Superiority of an antagonist of the luteinizing hormone releasing hormone with emphasis on arginine in position 8, named Argtide. |
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| Authors: | A Janecka A Ljungqvist C Bowers K Folkers |
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| Institution: | Institute for Biomedical Research, University of Texas, Austin 78712. |
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| Abstract: | In the research for more potent antagonists of the luteinizing hormone releasing hormone (LHRH), 13 new peptides with emphasis on arginine in position 8 were designed, synthesized and tested for anti-ovulatory activity (AOA). Two very potent analogs were achieved. N-Ac-D-3-Qal, D-pClPhe, D-3-Pal, Ser, cis-PzACA1a, D-PicLys, Leu, Arg, Pro, D-AlaNH2 showed 63% AOA at 0.125 microgram and 89% at 0.25 microgram, and an ED50 of 30.8 +/- 0.59 and presently may be the most promising antagonist reported. It is named Argtide. N-Ac-D-3-Qal, D-pClPhe, D-3-Pal, Ser, cis-PzACA1a, D-PicLys, Val, Arg, Pro, D-AlaNH2 showed 18% AOA at 0.125 microgram. Arg8 in antagonists may be significant for receptor binding. |
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