Gonadotropin-releasing hormone modulator
| Gonadotropin-releasing hormone modulator | |
|---|---|
small-molecule (non-peptide) | |
| Legal status | |
| In Wikidata |
A GnRH modulator, or GnRH receptor modulator, also known as an LHRH modulator or LHRH receptor modulator, is a type of
, which are structurally distinct from and unrelated to GnRH analogues.GnRH modulators affect the
Shortly after the discovery of GnRH by
the receptor. Subsequent to the development and introduction of GnRH analogues, non-peptide or small-molecule GnRH modulators were developed and introduced.All GnRH modulators are contraindicated in pregnancy (pregnancy category X).
GnRH agonists
A gonadotropin-releasing hormone agonist (GnRH agonist) is a GnRH modulator that activates the GnRH receptor resulting in increased secretion of FSH and LH. Initially it was thought that GnRH agonists could be used as potent and prolonged stimulators of pituitary gonadotropin release, but it was soon recognized that GnRH agonists, after their initial stimulating action – termed a "flare" effect – eventually caused a paradoxical and sustained drop in gonadotropin secretion. This second effect was termed "downregulation" and can be observed after about 10 days. While this phase is reversible upon stopping the medication, it can be maintained when GnRH agonists use is continued for a long time. GnRH agonists can also be administered in a pulsatile manner through the use of a pump to produce a long-term stimulation of gonadotropin secretion, for instance to induce puberty.
Peptides (analogues)
GnRH antagonists
A gonadotropin-releasing hormone antagonist (GnRH antagonist) is a GnRH modulator that blocks the GnRH receptor resulting in an immediate drop in gonadotropin (FSH, LH) secretion. GnRH antagonists are primarily used in
Peptides (analogues)
Non-peptides (small-molecules)
a = Under development; not yet marketed.
See also
References
- PMID 23887363.
- ISBN 978-1-4419-8456-2.
External links