Azacyclonol, also known as γ-pipradol, is used to diminish hallucinations in psychotic individuals. The formation of Azacyclonol in human intestinal microsomes is linear with
respect to time up to 60 min. The rates of it's formation increases
linearly with microsomal protein concentration up to 2 mg/mL. The apparent Km of Azacyclonol is 0.82 μM and the Vmax values is 60 pmol/min/mg protein in
microsomes from human liver. The formation of Azacyclonol and terfenadine
alcohol from terfenadine is confirmed to be catalyzed predominantly by CYP3A(4)
isozyme, and the ratio of the rate of terfenadine alcohol formation to that of
Azacyclonol is 3:1. The amount of Azacyclonol eliminated renally increases
on average 2-fold after rifampin dosing.
| Molecular Weight | 267.37 |
| Formula | C18H21NO |
| CAS Number | 115-46-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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