Brain regional pharmacokinetics of biperiden in rats

✍ Scribed by Koichi Yokagawa; Emi Nakashima; Junko Ishizaki; Mitsuru Hasegawa; Hideki Kido; Fujio Ichimura

• Publisher: John Wiley and Sons
• Year: 1992
• Tongue: English
• Weight: 501 KB
• Volume: 13
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.2510130207

✦ Synopsis

Abstract

The pharmacokinetic profiles of biperiden (BP) in blood and in specific brain regions were investigated in rats after acute i.v. administration. The regional brain‐to‐blood unbound concentration ratios (K~pf~) were also determined after 16h intravenous infusion of BP. The K~pf~ values ranged from 30 to 75 in the different brain regions and showed decreasing concentrations in the following order: pons + medulla oblongata, basal ganglia, amygdala, hypothalamus, thalamus, mesencephalon, bulbus olfactorius + septum, hippocampus, frontal cortex, occipital cortex, cerebellum. The relationship between BP and acetylcholine (ACh) concentrations in the brain regions was examined. ACh levels in the various brain regions ranged from 8 to 44 ng g^−1^ tissue. There was a significant correlation between the K~pf~ values of BP and the levels of ACh in the brain regions except for the pons + oblongata. BP concentrations in the brain regions after BP administration were predicted based on the physiological pharmacokinetics. There was reasonable agreement between the model predictions and the observed data.