delta-9-Tetrahydrocannabinol inhibits the binding of theophylline to mammalian neuronal and non-neuronal membranes.
Theophylline (Th) (11.0 x 10(-6)-550.0 x 10(-6) M) shows dose dependent binding to the subcellular membranes of rat brain and liver. Its binding to neuronal membranes is in the order of synaptosome > microsome or mitochondrion > myelin. However, in the liver, Th binding to microsomes is greater than that to mitochondria. In all the membranes studied delta-9-tetrahydrocannabinol (THC) (1.6 x 10(-6)-13.33 x 10(-6) M) reduces the binding of Th. Scatchard plot analysis data suggest that this inhibitory effect of THC may arise from an allosteric change in the conformation of the Th binding sites not affecting the binding affinity of Th. Abrogation of the THC-induced inhibition of Th binding to control membranes after solubilization and restoration of the inhibitory effect of THC on Th binding in reconstituted membranes suggest the involvement of membrane lipid in the THC-induced inhibition of Th binding to neuronal and non-neuronal membranes.
Department of Biochemistry, University College of Science, University of Calcutta, India.
S K
SK
Ghosh
M K
MK
Poddar
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D013759:Dronabinol / Q000494:pharmacology*; D007425:Intracellular Membranes / Q000378:metabolism; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008563:Membrane Lipids / Q000378:metabolism; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D051381:Rats; D013806:Theophylline / Q000378:metabolism*
D008563:Membrane Lipids; D013759:Dronabinol; D013806:Theophylline