Abstract
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 language | English (US) |
|---|---|
| Pages (from-to) | 325-328 |
| Number of pages | 4 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 20 |
| Issue number | 3 |
| DOIs | |
| State | Published - Mar 1 1977 |
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Li, C. H., Yamashiro, D., Tseng, L. F., & Loh, H. H. (1977). Synthesis and Analgesic Activity of Human β-Endorphin. Journal of Medicinal Chemistry, 20(3), 325-328. https://doi.org/10.1021/jm00213a001