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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone and Men's Health Articles
GnRH: Physiological and pharmacological overview
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<blockquote data-quote="madman" data-source="post: 258387" data-attributes="member: 13851"><p><em>Gonadotropin-Releasing Hormone (GnRH) is a peptide controlling reproductive functions. It binds to GNRHR receptors and has diverse effects. GnRH plays a role in infertility, reproductive disorders, assisted reproduction technology, endometrium, ovary, prostate physiology, tumor transformation, neurogenesis, and neuroprotection. This review provides an overview of GnRH physiology and the pharmacological use of synthetic analogs in managing reproductive and non-reproductive diseases.</em></p><p></p><p></p><p></p><p></p><ul> <li data-xf-list-type="ul"><em>GnRH-I neurons in humans begin migration around gestational weeks 5-6 and approach the hypothalamic region by weeks 11-12</em></li> <li data-xf-list-type="ul"><em>Humans have a significantly higher number of GnRH immunoreactive neurons compared to rodents</em></li> <li data-xf-list-type="ul"><em>In the human fetal brain, there are about 10,000 GnRH neurons, with 2,000 located in the hypothalamus and 8,000 distributed in other brain areas</em></li> <li data-xf-list-type="ul"><em>GnRH-I neurons establish specific contacts with capillaries and form synaptic connections with various neuronal networks</em></li> <li data-xf-list-type="ul"><em>The activity of GnRH-I neurons is regulated by neurotransmitters, glial-derived growth factors, neuropeptides, genetic and/or epigenetic factors, and the hormonal milieu</em></li> </ul><p></p><p></p><p></p><p></p><p><strong>Key takeaways:</strong></p><p></p><p></p><ul> <li data-xf-list-type="ul"><em>GnRH is released in a pulsatile manner to synchronize gonadotropin secretion</em></li> <li data-xf-list-type="ul"><em>The GnRH neuronal network is active during late fetal maturation, early neonatal period, and puberty</em></li> <li data-xf-list-type="ul"><em>The release of GnRH is controlled by a complex neuronal network and peripheral signals</em></li> <li data-xf-list-type="ul"><em>Various factors, such as kisspeptin, norepinephrine, neuropeptide Y, estrogens, opioids, interleukin-1, progesterone, and androgens, modulate GnRH secretion</em></li> <li data-xf-list-type="ul"><em>GnRH may regulate its own secretion through a feedback loop on hypothalamic neurons</em></li> <li data-xf-list-type="ul"><em>In humans, GnRH cannot be accurately measured in peripheral blood but can be inferred through plasma LH or FAS measurement</em></li> <li data-xf-list-type="ul"><em>GnRH pulses occur approximately every 120 minutes in adult males</em></li> <li data-xf-list-type="ul"><em>The pattern of pulsatile GnRH release in women varies during reproductive stages and the ovulatory cycle</em></li> </ul><p></p><p></p><p></p><p><strong>Key takeaways:</strong></p><p></p><p></p><ul> <li data-xf-list-type="ul"><em><em>GnRH regulates LH and FSH differently based on pituitary gonadotrope cells' decoding capacity</em></em></li> <li data-xf-list-type="ul"><em><em>Pulsatile GnRH release is necessary for the efficient activation of gonadotrope cells</em></em></li> <li data-xf-list-type="ul"><em><em>Continuous GnRH infusion suppresses LH and FSH release, causing a reversible shutdown of the reproductive axis</em></em></li> <li data-xf-list-type="ul"><em><em>GnRH receptor modulation plays a role in the dual effect of GnRH on gonadotrope cells</em></em></li> <li data-xf-list-type="ul"><em><em>Different G protein subunits are activated by rhythmic stimulation of pituitary GnRH receptors</em></em></li> <li data-xf-list-type="ul"><em><em>Intracellular signal cascades and transcription factors drive LH and FSH gene expression</em></em></li> <li data-xf-list-type="ul"><em><em>LH expression is induced by high-frequency GnRH pulses, while FSH expression is induced by low-frequency pulses</em></em></li> <li data-xf-list-type="ul"><em><em>Efficient therapeutic application of GnRH requires intermittent delivery, while continuous administration leads to "medical castration"</em></em></li> <li data-xf-list-type="ul"><em><em>Continuous GnRH exposure alters the fine-tuning control of gonadotropin synthesis and release</em></em></li> </ul><p></p><p></p><p></p><p><em><strong>GnRH analogs (agonists and antagonists) are widely used in therapeutic protocols to restore GnRH deficiency and suppress fertility. They are effective not only in reproductive disorders but also in treating cancer and neurological conditions. While new non-peptide analogs are being developed for improved patient compliance, further studies and characterization of these drugs will enhance their efficacy and delivery protocols.</strong></em></p></blockquote><p></p>
[QUOTE="madman, post: 258387, member: 13851"] [I]Gonadotropin-Releasing Hormone (GnRH) is a peptide controlling reproductive functions. It binds to GNRHR receptors and has diverse effects. GnRH plays a role in infertility, reproductive disorders, assisted reproduction technology, endometrium, ovary, prostate physiology, tumor transformation, neurogenesis, and neuroprotection. This review provides an overview of GnRH physiology and the pharmacological use of synthetic analogs in managing reproductive and non-reproductive diseases.[/I] [LIST] [*][I]GnRH-I neurons in humans begin migration around gestational weeks 5-6 and approach the hypothalamic region by weeks 11-12[/I] [*][I]Humans have a significantly higher number of GnRH immunoreactive neurons compared to rodents[/I] [*][I]In the human fetal brain, there are about 10,000 GnRH neurons, with 2,000 located in the hypothalamus and 8,000 distributed in other brain areas[/I] [*][I]GnRH-I neurons establish specific contacts with capillaries and form synaptic connections with various neuronal networks[/I] [*][I]The activity of GnRH-I neurons is regulated by neurotransmitters, glial-derived growth factors, neuropeptides, genetic and/or epigenetic factors, and the hormonal milieu[/I] [/LIST] [B]Key takeaways:[/B] [LIST] [*][I]GnRH is released in a pulsatile manner to synchronize gonadotropin secretion[/I] [*][I]The GnRH neuronal network is active during late fetal maturation, early neonatal period, and puberty[/I] [*][I]The release of GnRH is controlled by a complex neuronal network and peripheral signals[/I] [*][I]Various factors, such as kisspeptin, norepinephrine, neuropeptide Y, estrogens, opioids, interleukin-1, progesterone, and androgens, modulate GnRH secretion[/I] [*][I]GnRH may regulate its own secretion through a feedback loop on hypothalamic neurons[/I] [*][I]In humans, GnRH cannot be accurately measured in peripheral blood but can be inferred through plasma LH or FAS measurement[/I] [*][I]GnRH pulses occur approximately every 120 minutes in adult males[/I] [*][I]The pattern of pulsatile GnRH release in women varies during reproductive stages and the ovulatory cycle[/I] [/LIST] [B]Key takeaways:[/B] [LIST] [*][I][I]GnRH regulates LH and FSH differently based on pituitary gonadotrope cells' decoding capacity[/I][/I] [*][I][I]Pulsatile GnRH release is necessary for the efficient activation of gonadotrope cells[/I][/I] [*][I][I]Continuous GnRH infusion suppresses LH and FSH release, causing a reversible shutdown of the reproductive axis[/I][/I] [*][I][I]GnRH receptor modulation plays a role in the dual effect of GnRH on gonadotrope cells[/I][/I] [*][I][I]Different G protein subunits are activated by rhythmic stimulation of pituitary GnRH receptors[/I][/I] [*][I][I]Intracellular signal cascades and transcription factors drive LH and FSH gene expression[/I][/I] [*][I][I]LH expression is induced by high-frequency GnRH pulses, while FSH expression is induced by low-frequency pulses[/I][/I] [*][I][I]Efficient therapeutic application of GnRH requires intermittent delivery, while continuous administration leads to "medical castration"[/I][/I] [*][I][I]Continuous GnRH exposure alters the fine-tuning control of gonadotropin synthesis and release[/I][/I] [/LIST] [I][B]GnRH analogs (agonists and antagonists) are widely used in therapeutic protocols to restore GnRH deficiency and suppress fertility. They are effective not only in reproductive disorders but also in treating cancer and neurological conditions. While new non-peptide analogs are being developed for improved patient compliance, further studies and characterization of these drugs will enhance their efficacy and delivery protocols.[/B][/I] [/QUOTE]
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Testosterone Replacement, Low T, HCG, & Beyond
Testosterone and Men's Health Articles
GnRH: Physiological and pharmacological overview
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