An in vivo assay for anti-LH-RH and anti-FSH-RH activity of inhibitory analogues of LH-RH

Jesus A. Vilchez-Martinez, Andrew V. Schally, David H. Coy, Esther J. Coy, Clinton M. Miller, Akira Arimura

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19 Scopus citations

Abstract

A convenient and sensitive method for testing anti LH and FSH releasing activities of antagonists of LH RH was devised. The peptides tested were injected subcutaneously together with synthetic LH releasing hormone (LH RH) in immature male rats. Serum LH and FSH concentrations were measured 30 min later by radioimmunoassay. In this system, (DesHis 2) LH RH failed to block the pituitary response to LH RH in agreement with previous data. The administration of [DesHis 2, desGly 10] LH RH ethylamide, [DesHis 2, Leu 3, desGly 10 LH RH ethylamide, [DesHis 2, D Ala 6, desGly 10] LH RH ethylamide, and [DesHis 2, D Ala 6] LH RH in doses of 200 μg/rat, and [DesHis 2, Leu 3, D Ala 6, desGly 10] LH RH ethylamide in doses ranging from 100-400 μg/rat caused a significant inhibition of LH RH induced release of LH and FSH. On the other hand, [DesHis 2, desGly 10] LH RH propylamide, and [Leu 2, Leu 3, D Ala 6, desGly 10] LH RH ethylamide failed to block the response to LH RH. Among the peptides tested, [DesHis 2, D Ala 6, desGly 10] LH RH ethylamide, [Leu 4, Leu 3, D Ala 6, des Gly 10] LH RH ethylamide in doses of 200 μg and [DesHis 2, Leu 3, D Ala 6, desGly 10] LH RH ethylamide in a dose of 400 μg/rat showed some intrinsic LH and FSH releasing activities. The method described is simple and convenient for studying the anti LH RH release activity of inhibitory analogues of LH RH, and also enabled the demonstration of an in vivo inhibition of FSH release by these analogues.

Original languageEnglish (US)
Pages (from-to)1130-1134
Number of pages5
JournalEndocrinology
Volume96
Issue number5
DOIs
StatePublished - May 1975

ASJC Scopus subject areas

  • Endocrinology

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    Vilchez-Martinez, J. A., Schally, A. V., Coy, D. H., Coy, E. J., Miller, C. M., & Arimura, A. (1975). An in vivo assay for anti-LH-RH and anti-FSH-RH activity of inhibitory analogues of LH-RH. Endocrinology, 96(5), 1130-1134. https://doi.org/10.1210/endo-96-5-1130