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Comparative Study
. 1987 Oct 29;148(2):849-56.
doi: 10.1016/0006-291x(87)90953-3.

Design, synthesis and bioassays of antagonists of LHRH which have high antiovulatory activity and release negligible histamine

A Ljungqvist  1 , D M Feng, P F Tang, M Kubota, T Okamoto, Y W Zhang, C Y Bowers, W A Hook, K Folkers
Affiliations
Comparative Study

Design, synthesis and bioassays of antagonists of LHRH which have high antiovulatory activity and release negligible histamine

A Ljungqvist et al. Biochem Biophys Res Commun. .

Abstract

Potent antagonists of the luteinizing hormone releasing hormone have been achieved which release negligible histamine. [N-Ac-D-2-Nal1, D-pClPhe2, D-3-Pal3, NicLys5, D-NicLys6, ILys8, D-Ala10]-LHRH showed 100%AOA/1 microgram and 36%/0. 5 micrograms; ED50 greater than 300. [N-Ac-D-2-Nal1,D-pClPhe2,D-3-Pal3, PicLys5, D-PicLys6, ILys8, D-Ala10]-LHRH showed 100% AOA/0.5 micrograms and 40%/0.25 micrograms; ED50, 93 +/- 11, and is the most potent of 52 new peptides. These antagonists feature designs with weakly basic acylated D-Lys6, notably D-NicLys6 and D-PicLys6 and alkylated Lys8 or Orn8, e.g., ILys8 and IOrn8, and NicLys5 and PicLys5. Concepts included balanced overall basicity, superiority of ILys8 and IOrn8 which are sequence dependent and sensitivity of positions 5 and 6 for potency.

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