Synthesis and biological properties of [Leu-6]-LH-RH and [D-leu-6,desGly-NH 210]-LH-RH ethylamide

[Leu 6,desGly-NH 2 10]-LH-RH ethylamide and [Leu 6]-LH-RH, two analogs of LH-RH, were prepared by the solid phase method. LH- and FSH-releasing activity of these peptides was assayed against LH-RH by subcutaneous administration in immature male rats. When the integrated levels of LH and FSH over a 6...

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Veröffentlicht in:	Biochemical and biophysical research communications 1974-08, Vol.59 (4), p.1226-1232
Hauptverfasser:	Vilchez-Martinez, Jesus A., Coy, David H., Arimura, Akira, Coy, Esther J., Hirotsu, Yoshihiro, Schally, Andrew V.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides Amino Acids - analysis Animals Biological Assay Chromatography, Gel Chromatography, Thin Layer Follicle Stimulating Hormone - blood Glycine Gonadotropin-Releasing Hormone - analogs & derivatives Gonadotropin-Releasing Hormone - chemical synthesis Gonadotropin-Releasing Hormone - pharmacology Leucine Luteinizing Hormone - blood Male Optical Rotation Pituitary Gland - drug effects Rats Structure-Activity Relationship Time Factors
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Zusammenfassung:	[Leu 6,desGly-NH 2 10]-LH-RH ethylamide and [Leu 6]-LH-RH, two analogs of LH-RH, were prepared by the solid phase method. LH- and FSH-releasing activity of these peptides was assayed against LH-RH by subcutaneous administration in immature male rats. When the integrated levels of LH and FSH over a 6 hr period after the injection were used as parameter of the LH- and FSH-releasing activities, the [Leu 6]-LH-RH showed LH-releasing activity of 9 times and FSH-releasing activity of 5 times greater than that of LH-RH. [Leu 6,desGly-NH 2 10]-LH-RH ethylamide showed LH- and FSH-releasing activities of 53.6 and 14.5 times greater, respectively, than that of LH-RH.
ISSN:	0006-291X 1090-2104
DOI:	10.1016/0006-291X(74)90445-8