A new category of ovulation inhibitors: linear LH-RH analogues having more than ten residues. |
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Authors: | T Wasiak J Humphries K Folkers C Y Bowers |
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Affiliation: | Institute for Biomedical Research The University of Texas at Austin Austin, Texas 78712 USA;Tulane University School of Medicine New Orleans, Louisiana 70112 USA |
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Abstract: | A linear analogue of the luteinizing hormone-releasing hormone, longer than a decapeptide, is described for the first time, which is equivalent in potency to the best known inhibitors of ovulation, and which constitutes an important new lead to the design of inhibitors of even greater potency. At a dosage of 200 μg/rat, the undecapeptide [(1, -Phe2, -Trp3, -Trp6]-LH-RH caused 100% inhibition of ovulation. The related analogues, [(1, -Phe2, -Trp3, -Trp6]-LH-RH and [(Gly-Pro)1, -Phe2, -Trp3, -Trp6]-LH-RH, were less active, . All of these undecapeptides inhibited the action of 0.6 ng/ml of LH-RH by greater than 50% at the very low level of 10 ng/ml. |
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