I see gonadotropin-releasing hormone (GnRH) as a replacement for anti-androgens, yup!, you won't need them if the pituitary suppresses the release of lutenizng hormone LH, and FSH follicle stimulating hormone. In this case, the use of GnRH antagonists effectively shuts testosterone production in the testes/adrenals off, thus eliminating the need for AA's, this leaves estrogen unopposed, and reducing the need for increased amounts of supplements sparing the endocrine system.
So, we be looking (lol, sending out a
bolo) for a plant origin non-peptide orally-active GnRH antagonists, easy huh?.
Unlike the
GnRH agonists, which cause an initial stimulation of the hypothalamic-pituitary-gonadal axis (HPGA), leading to a surge in testosterone or estrogen levels,
GnRH antagonists have an immediate onset of action, rapidly reducing sex hormone levels without an initial surge.
source:wiki
Progress towards the development of non-peptide orally-active gonadotropin-releasing hormone (GnRH) antagonists: therapeutic implications.
Review article
Millar RP, et al. Br Med Bull. 2000.
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Abstract
Gonadotropin-releasing hormone (GnRH) is a decapeptide (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly.NH2) which is produced from a precursor polypeptide in hypothalamic neurons and secreted in a pulsatile fashion to stimulate the secretion of LH and FSH via its interaction with a cognate receptor on gonadotropes. Low doses of the native peptide delivered in a pulsatile manner to mimic that found in the hypothalamic portal vessels restore fertility in hypogonadal patients, and are also effective in treating cryptorchidism and delayed puberty. Administration of high doses of GnRH, or agonist analogues, causes desensitization of the gonadotrope with consequent decline in gonadal gametogenesis and steroid and peptide hormone synthesis. This phenomenon finds extensive therapeutic application in clinical medicine in a wide spectrum of disease (Table 1). In addition, GnRH analogues have promise as new generation male and female contraceptives in conjunction with steroid hormone replacement.
GnRH antagonists inhibit the reproductive system through competition with endogenous GnRH for the receptor and, in view of their rapid effects, are being increasingly used for the above mentioned applications. The peptide agonists and antagonists currently available require parenteral administration, typically in the form of long-acting depots.
A new generation of non-peptide GnRH antagonists are beginning to emerge which should allow oral administration and, therefore, may provide greater flexibility of dosing, lower costs and increased patient acceptance.
