Endorphin: Synthesis and properties of double-headed and related analogs (original) (raw)
International Journal of Peptide and Protein Research, 2009
Abstract
A double-headed analog of human β-endorphin (βh-EP), N, N'-bis (β-endorphinyl)-cystine (II), has been synthesized by the solid-phase method, along with βh-EP-Cys(CH2CONH2)-OH (I) and (Tyr31]-βh-EP (III). Their relative potencies in a radioreceptor-binding assay were: Bh-EP, 100; II, 235; I, 170; and III, 204. In the tail-flick test for analgesic activity their relative potencies were: βhEP, 100; II, 86; I, 93; and III, 116.
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