Beta-Endorphin. Synthesis and properties of double-headed and related analogs.
A double-headed analog of human beta-endorphin (betah-EP), N,N'-bis (beta-endorphinyl)-cystine (II), has been synthesized by the solid-phase method, along with betah-EP-Cys(CH2CONH2)-OH (I) and [Tyr31]-betah-EP (III). Their relative potencies in a radioreceptor-binding assay were: betah-EP, 100; II, 235; I, 170; and III, 204. In the tail-flick test for analgesic activity their relative potencies were: betah-EP, 100; II, 86; I, 93; and III, 116.
D000595:Amino Acid Sequence; D000818:Animals; D001681:Biological Assay; D001921:Brain / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D004723:Endorphins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008722:Methods; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism; D013329:Structure-Activity Relationship; D001615:beta-Endorphin
D004723:Endorphins; D007202:Indicators and Reagents; D011957:Receptors, Opioid; D001615:beta-Endorphin