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

Autor: David H. Coy, Andrew V. Schally, Jesus A. Vilchez-Martinez, Esther J. Coy, Karoly Nikolics
Rok vydání: 2009
Předmět:
Zdroj: International Journal of Peptide and Protein Research. 9:57-62
ISSN: 0367-8377
DOI: 10.1111/j.1399-3011.1977.tb01837.x
Popis: (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, hydroxyproline1-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.
Databáze: OpenAIRE