Description

As a potent LHRH agonist, histrelin stimulates LH and FSH release and inhibits the actions of sex steroids on the male and female reproductive tracts. Its potency in vivo and in vitro is similar to that of the D-Trp6-containing analog. Especially because of its high water solubility and greater lipophilic character, histrelin appears promising for clinical application.Slow-release implants containing histreline implants were approved for the palliative treatment of advanced hormone-dependent prostate cancer.

SEQUENCE: Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt (acetate salt)

ONE-LETTER SEQUENCE: Pyr-HWSYh(Bzl)-LRP-NHEt

MOLECULAR FORMULA: C₆₆H₈₆N₁₈O₁₂

MOLECULAR WEIGHT: 1323.52

STORAGE CONDITIONS: -20 ± 5 °C

CAS REGISTRY NUMBER: [220810-26-4]

SYNONYMS:

RESEARCH AREA: Hormonal

REFERENCES:
K.Sundaram et al., Life Sci., 28, 83 (1981)
J.DeFazio et al., Endocr. Res., 10, 163 (1984)
M.J.Gibson and D.S.Kohtz, Contraception, 31, 91 (1985)
M.J.Karten and J.E.Rivier, Endocr. Rev., 7, 44 (1986)
G.C.Doelle et al., Horm. Metab. Res., 18, 201 (1986)
J.W.Gunnet et al., J. Endocrinol., 131, 211 (1991)
M.Montagner et al., Reprod. Fertil. Dev., 17, 222 (2005)
Merck Index, 14th ed., No. 4722, (2006)
E.D.Deeks, Drugs, 70, 623 (2010)
N.Shore et al., BJU Int., 109, 226 (2012)

SKU(s): LHRH-014A, LHRH-014B

KEYWORDS: hormone