Nonclassical and endogenous cannabinoids: effects on the ordering of brain membranes. Neurochem Res 1997 May;22(5):563-8
Date
05/01/1997Pubmed ID
9131634DOI
10.1023/a:1022413901857Scopus ID
2-s2.0-0030998073 (requires institutional sign-in at Scopus site) 36 CitationsAbstract
The effects of several nonclassical cannabinoids and the endogenous cannabinoid ligand, anandamide on the lipid ordering of rat brain synaptic plasma membranes (SPM) were examined and compared to delta 9-tetrahydrocannabinol (delta 9-THC). SPM order was determined using fluorescence polarization. All compounds tested affected membrane ordering. delta 9-THC, CP-55,940, CP-55,244 and WIN-55212 decreased lipid ordering in SPM. Some stereospecificity was observed with delta 9-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.
Author List
Bloom AS, Edgemond WS, Moldvan JCMESH terms used to index this publication - Major topics in bold
AnalgesicsAnimals
Arachidonic Acid
Arachidonic Acids
Benzoxazines
Brain
Cannabinoids
Cyclohexanols
Dronabinol
Endocannabinoids
Male
Membrane Lipids
Morpholines
Naphthalenes
Phenanthridines
Polyunsaturated Alkamides
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Synaptic Membranes