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Prospects for LHRH analogs as contraceptives

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LHRH and Its Analogs

Part of the book series: Advances in Reproductive Health Care ((ARHE,volume 1))

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Abstract

Chemical modifications to the LHRH structure have resulted in highly active agonists and several such compounds, e.g. [d-Ser(tBu)6,Pro9 -NHEt]LHRH, [d-Trp6,Pro9 -NHEt]LHRH and [d-Nal(2)6]6]LHRH have been studied clinically. Highly active antagonists were discovered more recently, e.g. [Ac_d-pC1_Phe1,d-pC1_Phe2,d-Trp3,d-Arg6,d-Ala10]LHRH and [N-Ac-d- Nal(2)1,d-pF-Phe2,d-Trp3,d-Arg6]LHRH, but these are only just reaching the stage of clinical trial. There are now available sufficiently potent analogs of both types for adequate testing as contraceptive agents. There is still scope for improvement in design, e.g. increased resistance to metabolism and hence prolonged in vivo bioactivity may be possible. More potent compounds may be discovered, but their mode of action probably will be the same as those already described. LHRH analogs have proved non-toxic, despite their interference with endocrinological control mechanisms. It is possible to evaluate the potential of these compounds for contraception. Already certain trends are clear. Although there was hope that LHRH analogs might be contraceptive by several mechanisms (e.g. luteolytic, abortifacient and defective luteal phase), present evidence suggests that only inhibition of ovulation in the female and inhibition of spermatogenesis in the male will be effective. Even in the modalities where contraception may be achieved, it will probably be necessary to use steroids – progestins in the female and androgens in the male – as adjuncts to LHRH analog treatment.

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  1. M. J. K. Harper
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B. H. Vickery J. J. Nestor Jr. E. S. E. Hafez

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© 1984 MTP Press Limited

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Harper, M.J.K. (1984). Prospects for LHRH analogs as contraceptives. In: Vickery, B.H., Nestor, J.J., Hafez, E.S.E. (eds) LHRH and Its Analogs. Advances in Reproductive Health Care, vol 1. Springer, Dordrecht. https://doi.org/10.1007/978-94-009-5588-2_34

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  • DOI: https://doi.org/10.1007/978-94-009-5588-2_34

  • Publisher Name: Springer, Dordrecht

  • Print ISBN: 978-94-010-8963-0

  • Online ISBN: 978-94-009-5588-2

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