Tobacco mosaic virus-enkephalin conjugates: potentiation of opioid activity.
Covalent tobacco mosaic virus-enkephalin analogue conjugates containing between 5 and 450 agonist molecules attached through their C-terminal amino acids were prepared and assayed in pharmacological and binding assays that distinguish between mu- and delta-receptors. Increases in peptide- and receptor-specific potency and affinity were observed with a certain preference of mu- over delta-receptors. The results may become important for mapping receptors or for isolating opiate receptor-bearing membrane vesicles.
D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D004090:Dihydromorphine / Q000378:metabolism; D004357:Drug Synergism; D004723:Endorphins / Q000494:pharmacology*; D004745:Enkephalins / Q000494:pharmacology*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D009197:Myenteric Plexus / Q000187:drug effects; D011957:Receptors, Opioid / Q000378:metabolism; D013329:Structure-Activity Relationship; D014027:Tobacco Mosaic Virus; D014649:Vas Deferens / Q000187:drug effects
D004723:Endorphins; D004745:Enkephalins; D011957:Receptors, Opioid; D004090:Dihydromorphine