Ganirelix (acetate)

Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity^[1][2]. IC50 & Target:GnRH^[1] In Vitro:Ganirelix (1 nM-1 μM) acetate has no effect on Carbachol-induced or nerve-induced detrusor contractions in isolated bladder preparations from female rats^[2]. In Vivo:Ganirelix (0.1 mg/kg; subcutaneous injection; daily; for 14 consecutive days) acetate reduces plasma LH levels in female rats, significantly attenuates Prostaglandin E2-induced detrusor overactivity, and enhances detrusor contractions induced by high concentrations of Carbachol^[2].
Ganirelix (1.4 mg/L; intravesical administration; single dose) acetate regulates normal micturition function in female rats by prolonging micturition intervals, increasing voided volume and bladder capacity, while reducing basal urodynamic pressure, threshold urodynamic pressure and maximum urodynamic pressure parameters; its reduction in flow pressure does not reach statistical significance^[2].