Synthesis and Biological Evaluation of LH and FSH Releasing Hormone and Its Analogs

Noboru Yanaihara, Chizuko Yanaihara, Masanori Sakagami, Kazuyasu Tsuji, Tadashi Hashimoto, Toshio Kaneko, Hiroshi Oka, Andrew V. Schally, Akira Arimura, Tommie W. Redding

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

Details and additional information about another synthesis of LH-RH/FSH-RH, pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 (I), are described. In order to obtain enough highly purified material, the synthesis was performed by stepwise elongation according to the conventional method for peptide synthesis. The product was purified effectively by column chromatography on CM-Sephadex C-25. Homogeneity of the purified product was confirmed by tlc as well as by elementary analysis and acid and enzyme hydrolyses. The in vivo and in vitro activities of the synthetic LH-RH/FSH-RH (I) were of the same order of magnitude as those of pure natural LH-RH/FSH-RH. On the other hand, nonapeptide amide, des-pGlu1-LH-RH/FSH-RH (II), and octapeptide amide, des-pGlu1-des-His2-LH-RH/FSH-RH (III), were, at best, only very weakly active. In addition, I stimulated cyclic AMP formation in rat anterior pituitary, while II and III exhibited no stimulation.

Original languageEnglish (US)
Pages (from-to)373-377
Number of pages5
JournalJournal of Medicinal Chemistry
Volume16
Issue number4
DOIs
StatePublished - Apr 1 1973
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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