别名 | N-((4R,7R,10R,13S,16S,19R)-19-(((S)-1-(((S)-1-((S)-2-((R)-1-氨基-1-氧代丙烷-2-基)氨基甲酰基)吡咯烷-1-基)-6-(异丙基氨基)-1-氧代己基-2-基)氨基)-4-甲基-1-氧代戊烷-2-基)氨基甲酰基)-7-(4-氯苄基)-13-(羟甲基)-4-(萘-2-基甲基)-16-(4-(烟酰胺基)丁基)-2,5,8,11,14,17-六氧代-10-(吡啶-3-基甲基)-3,6,9,12,15,18-六氮杂二十三烷-23-基)烟酰胺乙酸盐 |
产品描述 | Antide is a third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist.1,2,3,4It 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).1,3Antide (250 µg/kg, i.v.) reduces serum LH and FSH levels in orchidectomized cynomolgus monkeys.2It inhibits ovulation in rats when administered at a dose of 2 µg/animal.3Antide (10 µg/animal, s.c.) reduces the intensity and duration of catalepsy induced by haloperidol in rats.4 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) |