Gonadorelin is the synthetic decapeptide with an amino-acid sequence identical to endogenous gonadotropin-releasing hormone (GnRH/LHRH). Historically approved in several countries for diagnostic testing of pituitary function and for fertility indications (pump systems). A defining feature is the opposite effect of pulsatile versus continuous administration: pulsatile stimulates, continuous leads to receptor desensitisation.
Gonadorelin acts as an agonist at the GnRH receptor on the gonadotroph cells of the pituitary and triggers release of the gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH). The temporal pattern of receptor exposure is decisive: pulsatile administration mimics the natural hypothalamic secretory rhythm and sustains LH/FSH release, whereas continuous exposure leads to receptor internalisation and desensitisation with subsequent paradoxical suppression of gonadotropins. The latter principle is exploited therapeutically by longer-acting GnRH agonists.
Theoretische concentratiecurve bij een halfwaardetijd van 0.1 h. Puur farmacokinetisch model — geen doseringsaanbeveling.
Open in PK tool →Peptiden komen als droog poeder. Eenmaal opgelost in een vloeistof (reconstitutie) beantwoordt deze calculator één enkele vraag: hoeveel stof zit er daarna in één milliliter oplossing?
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