Azacyclonol

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.