On the inhibitory effects of luteinizing hormone-releasing hormone analogs

Endocrinology
C Y BowersL E Reichert

Abstract

A detailed study of the activity of LHRH analog antagonists has been made in four assay systems which measure inhibition of the action of LHRH on isolated rat pituitaries in vitro, inhibition of the release of the LH induced by LHRH in vivo in adult male rats and adult male chimpanzees, and inhibition of spontaneous ovulation in cycling female rats. Only a partial correlation was observed between the in vitro and in vivo assays. Currently, the most potent LHRH analog antagonists in the present study were based on a 1,2,3,6-tetra-substituted LHRH sequence. The analogs [D less than Glu1,DPhe2,DTrp3,DTrp6]-LHRH, Ac-[Pro1,DPhe2,DTrp3,DTrp6]LHRH and [(Glu-Pro)1, dphe2,DTrp3,DTrp6]LHRH completely inhibited spontaneous ovulation in cycling rats at a dosage of 200 microgram/rat, sc. The most potent inhibitors of ovulation were always very potent in vitro, but other analogs having identical in vitro activities had little or no antiovulatory activity even at substantially higher dosages. The analogs inhibited the action of LHRH in the rat more easily than in the chimpanzee. Twelve of 13 analogs at the analog to LHRH ratio of 100:1 significantly inhibited the LH response, while only 5 of 9 of these same analogs inhibited the LH response i...Continue Reading

Citations

Dec 16, 1980·Biochemical and Biophysical Research Communications·A F SpatolaW W Vale
Oct 1, 1990·Journal of Inorganic Biochemistry·H KozlowskiA Walczewska-Sumorok
Feb 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·K FolkersM Kubota
Feb 12, 1998·Proceedings of the National Academy of Sciences of the United States of America·C VillalobosA Sánchez
Oct 18, 2006·Bioorganicheskaia khimiia·S V BurovM Fridkin
Jan 1, 1981·American Journal of Primatology·Charles E Graham

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