Biological Activity
Antide is a third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist.1,2,3,4 It inhibits GnRH-induced secretion of luteinizing hormone (LH), follicle-stimulating hormone (FSH), and gonadotropin in isolated rat pituitary cells when used at concentrations ranging from 0.001 to 1,000 nM but does not induce histamine release in isolated rat mast cells (EC50 = >300 μg/ml).1,3 Antide (250 μg/kg, i.v.) reduces serum LH and FSH levels in orchidectomized cynomolgus monkeys.2 It inhibits ovulation in rats when administered at a dose of 2 μg/animal.3 Antide (10 μg/animal, s.c.) reduces the intensity and duration of catalepsy induced by haloperidol in rats.4
References
1.Danforth, D.R., Williams, R.F., Gordon, K., et al.Inhibition of pituitary gonadotropin secretion by the gonadotropin-releasing hormone antagonist antide. I. In vitro studies on mechanism of actionEndocrinology128(4)2036-2040(1991)
2.Weinbauer, G.F., and Nieschlag, E.Comparison of the antigonadotropic activity of three GnRH antagonists (Nal-Glu, Antide and Cetrorelix) in a non-human primate model (Macaca fascicularis)Andrologia25(3)141-147(1993)
3.Flouret, G., Arnold, Z.S., Majewski, T., et al.Antiovulatory antagonists of LHRH related to antideJ. Pept. Sci.1(2)89-108(1995)
4.Umathe, S.N., Wanjari, M.M., Manna, S.S.S., et al.A possible participation of gonadotropin-releasing hormone in the neuroleptic and cataleptic effect of haloperidolNeuropeptides43(3)251-257(2009)
