Effects of structurally different (Leu5) enkephalinamides on electrically-evoked contractions of guinea pig ileum.
The incorporation of D-Leu5 and the substitution of L-Gly2 by D-Ala2 into (Leu5)enkephalinamide, using direct coupling of enzymatic and azide methods for peptide bond formation, increased the relative potency of (Leu5)enkephalinamides to inhibit the electrically-evoked contractions of guinea pig ileum, probably activating a delta-type opiate receptor.
Radomirov
R
R
Department of Experimental Pharmacology, Bulgarian Academy of Sciences, Sofia.
Petkov
V D
VD
Venkova
K
K
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004558:Electric Stimulation; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000494:pharmacology*; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives*; D005069:Evaluation Studies as Topic; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects*; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology; D013329:Structure-Activity Relationship
D011957:Receptors, Opioid; D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine; C030279:enkephalinamide-Leu, Ala(2)-