Enkephalin analogs containing the dipeptide unit Tyr-Arg (kyotorphin).
- 1 January 1980
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 28 (9) , 2580-2586
- https://doi.org/10.1248/cpb.28.2580
Abstract
Eight Met- and Leu-enkephalin analogs substituted with L- or D-Arg at position 2 were synthesized using NG-mesitylene-2-sulfonylarginine. Among them, H-Tyr-D-Arg-Gly-Phe-Met-OH was found to possess an analgesic effect 2.4 times higher than that of morphine on a molar basis, when injected intracisternally. This compound was also found to produce analgesia when administered intravenously.Keywords
This publication has 3 references indexed in Scilit:
- Studies on peptides. XCIV. Synthesis and activity of kyotorphin and its analogs.CHEMICAL & PHARMACEUTICAL BULLETIN, 1980
- Potent analgesic activity of the enkephalin-like tetrapeptide H-Tyr-D-Ala-Gly-Phe-NH2Life Sciences, 1978
- Enhanced analgesic activity of D-Ala2 enkephalinamides following D-isomer substitutions at position fiveLife Sciences, 1978