Sandbox Reserved 1646: Difference between revisions
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Like GnRH, peptide antagonists of the GnRH receptor are decapeptides, but with 50–70% of amino acids substituted , and they exhibit classical competitive antagonism ; | Like GnRH, peptide antagonists of the GnRH receptor are decapeptides, but with 50–70% of amino acids substituted , and they exhibit classical competitive antagonism ; | ||
Blockade of GnRH effects may be wanted for a variety of reasons—eg, to prevent untimely luteinisation during assisted reproduction or in the treatment of sex-hormone-dependent disorders | Blockade of GnRH effects may be wanted for a variety of reasons—eg, to prevent untimely luteinisation during assisted reproduction or in the treatment of sex-hormone-dependent disorders | ||
Unlike the agonists, GnRH antagonists do not induce an initial stimulation of gonadotropin release, but cause an immediate and rapid, reversible suppression of gonadotropin secretion. The principal mechanism of action of GnRH antagonists is competitive receptor occupancy of GnRH-r. | Unlike the agonists, GnRH antagonists do not induce an initial stimulation of gonadotropin release, but cause an immediate and rapid, reversible suppression of gonadotropin secretion. The principal mechanism of action of GnRH antagonists is competitive receptor occupancy of GnRH-r. <ref>DOI: 10.1016/S0140-6736(01)06797-6</ref> | ||
== Disease == | == Disease == | ||
