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Titlebook: LHRH and Its Analogs; Contraceptive and Th B. H. Vickery,J. J. Nestor,E. S. E. Hafez Book 1984 MTP Press Limited 1984 contraception.fertili

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Biological assays utilized to characterize LHRH and its analogsen shorter and the endpoints more easily determined. Although the number and variations of the assays used to evaluate LHRH analogs have proliferated, they can be conveniently divided for ease of review into . and . assays.
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Biological activity of a highly potent LHRH antagonist975). Developments in the antagonist field were therefore overshadowed when, starting in 1975, it was demonstrated that LHRH and its agonist analogs were capable of exerting ‘paradoxical’ antireproductive effects in doses of 0.5 .g per day or less (Oshima .., 1975).
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Development of agonistic LHRH analogse molecule required for action and at the synthesis of analogs with increased potency and prolonged action. This historical review outlines the development of the synthesis programs which have produced the highly potent LHRH agonistic analogs now under clinical development. Other detailed reviews are available (Schally .., 1981; Corbin, 1982).
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LHRH agonists and antagonists containing very hydrophobic amino acids) and gonads (Hsueh and Erickson, 1979) upon prolonged treatment has caused increased interest in their potential as contraceptive and as anti-steroidal therapeutic agents (Corbin and Beattie, 1975; Vickery, 1981). The most potent agonists can block estrous cyclicity in the rat with doses less than 0.1 .g twice daily (Nestor .., 1982.).
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Direct antigonadal actions of LHRHHRH as an ovulation-inducing agent in anovulatory women have been only partially successful. Similarly, the early use of LHRH and LHRH agonists in the therapy of hypogonadotropic hypogonadism in men resulted in only limited success, and actual decreases in testicular steroidogenesis were reported.
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LHRH antagonists in femalespotency in males (Rabin .., 1981). Low doses of steroids are given concurrently in some trials (Heber and Swerdloff, 1980). The necessity for frequent administration and for steroid replacement may negate the clinical usefulness of the agonists.
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