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Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.
Description | Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity. |
In vivo | Pazinaclone (5 mg/kg; oral; rats, mice, hamsters, and guinea pigs) unchanged drug concentration in plasma was highest in mice (AUC; 90 ng/h/ml), followed in decreasing order by guinea pigs (AUC; 41 ng/h/ml), hamsters (AUC; 18 ng/h/ml), and rats (AUC; 17 ng/h/ml). Among rabbits, dogs, and monkeys, the dogs had the highest plasma drug concentrations: AUCs of pazinaclone in dogs and monkeys were 1035 and 458 ng. h/ml, respectively (drug concentration in rabbit plasma was very low). Of the two polymorphs, forms 1 and 2 with particle size of < or = 5 microns, the oral absorption of form 2 in rats was more efficient than that of form 1 at 1000 mg/kg: AUCs of pazinaclone after dosing of form 1 and 2 were 489 and 965 ng.h/ml, respectively.[2] |
Alias | DN-2327, DN2327, DN 2327, A-77000, A77000, A 77000 |
Molecular Weight | 478.93 |
Formula | C25H23ClN4O4 |
Cas No. | 103255-66-9 |
Smiles | C(C(=O)N1CCC2(CC1)OCCO2)C3N(C(=O)C=4C3=CC=CC4)C5=NC6=C(C=C5)C=CC(Cl)=N6 |
Relative Density. | 1.48 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.79 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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