Hormone / Fertility
    Investigational

    Gonadorelin Acetate

    Also known as: GnRH, LHRH, Factrel, gonadotropin releasing hormone

    Synthetic GnRH that stimulates pituitary release of LH and FSH, studied in gonadotropin and reproductive-axis research.

    Research overview

    Gonadorelin is the synthetic form of gonadotropin-releasing hormone (GnRH, also called LHRH), a ten-amino-acid peptide made by nerve cells in the hypothalamus and released in pulses. Its structure was worked out from pig hypothalamus in 1971 (Schally et al., Science 1971). In the UK, gonadorelin is licensed as a prescription medicine for a single test of how the pituitary responds, for example when gonadotropin deficiency is suspected or after pituitary surgery or radiotherapy. Human products approved in the US in 1982 and 1989 are now listed as discontinued, while US-approved veterinary products are used in cattle for ovarian follicular cysts and to time artificial insemination. In rhesus monkeys with hypothalamic damage, pulses of GnRH re-established LH and FSH release, while constant exposure did not and switched the response off (Belchetz et al., Science 1978). In people, pulsed GnRH has been studied in women with hypothalamic amenorrhoea (absent periods caused by low GnRH output). A 2018 review pooled 35 studies with 1,002 women, but only three were randomised and the rest were observational (Tranoulis et al., 2018). These research materials are not the licensed medicine. Supplied for laboratory research use only.

    Mechanism of action

    Gonadorelin binds the GnRH receptor, a G-protein coupled receptor on the gonadotroph cells of the anterior pituitary. Binding triggers the making and release of luteinising hormone (LH) and follicle-stimulating hormone (FSH), which act on the ovaries and testes. The pattern of exposure matters: in monkey studies, pulses kept LH and FSH release going, while constant exposure switched it off.

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