Novel analogues of enkephalin: indentification of functional groups required for biological activity.
Novel tri- and tetrapeptide analogues of enkephalin, in conjunction with earlier structure-activity data, confirm that chemical substitutents present in the first and fourth residues of enkephalin are required for in vitro biological activity. A class of arylamino and alkylamino derivatized tripeptides also were found to have significant in vitro opioid-like activity indistinguishable from [D-Ala2,D-Leu5]enkephalin and morphine.
D000818:Animals; D001414:Bacitracin / Q000494:pharmacology; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004723:Endorphins / Q000138:chemical synthesis*; D004745:Enkephalins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009270:Naloxone / Q000378:metabolism; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism; D013329:Structure-Activity Relationship
D004723:Endorphins; D004745:Enkephalins; D011957:Receptors, Opioid; D001414:Bacitracin; D009270:Naloxone