Details

Autor(en) / Beteiligte

• Folkers, K
• Bowers, C Y
• Shieh, H M
• Liu, Y Z
• Xiao, S B
• Tang, P F
• Chu, J Y

Titel

Antagonists of the luteinizing hormone releasing hormone (LHRH) with emphasis on the TRP7 of the salmon and chicken II LHRH's

Ist Teil von

• Biochemical and biophysical research communications, 1984-09, Vol.123 (3), p.1221-1226

Ort / Verlag

United States

Erscheinungsjahr

1984

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• The sequences of four naturally occurring luteinizing hormone releasing hormones (LHRH's) differ only in positions 5, 7 and 8. Salmon and chicken II LHRH's have Trp7; porcine/ovine (P/O) and chicken I LHRH's have Leu7. The receptor for P/O LHRH might effectively bind certain antagonists with Trp7. Thirteen antagonists having Trp7 and eight antagonists with other substitutions in position 7 were synthesized. One of the thirteen antagonists with the natural Trp7, [N-Ac-D-2-Nal1,D-pClPhe2,D-3-Pal3,D-Arg6,Trp7,D- Ala10]-LHRH, not only maintained activity, but had increased potency (ca. 58%; 90% antiovulatory activity/250 ng; rats) in comparison with the companion analog with the natural Leu7 of P/O LHRH. The other twelve Trp7-antagonists had lower potency.