chloroform (Slightly) |
Vapor Presure | 3.11E-11mmHg at 25°C |
Appearance | White to white-like powder |
Color | White to Off-White |
pKa | 8.84±0.10(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
Refractive Index | 1.578 |
MDL | MFCD00912833 |
Physical and Chemical Properties | White or off-white crystalline powder |
Use | Donepezil hydrochloride monohydrate is a central reversible acetylcholinesterase inhibitor. |
In vitro study | Donepezil has a reversible, non-competitive inhibitory effect on AChE. It is 500-1000 times more selective for AChE than BuChE. Short-and long-term drug exposure to human SH-SY5Y neuroblastoma cells induces a concentration-dependent inhibition of cell proliferation that is independent of muscarinic or nicotinic receptor blockade and apoptosis. Donepezil reduces the number of cells in the S-G2/M phase of the cell cycle, increases the number of cells in the G0/G1 phase, and reduces the expression of two cyclins in the G1/S and G2/M transitions: cyclin E and cyclin B. At the same time, it also increases the expression of the cell cycle inhibitor p21. In addition, donepezil increases action potential-dependent dopamine release and modulates nicotinic receptors in substantia nigra dopaminergic neurons. |
In vivo study | Donepezil is slowly absorbed from the gastrointestinal tract, with a terminal half-life of 50-70 hours in young volunteers and greater than 100 hours in the elderly. After extensive liver metabolism, the plasma protein binding of this parent compound was 93%. Donepezil is metabolized in the liver by the cytochrome P450 system (CYP1A2-, CYP2D6-, CYP3A4-related). In animals, donepezil is unchanged in the brain, and no metabolites are found in neural tissues. In plasma, urine and bile, most of the donepezil metabolites are O-glucuronides. After oral ingestion, the peak plasma concentration is reached within 3-5 hours, and its absorption is not affected by food. Donepezil has linear pharmacokinetics in the concentration range 1-10 mg/day. 96% of the circulating donepezil is protein-bound. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
UN IDs | UN 2811 |
HS Code | 29333990 |