Synthesis and Analgesic Activity of Human β-Endorphin

Choh Hao Li, Donald Yamashiro, Liang Fu Tseng, Horace H. Loh

Research output: Contribution to journalArticlepeer-review

133 Scopus citations


The solid-phase synthesis of human β-endorphin is described. A yield of 32% is achieved based on starting resin. The synthetic product behaves as a homogeneous peptide in partition chromatography, paper electrophoresis, thin-layer chromatography, disc electrophoresis, amino acid composition, and a tryptic map. The synthetic βh-endorphin possesses antinociceptive properties as estimated by the tail-flick, hot-plate, and writhing tests in mice. When applied centrally, βh-endorphin is 17-48 times more potent than morphine. It is 3.4 times more potent than morphine when injected intravenously. The analgesic responses are blocked by the specific opiate antagonist, naloxone.

Original languageEnglish (US)
Pages (from-to)325-328
Number of pages4
JournalJournal of Medicinal Chemistry
Issue number3
StatePublished - Mar 1 1977


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