Azacyclonol (Synonyms: MDL 4829, MER 17, γ-Pipradol)

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.Target: OthersAzacyclonol is a drug which is a so-called ataractive, or agent which diminishes 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 formation of Azacyclonol increases linearly with microsomal protein concentration up to 2 mg/mL. The apparent Km and Vmax values of Azacyclonol are 0.82 μM and 60 pmol/min/mg protein in microsomes from human liver [1]. 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 [2]. The amount of Azacyclonol eliminated renally increases on average 2-fold after rifampin dosing [3].

References:
[1]. Raeissi, S.D., et al., Comparison of CYP3A activities in a subclone of Caco-2 cells (TC7) and human intestine. Pharm Res, 1997. 14(8): p. 1019-25.
[2]. Ling, K.H., et al., Metabolism of terfenadine associated with CYP3A(4) activity in human hepatic microsomes. Drug Metab Dispos, 1995. 23(6): p. 631-6.
[3]. Brown, D.A. and J.P. Quilliam, The effects of some centrally acting drugs on ganglionic transmission in the cat. Br J Pharmacol Chemother, 1964. 23(2): p. 241-56.