Identification | Back Directory | [Name]
PGLU-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2 | [CAS]
54784-44-0 | [Synonyms]
wy-18,185 LHRH, Phe(2)-Ala(6)- [D-PHE2, D-ALA6]-LH-RH [D-PHE2, D-ALA6]-LH-RH (HUMAN) (d-phe(sup2))-(d-ala(sup6))-lhrh D-PHE2 D-ALA6-LUTEINIZING HORMONE & GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2 PYR-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2 PGLU-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2 D-phe2,D-ala6-luteinizing hormone*releasing hormo [D-Phe2,D-Ala6]lutenizing hormone-releasing factor [DPHE2,DALA6] LUTEINIZING HORMONE-RELEASING HORMONE [D-PHE2, D-ALA6]-LUTEINIZING HORMONE-RELEASING HORMONE (HUMAN) (d-phe(sup2))-(d-ala(sup6))-luteinizinghormone-releasinghormon (d-phe(sup2))-(d-ala(sup6))-luteinizinghormone-releasinghormone 5-Oxo-L-Pro-D-Phe-L-Trp-L-Ser-L-Tyr-D-Ala-L-Leu-L-Arg-L-Pro-Gly-NH2 GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2: GLP-DF-WSY-DA-LRPG-NH2 2-d-phenylalanine-6-d-alanine-luteinizinghormone-releasinghormone(pig Glycinamide, 5-oxo-L-prolyl-D-phenylalanyl-L-tryptophyl-L-seryl-L-tyrosyl-D-alanyl-L-leucyl-L-arginyl-L-prolyl- | [Molecular Formula]
C59H79N15O13 | [MDL Number]
MFCD00079994 | [MOL File]
54784-44-0.mol | [Molecular Weight]
1206.35 |
Hazard Information | Back Directory | [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 |
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