| | 1 | Author
| Karl Folkers, CyrilY. Bowers, Yin-Zeng Liu, Xiao Shao-Bo, Hong-Ming Shieh, Chu Ji-Yu | Requires cookie* | | | Title
| Antagonists of the Luteinizing Hormone Releasing Hormone with Emphasis on Amino Acids in Position Five  | | | | Abstract
| Seventeen analogs of the luteinizing hormone releasing hormone (LHRH) have been syn-thesized, bioassayed, and compared for antiovulatory activity (AOA) in rats. The emphasis of design was replacement of Tyr 5 of LHRH. Position 5 has not been extensively studied. [N—Ac—D-2-Nal 1 , D-pClPhe 2 , D-3-Pal 3 , D-Arg 6 , D—Ala 10 ]-LHRH was the baseline for new designs. Comparison of the AOA's of the 17 analogs with the baseline revealed the two peptides with Phe 5 and 3-Pal 5 had equivalent AOA's, and were the best of the 17, and about 45% more potent than the baseline. Analogs with pClPhe 5 , oClPhe 5 , a-MepClPhe 5 , 2-Nal 5 , Trp 5 , and His 5 were less potent than the Phe 5 -and 3-Pal 5 -analogs. Based on the Phe 5 -analog, eight other analogs were synthesized with changes in positions 1, 2, 3 and 7 and although none were better than the baseline, 5/8 showed 20—60% AOA's at 250 ng and revealed optimum positions for new designs. | | | |
Reference
| Z. Naturforsch. 40b, 313—316 (1985); received August 20 1984 | | | |
Published
| 1985 | | | |
Keywords
| Peptide, Hormone, Ovulation, Luteinizing Hormone Releasing Hormone, Antagonist | | | |
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| default:Reihe_B/40/ZNB-1985-40b-0313.pdf | | | | Identifier
| ZNB-1985-40b-0313 | | | | Volume
| 40 | |
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