Sandbox Reserved 1646: Difference between revisions
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==Gonadotrophin releasing hormone== | ==Gonadotrophin releasing hormone== | ||
===Hormone=== | |||
GnRH is a decapeptid that was isolated and characterised by the groups of A V Schally and R C L Guillemin, the 1977 Nobel laureates. | GnRH is a decapeptid that was isolated and characterised by the groups of A V Schally and R C L Guillemin, the 1977 Nobel laureates. | ||
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In most vertebrates there are at least two, and usually three, forms of GnRH. In mammals, there are two forms, GnRH I which regulates gonadotropin and GnRH II which appears to be a neuromodulator and stimulates sexual behaviour. | In most vertebrates there are at least two, and usually three, forms of GnRH. In mammals, there are two forms, GnRH I which regulates gonadotropin and GnRH II which appears to be a neuromodulator and stimulates sexual behaviour. | ||
=== | ===Antagonist=== | ||
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 | |||
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. | |||
== Disease == | == Disease == | ||
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GnRH agonists and antagonists also have promise as novel contraceptives. Indeed, concerning animals, the GnRH receptor could be a good target for contraception with a DNA vaccine <ref>DOI: 10.1007/s12033-018-0137-9</ref> | GnRH agonists and antagonists also have promise as novel contraceptives. Indeed, concerning animals, the GnRH receptor could be a good target for contraception with a DNA vaccine <ref>DOI: 10.1007/s12033-018-0137-9</ref> | ||
Besides, on pharmacological grounds the primary indications for GnRH antagonists will be in any situation in which chemical gonadotropic hypophysectomy is required. | |||
<scene name='86/868179/Test1/1'>Test</scene> | <scene name='86/868179/Test1/1'>Test</scene> | ||
