Prolonged Release of LH and FSH and Depletion of Pituitary Gonadotropin Content after Administration of [d-LEU6, desGly-NH210]-LH-RH Ethylamide

Abstract
LH [luteinizing hormone] and FSH [follicle-stimulating hormone] releasing activities of [D-Leu6, desGly-NH210]-LH-RH [luteinizing hormone-releasing hormone] ethylamide were examined using immature male rats. The gonadotropin release induced by various doses of [D-Leu6, desGlyNH210]-LH-RH ethylamide followed a different pattern than when LH-RH was given, reaching a peak at 2 h after injections, serum LH and FSH being still elevated at 4 h. The LH and FSH release induced by LH-RH reached a peak in 15 min and declined at 1 h. This provides further evidence that this analog is indeed long-acting. The LH-RH analog had a potency 20-60 times greater for LH release and 10-30 times higher for FSH release than LH-RH. [D-Leu6, desGly-NH210]-LH-RH ethylamide also caused a significant depletion of the pituitary gonadotropin content.