Molecular mechanisms of ligand binding to opioid receptors: selective inhibition by ethanol?
Effects of varying concentrations of ethanol on the conformations of DAGO, a mu-specific opioid ligand were monitored by FT-IR spectroscopy. The binding of 3H-labeled DAGO (mu-agonist) and DSLET (delta-agonist) to opioid receptors in the presence of varying concentrations of alcohol was also determined. The results indicate that the conformational features of the ligands are altered and conformational factors may play a role in ligand-receptor interaction.
Rapaka
R S
RS
Division of Preclinical Research, National Institute on Drug Abuse, Rockville, MD 20857.
Bhargava
H N
HN
Renugopalakrishnan
V
V
Collins
B J
BJ
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives*; D004745:Enkephalins / Q000378:metabolism; D000431:Ethanol / Q000494:pharmacology*; D009842:Oligopeptides / Q000378:metabolism; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D013055:Spectrophotometry, Infrared
D004745:Enkephalins; D009842:Oligopeptides; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D000431:Ethanol; D004743:Enkephalin, Leucine; C034318:enkephalin, Ser(2), Leu(5), Thr(6)-