LHRH, Phe(2)-Pro(3)-Phe(6)-
Names
[ CAS No. ]:
64789-67-9
[ Name ]:
LHRH, Phe(2)-Pro(3)-Phe(6)-
Biological Activity
[Description]:
[D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist[1].
[Related Catalog]:
[In Vitro]
[D-Phe2,6, Pro3]-LH-RH (0.1 pM-1 mM; 24 h) does not alter GnRH binding capacity in pituitary cells but blocks the increase in sites induced by GnRH[2]. [D-Phe2,6, Pro3]-LH-RH (2.7 μM) causes significant increases in thyrotropin (TSH) secretion in pituitaries[3].
[In Vivo]
[D-Phe2,6, Pro3]-LH-RH (300 mg/monkey, SC, 50 mg/injection; six injections) inhibits spontaneous preovulatory gonadotropin surges and prevents ovulation in the rhesus monkey[1]. [D-Phe2,6, Pro3]-LH-RH (750 μg, single injection at 12:00 h on the day of proestrus) inhibits ovulation in 100% of treated rats[1]. Animal Model: Adult rhesus monkeys[1] Dosage: 300 mg/monkey Administration: SC, every 8 h at a dose of 50 mg/injection; six injections Result: Showed antagonistic activity: 1) an immediate cessation of the LU and FSH surges; 2) prolonged surges and/or abnormal, discontinuous gonadotropin secretion; 3) LH and FSH peaks of diminished magnitude; 4) the absence of concomitant LH and FSH midcycle peaks; 3) LH and FSH peaks of diminished magnitude; 4) the absence of concomitant LH and FSH midcycle peaks; 5) suppression of serum estradiol concentrations without concurrent reductions in serum gonadotropin values; or 6) a failure to identify corpora lutea at the time of laparoscopic visualization of the ovaries.
[References]
Chemical & Physical Properties
[ Density]:
1.44g/cm3
[ Molecular Formula ]:
C59H80N14O13
[ Molecular Weight ]:
1193.35000
[ Exact Mass ]:
1192.60000
[ PSA ]:
421.37000
[ LogP ]:
2.32480
[ Index of Refraction ]:
1.679