Effects of chlorpromazine HCl on the structural parameters of bovine brain membranes.
Fluorescence probes located in different membrane regions were used to evaluate the effects of chlorpromazine .HCl on structural parameters (transbilayer lateral mobility, annular lipid fluidity, protein distribution, and lipid bilayer thickness) of synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortex. The experimental procedure was based on the selective quenching of 1,3-di(1-pyrenyl)propane (Py-3-Py) by trinitrophenyl groups, radiationless energy transfer from the tryptophan of membrane proteins to Py-3-Py, and energy transfer from Py-3-Py monomers to 1-anilinonaphthalene-8-sulfonic acid (ANS). In this study, chlorpromazine .HCl decreased the lateral mobility of Py-3-Py in a concentration dependent-manner, showed a greater ordering effect on the inner monolayer than on the outer monolayer, decreased annular lipid fluidity in a dose dependent-manner, and contracted the membrane lipid bilayer. Furthermore, the drug was found to have a clustering effect on membrane proteins.
Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University, Pusan 602-739, Korea.
Hye-Ock
HO
Jang
Dong-Keun
DK
Jeong
Shin-Ho
SH
Ahn
Chang-Dae
CD
Yoon
Soo-Cheol
SC
Jeong
Seong-Deok
SD
Jin
Il
I
Yun
D000818:Animals; D001921:Brain / Q000166:cytology / Q000187:drug effects*; D002417:Cattle; D002746:Chlorpromazine / Q000378:metabolism / Q000494:pharmacology*; D008051:Lipid Bilayers / Q000737:chemistry; D013570:Synaptic Membranes / Q000187:drug effects*; D013574:Synaptosomes / Q000187:drug effects
D008051:Lipid Bilayers; D002746:Chlorpromazine