| Identification | Back Directory | [Name]
antarelix | [CAS]
151272-78-5 | [Synonyms]
antarelix
D-Alaninamide, N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-L-tyrosyl-N6-(aminocarbonyl)-D-lysyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl- | [Molecular Formula]
C74H100ClN15O14 | [MDL Number]
MFCD08056228 | [MOL File]
151272-78-5.mol | [Molecular Weight]
1459.13 |
| Hazard Information | Back Directory | [Uses]
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer[1][2]. | [in vivo]
Teverelix (3-300 μg/kg, intramuscular injection) inhibits testosterone in rats[3].
Teverelix (1 mg/kg, s.c, daily for 3 days) abolishes luteal function in stumptailed macaques[4].
| Animal Model: | Rats[3] | | Dosage: | 300, 100, 30, 10 and 3 μg/kg | | Administration: | Intramuscular injection | | Result: | Showed dose-response and time-course of testosterone inhibitory activity. |
| [References]
[1] MacLean CM, et al. Pharmacokinetic, Safety, and Pharmacodynamic Properties of Teverelix Trifluoroacetate, a Novel Gonadotropin-Releasing Hormone Antagonist, in Healthy Adult Subjects. Clin Pharmacol Drug Dev. 2022 Feb;11(2):257-269. DOI:10.1002/cpdd.1008
[2] Sperduti S, et al. GnRH Antagonists Produce Differential Modulation of the Signaling Pathways Mediated by GnRH Receptors. Int J Mol Sci. 2019 Nov 7;20(22):5548. DOI:10.3390/ijms20225548
[3] Deghenghi R, et al. Antarelix (EP 24332) a novel water soluble LHRH antagonist. Biomed Pharmacother. 1993;47(2-3):107-10. DOI:10.1016/0753-3322(93)90299-z
[4] Fraser HM, et al. Initiation of high dose gonadotrophin-releasing hormone antagonist treatment during the late follicular phase in the macaque abolishes luteal function irrespective of effects upon the luteinizing hormone surge. Hum Reprod. 1997 Mar;12(3):430-5. DOI:10.1093/humrep/12.3.430 |
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