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.
Jang
Hye-Ock
HO
Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University, Pusan 602-739, Korea.
Jeong
Dong-Keun
DK
Ahn
Shin-Ho
SH
Yoon
Chang-Dae
CD
Jeong
Soo-Cheol
SC
Jin
Seong-Deok
SD
Yun
Il
I
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