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编 号：F759448
分子式：C59H80N14O13
分子量：1193.35
分子式：C59H80N14O13
分子量：1193.35
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CAS No: 64789-67-9
产品详情
生物活性：
[D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist.
体内研究：
[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.[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.Animal Model:Adult rhesus monkeys
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.
体外研究：
[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. [D-Phe2,6, Pro3]-LH-RH (2.7 μM) causes significant increases in thyrotropin (TSH) secretion in pituitaries.
[D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist.
体内研究：
[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.[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.Animal Model:Adult rhesus monkeys
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.
体外研究：
[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. [D-Phe2,6, Pro3]-LH-RH (2.7 μM) causes significant increases in thyrotropin (TSH) secretion in pituitaries.
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