PMID: 2109164Jan 1, 1990Paper

Evaluation of in vivo [corrected] biological activity of new agmatine analogs of growth hormone-releasing hormone (GH-RH)

Life Sciences
L BokserA V Schally

Abstract

The effects of agmatine analogs of growth hormone releasing hormone (GH-RH) were compared to GH-RH(1-29)-NH2 after intravenous (iv) and subcutaneous (sc) administration to pentobarbital-anesthetized male rats. After the iv injection, the analogs [desNH2-Tyr1,Ala15,Nle27] GH-RH(1-28)Agm (MZ-2-51); [desNH2-Tyr1,D-Lys12,Ala15,Nle27] GH-RH(1-28)Agm (MZ-2-57); [desNH2-Tyr1,Ala15,D-Lys21,Nle27] GH-RH(1-28)Agm (MZ-2-75) and [desNH2-Tyr1, D-Lys12,21, Ala15, Nle27] GH-RH(1-28)Agm (MZ-2-87) showed a potency equivalent to 4.4, 1.9, 1.07 and 1.03 times that of GH-RH (1-29)-NH2, respectively, at 5 min and 5.6, 1.8, 1.9 and 1.8 times higher, respectively, at 15 min. After sc administration, analogs MZ-2-51, MZ-2-57 and MZ-2-75 showed to be 34.3, 14.3 and 10.5 times more potent than the parent hormone at 15 min and 179.1, 88.9 and 45.0 times more active, respectively, at 30 min. In addition, MZ-2-51 had prolonged GH-releasing activity as compared to the standard. We also compared the activity of MZ-2-51 and MZ-2-57 with their homologous L-Arg and D-Arg analogs [desNH2-Tyr1,Ala15,Nle27] GH-RH(1-29)-NH2 (MZ-2-117), [des-NH2Tyr1,D-Lys12, Ala15, Nle27] GH-RH(1-29)NH2 (MZ-2-123) and [desNH2-Tyr1,D-Lys12,Ala15, Nle27,D-Arg29] GH-RH(1-29)NH2 (MZ-2-1...Continue Reading

References

Mar 1, 1989·Journal of Reproduction and Fertility·L BokserA V Schally
Aug 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·M Mason-GarciaA V Schally
Feb 1, 1985·Journal of Medicinal Chemistry·D H CoyV A Lance
Feb 29, 1984·Biochemical and Biophysical Research Communications·V A LanceD H Coy
Sep 1, 1983·The Journal of Clinical Endocrinology and Metabolism·M C GelatoG R Merriam
Sep 15, 1983·Biochemical and Biophysical Research Communications·W B Wehrenberg, N Ling
Apr 1, 1984·Proceedings of the Society for Experimental Biology and Medicine·R GuilleminW B Wehrenberg
Nov 30, 1982·Biochemical and Biophysical Research Communications·W B WehrenbergR Guillemin

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Citations

Mar 1, 1992·International Journal of Peptide and Protein Research·M ZarandiA V Schally
Feb 1, 1993·International Journal of Peptide and Protein Research·K GrootA V Schally
Dec 1, 1990·International Journal of Peptide and Protein Research·M ZarandiA V Schally

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