A comparative study of the plasma membrane permeabilization and fluidization induced by antipsychotic drugs in the rat brain

• Murata Tetsuhito

• Maruoka Nobuyuki

• Omata Naoto

• Takashima Yasuhiro

• Fujibayashi Yasuhisa

• Yonekura Yoshiharu

• Wada Yuji

抄録

We compared the potency of the interaction of three antipsychotic drugs, i.e., chlorpromazine (CPZ), haloperidol (HAL) and sulpiride (SUL), with the plasma membrane in the rat brain. CPZ loading ( 100 M) dose-dependently increased both membrane permeability (assessed as [18F]2-fluoro-2-deoxy-D-glucose-6-phosphate release from brain slices) and membrane fluidity (assessed as the reduction in the plasma membrane anisotropy of 1,6-diphenyl-1,3,5-hexatriene). On the other hand, a higher concentration of HAL (1 mM) was required to observe these effects. However, SUL failed to change membrane permeability and fluidity even at a high concentration (1 mM). These results indicated the following ranking of the potency to interact with the membrane: CPZ > HAL > SUL. The difference among antipsychotic drugs in the potency to interact with the plasma membrane as revealed in the present study may be partly responsible for the difference among the drugs in the probability of inducing extrapyramidal side effects such as parkinsonism and tardive dyskinesia.

収録刊行物

• The international journal of neuropsychopharmacology

  The international journal of neuropsychopharmacology 10 (5), 683-689, 2007-10

  Cambridge University Press

キーワード

• Plasma membrane
• Chlorpromazine
• Haloperidol
• Sulpiride
• Extrapyramidal side effects

詳細情報

• CRID: 1570009752586501120
• NII論文ID: 120000807644
• ISSN: 14611457
• Web Site: http://hdl.handle.net/10098/1173
• 本文言語コード: en
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