| Name | 5-Oxo-L-prolyl-D-phenylalanyl-L-prolyl-L-seryl-L-tyrosyl-D-phenylalanyl-L-leucyl-N5-(diaminomethylene)-L-ornithyl-L-prolylglycinamide |
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| Description | [D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist[1]. |
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| 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 |
| Density | 1.44g/cm3 |
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| Molecular Formula | C59H80N14O13 |
| Molecular Weight | 1193.35000 |
| Exact Mass | 1192.60000 |
| PSA | 421.37000 |
| LogP | 2.32480 |
| Index of Refraction | 1.679 |