Uses
[D-Phe2,D-Ala6]-LH-RH is a potent LH-RH antagonist. [D-Phe2,D-Ala6]-LH-RH shows anti-LH/FSH-RH and antiovulatory activities[1].
in vivo
[D-Phe2,D-Ala6]-LH-RH inhibits the LH and FSH release induced by LH-RH in immature male rats[1].
[D-Phe2,D-Ala6]-LH-RH (1 mg/rat, SC) shows marked antiovulatory and contraceptive activity[2].
[D-Phe2,D-Ala6]-LH-RH (0.625, 1.25, 2.5 mg/kg; s.c.; single dose; sacrificed 30 minutes) results a dose-dependent increase in stalk-median eminence (SME)-LHRH activity and decreases plasma LHRH activity as well in rats with hypophysectomized (hypox) at 25 days old[3].
[D-Phe2,D-Ala6]-LH-RH (25 mg/kg; s.c.; single dsoe) is effective in blocking the ovulation normally induced by LRH alone[4].
| Animal Model: | Adult female Sprague-Dawley rats (200-250 g)[2] |
| Dosage: | 1 mg/rat |
| Administration: | SC injections, from 12:00 to 14:30 hr on the day of proestrus |
| Result: | Showed marked antiovulatory and contraceptive activity, with 96% inhibition of ovulation. |
References
[1] Vilchez-Martinez JA, et al. Comparison of the anti-LH/FSH-RH and anti-ovulatory activities of (D-Phe2, D-Leu6)-LH-RH and (D-Phe2, D-Ala6)-LH-RH. Endocr Res Commun. 1976;3(3-4):231-41. DOI:
10.3109/07435807609056903[2] Beattie CW, et al. Luteinizing hormone-releasing hormone. Antiovulatory activity of analogs substituted in positions 2 and 6. J Med Chem. 1975 Dec;18(12):1247-50. DOI:
10.1021/jm00246a016[3] Corbin A, et al. Effect of luteinizing hormone releasing hormone (LHRH) and an LHRH antagonist of hypothalamic and plasma LHRH of hypophysectomized rats. Endocrinology. 1976 Jan;98(1):247-50. DOI:
10.1210/endo-98-1-247[4] Corbin A, et al. Ihibition of the pre-ovulatory proestrous gonadotropin surge, ovulation and pregnancy with a peptide analogue of luteinizing hormone releasing hormone. Endocr Res Commun. 1975;2(1):1-23. DOI:
10.3109/07435807509053836
