Next Article in Journal
Five- and Six-Membered Nitrogen-Containing Compounds as Selective Carbonic Anhydrase Activators
Previous Article in Journal
One-Pot Lipase-Catalyzed Enantioselective Synthesis of (R)-(−)-N-Benzyl-3-(benzylamino)butanamide: The Effect of Solvent Polarity on Enantioselectivity
Article Menu
Issue 12 (December) cover image

Export Article

Open AccessReview
Molecules 2017, 22(12), 2188;

Recent Development of Non-Peptide GnRH Antagonists

School of Pharmacy, University of Oslo, 0316 Oslo, Norway
Norsk Medisinsk Syklotronsenter AS, Postboks 4950 Nydalen, 0424 Oslo, Norway
Realomics SFI, Department of Chemistry, University of Oslo, 0316 Oslo, Norway
Department of neuropsychiatry and psychosomatic medicine, Oslo University Hospital, 4950 Oslo, Norway
Betanien Hospital, 3722 Skien, Norway
Author to whom correspondence should be addressed.
Received: 16 November 2017 / Revised: 4 December 2017 / Accepted: 4 December 2017 / Published: 9 December 2017
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [30932 KB, uploaded 14 December 2017]   |  


The decapeptide gonadotropin-releasing hormone, also referred to as luteinizing hormone-releasing hormone with the sequence (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) plays an important role in regulating the reproductive system. It stimulates differential release of the gonadotropins FSH and LH from pituitary tissue. To date, treatment of hormone-dependent diseases targeting the GnRH receptor, including peptide GnRH agonist and antagonists are now available on the market. The inherited issues associate with peptide agonists and antagonists have however, led to significant interest in developing orally active, small molecule, non-peptide antagonists. In this review, we will summarize all developed small molecule GnRH antagonists along with the most recent clinical data and therapeutic applications. View Full-Text
Keywords: GnRH receptor; non-peptide GnRH antagonist GnRH receptor; non-peptide GnRH antagonist

Scheme 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Tukun, F.-L.; Olberg, D.E.; Riss, P.J.; Haraldsen, I.; Kaass, A.; Klaveness, J. Recent Development of Non-Peptide GnRH Antagonists. Molecules 2017, 22, 2188.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top