Kisspeptin-10 — Peptide Protocol Wiki reference

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Kisspeptin: HPG Axis Fertility Peptide Guide | Peptide Protocol Wiki Skip to main content 🧬 Peptide Protocol Wiki Peptides Side Effects New Learn Directory Tools Blog News About ⌘K ⌘K 🌱 New to Peptides? Start the 7-step beginner guide Peptides Side Effects New Directory Learn Tools Blog News About Kisspeptin 📋 Overview 🧬 Molecule 🔄 Similar ⚠️ Side Effects 💉 Dosing 🔬 Research 🚨 Risks 👥 Community 📊 Community Data Home Peptides Kisspeptin Hormonal Health Neuropeptides phase2 Kisspeptin Also known as: Kisspeptin-54, Kisspeptin-10, Metastin, KiSS-1 peptide Research compiled by Peptide Protocol Wiki 📅 Updated January 29, 2026 Citations Verified TL;DR Kisspeptin is a family of neuropeptides encoded by the KISS1 gene, acting as a master regulator of the hypothalamic-pituitary-gonadal (HPG) axis. It plays a critical role in puberty onset, reproductive function, and fertility through activation of the GPR54 (KISS1R) receptor.

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evidence_reference, safety_reference, dosing_reference, mechanism, contraindication_reference

Findings (92) · awaiting review (43)

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Puberty Regulation # Kisspeptin signaling is essential for the initiation of puberty.

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Not included in FDA compounding restrictions as of current information.

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Regulations vary by country and may change.

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mprehensive information on therapeutics, mechanisms, and safety.

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Additionally, the effects of kisspeptin on non-reproductive tissues expressing KISS1R, including the placenta, liver, and pancreas, du

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The receptor binds all kisspeptin isoforms through recognition of the conserved C-terminal RF-amide motif, with kisspeptin-10 being the minimal fragment required for full receptor activation.

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IP3 triggers calcium release from intracellular stores via IP3 receptors on the endoplasmic reticulum, while DAG activates protein kinase C (PKC).

safety · pending

dosing · pending

Start the 7-step beginner guide Peptides Side Effects New Directory Learn Tools Blog News About Kisspeptin 📋 Overview 🧬 Molecule 🔄 Similar ⚠️ Side Effects 💉 Dosing 🔬 Research 🚨 Risks 👥 Community 📊 Community Data Home Peptides Kisspeptin Hormonal Health Neuropeptides phase2 Kisspeptin Also known as: Kisspeptin-54, Kisspeptin-10, Metastin, KiSS-1 peptide Research compiled by Peptide Protocol Wiki 📅 Updated January 29, 2026 Citations Verified TL;DR Kisspeptin is a family of neuropeptides encoded by the KISS1 gene, acting as a master regulator of the hypothalamic-pituitary-gonadal (HPG) axis.

mechanism · pending

It plays a critical role in puberty onset, reproductive function, and fertility through activation of the GPR54 (KISS1R) receptor.

safety · pending

Browse all hormonal peptides → Table of Contents 📌 TL;DR • Master regulator of reproductive hormone axis • Phase 2 trials for IVF and fertility applications • Diagnostic tool for reproductive disorders • Potential treatment for hypogonadotropic hypogonadism Community-Reported Side Effects Anecdotal ?

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📋 Protocol Quick-Reference IVF oocyte maturation trigger with reduced OHSS risk, and HPG axis diagnostic testing 💉 Dosing

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Amount 9.6 nmol/kg SC (IVF trigger); 1 nmol/kg IV (diagnostic challenge) Frequency Single dose (IVF trigger); single dose (diagnostic) Duration Single administration per IVF cycle 💊 Administration Route SC Schedule Single dose (IVF trigger); single dose (diagnostic) Timing 36 hours before planned oocyte retrieval (IVF trigger) 📅 Cycle Duration Single administration per IVF cycle Repeatable Single cycle Preparation & Storage Diluent: Sterile water Storage: Store lyophilized kisspeptin at -20 degrees C or below.

mechanism · pending

The resulting elevation in intracellular calcium is the primary mechanism by which kisspeptin depolarizes and activates GnRH neurons.

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Additional signaling pathways downstream of KISS1R include activation of MAPK/ERK1/2, p38 M

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⚗️ Suggested Bloodwork ( 6 tests) LH and FSH When: Baseline Why: Baseline gonadotropin levels to confirm HPG axis readiness Estradiol When: Baseline Why: Confirm follicular development adequate for trigger Progesterone When: Baseline Why: Baseline; premature luteinization assessment LH When: 12-14 hours post-trigger Why: Confirm adequate LH surge response Progesterone When: Day of oocyte retrieval Why: Confirm luteinization LH surge When: Ongoing Why: Blunted response ( 15 IU/L peak) may indicate suboptimal trigger; consider rescue trigger ⚠️ Blunted response ( 15 IU/L peak) may indicate suboptimal trigger; consider rescue trigger 💡 Key Considerations → Requires intact hypothalamic-pituitary axis (will not work in pituitary failure) → Contraindication: Not effective in pitui

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Restore access No thanks, continue reading Related Reading Peptide VIP vasoactive intestinal neuropeptide Peptide GHRP-2 growth hormone releasing peptide Peptide Gonadorelin peptide How Kisspeptin works at the cellular level Overview of Kisspeptin benefits and applications Scientific Details Molecular Formula C257H383N69O74S3 Molecular Weight 5861.5 Da CAS Number 374675-21-5 Sequence (Kisspeptin-10) Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2 What is Kisspeptin?

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# Kisspeptin refers to a family of neuropeptides encoded by the KISS1 gene that serve as master regulators of the hypothalamic-pituitary-gonadal (HPG) axis, the central hormonal cascade controlling reproductive function.

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Its pivotal role in reproduction was established in 2003 through landmark genetic studies identifying loss-of-function mutations in the kisspeptin receptor (GPR54, now designated KISS

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All kisspeptin isoforms share the C-terminal Arg-Phe-NH2 motif that is essential for receptor binding and activation, and all signal through the same receptor, KISS1R.

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These two populations have distinct but complementary roles in reproductive neuroendocrine regulation.

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The arcuate kisspeptin neurons co-express neurokinin B and dynorphin (the KNDy neurons) and are responsible for generating the pulsatile release of gonadotropin-releasing hormone (GnRH), while the AVPV/preoptic kisspeptin neurons mediate the preovulatory GnRH/LH surge in females.

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nces in reproductive neuroendocrinology, providing the long-sought molecular explanation for how peripheral sex steroids feed back to the brain to regulate GnRH secretion.

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Mechanism of Action # KISS1R (GPR54) Receptor Signaling # Kisspeptin exerts its biological effects through binding to its cognate receptor, KISS1R (formerly GPR54), a Gq/11-coupled G-protein coupled receptor.

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KISS1R is expressed on GnRH neurons in the hypothalamus, as well as in the pituitary, placenta, and various peripheral tissues.

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In GnRH neurons, kisspeptin-mediated signaling also involves activation of TRPC (transient receptor potential canonical) channels, which contribute to sustained neuronal depolarization.

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KISS1R signaling is subject to desensitization through beta-arrestin-mediated receptor internalization, which is clinically relevant because continuous kisspeptin exposure leads to receptor desensitization and eventual suppression rather than sustained stimulation of GnRH release.

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Kisspeptin is the most potent known activator of GnRH secretion, with intravenous administration of kisspeptin-54 producing robust increases in circulating LH and FSH (reflecting GnRH release) at doses as low as 0.1-1.0 nmol/kg in humans.

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The pulse-generating mechanism involves reciprocal interactions among the three co-expressed peptides: neurokinin B (NKB, stimulatory via NK3 receptors) drives bursting activity, dynorphin (inhibitory via kappa opioid receptors) terminates each pulse, and kisspeptin provides the final output signal that directly activates GnRH n

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The pulsatile pattern of GnRH delivery is critical for maintaining gonadotroph responsiveness; continuous GnRH exposure paradoxically downregulates GnRH receptors and suppresses gonadotropin release, a principle exploited therapeutically by GnRH agonists used in conditions such as prostate cancer and endometriosis.

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Estrogen, progesterone, and testosterone regulate GnRH secretion not by acting directly on GnRH neurons (which lack estrogen receptor alpha and androgen receptors) but by modulating the activity of kisspeptin neurons, which express abundant sex steroid receptors.

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In the negative feedback loop, circulating sex steroids act on arcuate kisspeptin neurons to suppress KISS1 gene expression and kisspeptin release, reducing GnRH pulse frequency and amplitude.

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Estrogen receptor alpha (ERalpha) is the primary mediator of this negative feed

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In the positive feedback loop (unique to females), rising estradiol levels during the late follicular phase of the menstrual cycle stimulate kisspeptin expression in the AVPV/preoptic kisspeptin population, triggering the massive GnRH surge that induces the LH surge and ovulation.

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Absence of Approved Formulations # No kisspeptin formulation has received regulatory approval for any indication.

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This positive feedback mechanism is sexually dimorphic, present in females but largely absent in males, and depends on both ERalpha and progesterone receptor signaling in AVPV kisspeptin neurons.

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The onset of puberty is marked by a gradual increase in pulsatile GnRH secretion, which is driven by increasing kisspeptin expression and signaling in the hypothalamus.

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KISS1 and KISS1R gene expression in the hypothalamus increases dramatically during the pubertal transition in multiple species, and the timing of this increase correlates with the onset of pubertal events.

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Loss-of-function mutations in KISS1 or KISS1R in humans cause isolated hypogonadotropic hypogonadism with absent or incomplete puberty, confirming the indispensable role of kisspeptin signaling in pubertal onset.

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The developmental regulation of kisspeptin expression involves epigenetic modifications, including changes in DNA methylation and histon

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