Brain Extraction of 4-(4-Chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]pyridinium Ion (HPP+), a Neurotoxic Metabolite of Haloperidol: Studies Using [3H]HPP+ | Zendy

Hidekazu Kawashima | Zendy; Yasuhiko Iida | Zendy; Yoshihisa Kitamura | Zendy; Yasushi Kiyono | Zendy; Yasuhiro Magata | Zendy; Hideo Saji | Zendy

Open Access

Brain Extraction of 4-(4-Chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]pyridinium Ion (HPP+), a Neurotoxic Metabolite of Haloperidol: Studies Using [3H]HPP+

Author(s) -

Hidekazu Kawashima,

Yasuhiko Iida,

Yoshihisa Kitamura,

Yasushi Kiyono,

Yasuhiro Magata,

Hideo Saji

Publication year - 2002

Publication title -

the japanese journal of pharmacology

Language(s) - English

Resource type - Journals

eISSN - 1347-3506

pISSN - 0021-5198

DOI - 10.1254/jjp.89.426

Subject(s) - haloperidol , pyridinium , chemistry , metabolite , dopaminergic , pharmacology , biochemistry , endocrinology , dopamine , medicine , medicinal chemistry

Tritium-labeled 4-(4-chlorophenyl)-1-[4-(4-fluorophenyl)-4-oxobutyl]pyridinium ion (HPP+) was synthesized enzymatically from [3H]haloperidol using rat liver microsomal preparations, and using prepared [3H]HPP+, the passage of HPP+ into the brain was investigated. Consequently, HPP+ showed a moderate brain uptake index, indicating that it is able to permeate the blood-brain barrier. Furthermore, HPP+ was detected in murine brains after being intravenously injected. These results suggested that HPP+, produced mainly in the liver, is taken up into the brain and induces damage to brain dopaminergic neurons.

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