SYNTHESIS AND BIOLOGICAL ACTIVITY OF POSITION 1 ANALOGS OF LH‐RH

Karoly NikolicS, David H. Coy, Jesus A. Vilchez‐Martinez, Esther J. Coy, Andrew V. Schally

Research output: Contribution to journalArticlepeer-review

9 Scopus citations

Abstract

(Formyl-sarcosine) 1-LH-RH (I), (acetyl-sarcosine) 1-LH-RH (II), (2-pyrrolidone-4-carboxylic acid) 1-LH-RH (III), (N-methyl-2-pyrrolidone-4-carboxylic acid) 1-LH-RH (IV), hydroxyproline 1-LH-RH (V) and (cyclopentane-carboxylic acid) 1-LH-RH (VI) were synthesized by solid phase methods on a benzhydrylamine resin support. Peptides I-IV were assayed for LH- and FSH-releasing activity over a 4-h period after subcutaneous injection into immature male rats in order to detect any prolongation of activity. The peptides were found to have the following integrated LH-releasing activities compared with LH-RH: I, 64%; II, 72%; III, 19%; IV, 58%. None of the peptides were found to be longer acting than LH-RH. Peptides V and VI were far less active, 0.001% and 1.4%, respectively.

Original languageEnglish (US)
Pages (from-to)57-62
Number of pages6
JournalInternational journal of peptide and protein research
Volume9
Issue number1
DOIs
StatePublished - Jan 1977
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry

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