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Brain regional pharmacokinetics of biperiden in rats
Author(s) -
Yokagawa Koichi,
Nakashima Emi,
Ishizaki Junko,
Hasegawa Mitsuru,
Kido Hideki,
Ichimura Fujio
Publication year - 1992
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510130207
Subject(s) - pons , medulla oblongata , hippocampus , thalamus , pharmacokinetics , cerebellum , cortex (anatomy) , endocrinology , midbrain , medicine , basal ganglia , amygdala , hypothalamus , central nervous system , chemistry , biology , neuroscience
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.