Binding selectivity of short [D-Arg2,Leu5]enkephalin analogues to mu- and delta-subclasses of opiate receptors.
[D-Arg2,Leu5]enkephalin and its analogues, shortened from the C-terminus, were studied in a rat brain membrane fraction with the aid of radioreceptor analysis. The interaction between these compounds and the peripheral opiate receptors of isolated organs (guinea pig ileum and mouse vas deferens) was also investigated. The ethyl ester of the [D-Arg2]tripeptide retains approximately 10% of the mu-receptor activity of leucine-enkephalin. This implies that for interaction with the mu-subclass of opiate receptors there is no requirement for a second aromatic ring in addition to the tyramine group in the minimal active moiety of the enkephalin molecule.
Rosenthal
G F
GF
Institute of Organic Synthesis, Latvian Academy of Sciences, Riga, USSR.
Inkina
N M
NM
Abissova
N A
NA
Bobrova
I V
IV
Chipens
G I
GI
D000595:Amino Acid Sequence; D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives* / Q000378:metabolism; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism; D008297:Male; D051379:Mice; D008969:Molecular Sequence Data; D011485:Protein Binding; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000378:metabolism
D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D004743:Enkephalin, Leucine; C066412:enkephalin, Arg(2)-Leu(5)-