Synthetic pyridyl-alanyl decapeptides having antiovulatory activ

Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal

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2601125R, C07C10352

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active

045044147

ABSTRACT:
Pyridyl-alanyl decapeptides have been effectively synthesized and found to have antiovulatory activity. The exemplary [N-Ac-D-2-Nal.sup.1,pCl-D-Phe.sup.2, D-3-Pal.sup.3,D-Arg.sup.6,D-Ala.sup.10 ]-LHRH has very high potency to inhibit ovulation, both parenterally and orally. Also, this exemplary pyridyl-alanyl-decapeptide showed an unexpected prolonged duration of antiovulatory activity. Such pyridyl-alanyl-decapeptides are useful to control reproduction.

REFERENCES:
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Nestor et al., J. Med. Chem., 25, No. 7, 795-801 (1982).
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Nekola et al., Science, 218, 160-162 (1982).
Katzorke et al., Fertility and Sterility, vol. 36, 1981, p. 388, Contraceptic Effects of an Agonistic LH-RH Analog.
Asch, Fertility and Sterility, vol. 36, 1981, p. 388, Antiovulatory Activity of a Potent LH-RH Antagonistic Analogue (N-Ac-D-Trp.sup.1,3, D-p-Cl-Phe.sup.2, D-Phe.sup.6, D-Ala.sup.10) LH-RH (A-LH-RH).

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