• BMB Reports
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• 제33권6호
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• pp.541-547
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• 2000

Fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH) was used to evaluate the effects of chlorpromazine HCl on the range of the rotational mobility of bulk bilayer structure of the synaptosomal plasma membrane vesicles (SPMV) isolated from a bovine brain. In a dose-dependent manner, chlorpromazine HCl increased the anisotropy (r), limiting anisotropy ($r_{\infty}$) and order parameter (S) of DPH in the membranes. Cationic 1-[4-(trimethylammonio)-phenyl]-6-phenylhexa-1,3,5-hexatriene (TMA-DPH) and anionic 3-[p-(6-phenyl)-1,3,5-hexatrienyl]-phenylpropionic acid (PRO-DPH) were utilized to examine the range of transbilayer asymmetric rotational mobility of the neuronal membranes. The anisotropy (r) of TMA-DPH in the inner monolayer was 0.034 greater than the value of PRO-DPH in the outer monolayer of the membranes. Both cationic TMA-DPH and anionic PRO-DPH were also used to examine the transbilayer asymmetric effects of chlorpromazine HCl on the range of rotational mobility of the membranes. Chlorpromazine HCl have a decreasing effects on the rotational mobility of the bulk bilayer structures and have a greater decreasing effect on the mobility of the inner monolayer as compared to the outer monolayer of the membranes. It has been proven that chlorpromazine HCl exhibit a selective rather than nonselective fluidizing effect within the transbilayer domains of the SPMV.

• BMB Reports
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• 제37권5호
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• pp.603-611
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• 2004

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.

• 약학회지
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• 제33권4호
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• pp.211-218
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• 1989

Twenty-six injectable drug products, many of which are administered by i.v. infusion, were studied for loss from aqueous solutions stored in polyvinyl chloride (PVC) infusion bags for various periods of time. The PVC infusion bags were stored in the dark room at room temperature for up to one month. Drugs stored in glass bottle served as controls. The solutions were assayed Spectrophotometrically at regular intervals. The effect of drug concentration and pH on the loss of drug from solution were studied. Octanol-water partition coefficients were used as a guage of lipid solubility of drugs. The elution of di(2-ethylhexyl)phthalate(DEHT) from PVC infusion bags was studied. For most of the drug studied, minimal loss from the aqueous solutions were observed over periods of storage time. Six of the drug products - Thiopental sodium, Hydralazine HCl, Thioridazine HCl, Trifluoperazine 2HCl, Metronidazole, Chlorpromazine HCl - were found to be lost a substantial extent. DEHP was found to be migrating from PVC infusion bags.