Spin-labeled narcotics
Wu, W.Y.; Abood, L.G.; Gates, M.; Kreilick, R.W.
Molecular Pharmacology 13(4): 766-773
1977
ISSN/ISBN: 0026-895X PMID: 196177 Document Number: 111682
A series of spin-labeled derivatives of morphine and codeine were synthesized, and ESR spectroscopy was used to examine some molecular interactions. Animal studies were conducted to determine the relative analgesic potencies of these drugs. One of the spin-labeled drugs was isolated from rat brains, and ESR showed that enzymatic hydrolysis of the drug was a relatively slow process. The pharmacological effects of these drugs were due to the spin-labeled molecules and not to a hydrolysis product (morphine or codeine). ESR was used to demonstrate that spin-labeled drugs bind to isolated synaptic membrane preparations. ESR is a valuable tool for the study of the interaction of spin-labeled analgesic drugs with membranes.