- Directly couples to the GnRH receptor in the gonadotrope cells of the anterior pituitary.
- Forces the pituitary to release stored LH and FSH into the blood.
- Must be secreted in natural pulses (every 1-2 hours in men, variant in women) to work; continuous exposure to GnRH causes total inhibition (medical castration) instead of stimulation.
Hormonal Modulators
Peptide Hormones
Approved
Gonadorelina
Also known as: GnRH, Factrel
Gonadorelin (GnRH) is the synthetic version of the body's natural Gonadotropin-Releasing Hormone. It is produced in the hypothalamus and travels to the pituitary gland to instruct it to release LH (Luteinizing Hormone) and FSH (Follicle-Stimulating Hormone). These messengers are responsible for maintaining fertility, sperm and egg production, and testosterone/estrogen synthesis.
Mechanism of action
Uses & indications
- Testicular function recovery (TRT): In the sports community to prevent testicular shrinkage, it is used as a replacement for hCG, directly stimulating the axis from higher up.
- Infertility: Treatment of hypogonadotropic hypogonadism or amenorrhea in women using pulsatile infusion pumps.
Effects
Preservation of fertility and testicular volume in individuals on external testosterone therapy, reactivation of the endogenous axis.
Considerations & contraindications
- Unlike HCG (which mimics LH directly), Gonadorelin mimics brain GnRH, thus requiring a functional pituitary to be effective.
- Very high risk of desensitization if used in incorrect doses; the pituitary gland will stop responding and all hormone production will halt.
Regulatory approval
Medically approved as Factrel / Lutrepulse.
Dosage
For preventing testicular atrophy, athletes usually use micro-doses (e.g., 100mcg) twice a week or frequently, but practices vary widely due to the difficulty of mimicking pulses.
Storage
Lyophilized at -20°C.
Technical data
Regulatory status
Approved
Molecular weight
1182.3 Da
Half-life
Menos de 10-20 minutos
Administration routes
Subcutánea, Intravenosa (bomba pulsátil)
Categories
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