ISSN:
1573-6903
Keywords:
Cannabinoids
;
anandamide
;
membrane order
;
fluorescence polarization
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract The effects of several nonclassical cannabinoids and the endogenous cannabinoid ligand, anandam-ide on the lipid ordering of rat brain synaptic plasma membranes (SPM) were examined and compared to Δ9-tetrahydrocannabinol (Δ9-THC). SPM order was determined using fluorescence polarization. All compounds tested affected membrane ordering. Δ9-THC, CP-55,940, CP-55,244 and WIN-55212 decreased lipid ordering in SPM. Some stereospecificity was observed with Δ9-THC and WIN-55212, but not other compounds. Anandamide also decreased lipid order as did its putative precursor, arachidonic acid. In contrast to these compounds, levonantradol increased SPM lipid order. Although all pharmacologically active cannabinoids affect SPM lipid order, potency on this measure does not correlate well with their pharmacological potency. The results of this study suggest that membrane perturbation (either increases or decreases in lipid order) may be a necessary characteristic for cannabinoid pharmacological activity, but it is not a primary or sufficient determinate of action for this class of drugs.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1022413901857
Permalink
