Inhibition of preovulatory gonadotropin secretion in the rhesus monkey by [(&lt;Glu-Pro)1,D-Phe2,D-Trp3,6]-LHRH

Wilks, John W.; Folkers, Karl; Bowers, Cyril Y.; Humphries, John Eric; Schircks, Bernhard; Friebel, Klaus

doi:10.1016/s0010-7824(80)80009-6

Cited by 5 publications

(2 citation statements)

References 13 publications

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“…The testing of the anti-ovulatory properties of these antagonists in primates has been particularly frustrating. The timing of the LH surge cannot be accurately predicted as in the laboratory rat and administration of as much as 6 doses of 50 mg antagonist (<Glu-Pro'^-Pr^D-Trp^-GnRH) at 8-h intervals before the LH surge in rhesus monkeys had only limited success in preventing ovulation (Wilks et al, 1980 (Rivier et al, 1980) is awaited with interest. It will also be important to determine whether the corpus luteum could be a target for these GnRH antagonists, and whether the powerful antagonists can exert any direct effects on the ovary.…”

Section: Gnrh Antagonistsmentioning

confidence: 99%

Antifertility effects of GnRH

Fraser¹

1982

Reproduction

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Section: Gnrh Antagonistsmentioning

confidence: 99%

Antifertility effects of GnRH

Fraser¹

1982

Reproduction

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“…Since 1973, these research groups have made stepwise progress in the design and synthesis of antagonists, and it was found that exemplary antagonists do show antiovulatory activity in a primate [3], as well as in the rat models.…”

Section: Introductionmentioning

confidence: 99%

Antiovulatory Potency and Conformation of an Antagonist of the Luteinizing Hormone-Releasing Hormone Having Six D-Amino Acids

Folkers

Bowers

Momany

et al. 1982

Zeitschrift Für Naturforschung B

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Abstract [N-Ac-Thr 1 ,D-Phe 2,D-Trp 3,6]-LHRH was the model antagonist of LHRH, which was the basis for tho design, synthesis and bioassay of seven peptides having four, five and six D-amino acids, which resulted from three single, three double, and one triple introductions of D-amino acids in positions 4, 5 and 8 of the model. Only the analog with six D-amino acids, [N-Ac-Thr 1,D-Phe 2 ,D-Trp 3,D-Ser 4, D-Tyr 5 ,D-Trp 6 ,D-Arg 8]-LHRH, had antiovulatory activity which was higher than that of the model antagonist, i.e., 70% antiovulatory activity at 25 μg/rat compared with 50% activity at 50 μg/rat, respectively. Empirical energy calculations gave a conformational structure for [N-Ac-Thr 1,D-Phe 2,D-Trp 3, D-Ser 4,D-Tyr 5,D-Arg 6,D-Arg 8]-LHRH which is similar to that calculated for previous potent antagonists. These results are a basis of new designs of antagonists having D-sub-stituents in up to ten positions toward effective inhibitors of ovulation by the parenteral and oral routes of administration.

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Fertility control

Harper

1982

Medicinal Research Reviews

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Inhibition of preovulatory gonadotropin secretion in the rhesus monkey by [(<Glu-Pro)1,D-Phe2,D-Trp3,6]-LHRH

Cited by 5 publications

References 13 publications

Antifertility effects of GnRH

Antifertility effects of GnRH

Antiovulatory Potency and Conformation of an Antagonist of the Luteinizing Hormone-Releasing Hormone Having Six D-Amino Acids

Fertility control

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