Description
Histrelin, a synthetic gonadotrophin-releasing hormone (GnRH) agonist, was introduced
as a first-line therapy for the treatment of central precocious puberty. When administered over
a prolonged period, it suppresses the release of gonadotrophin, inhibits ovarian and testicular
steroidogenesis, and prevents sexual maturation. Superior to the traditional therapy with
progestational agents, histrelin appears to have decelerating effects on skeletal maturation
allowing more statural growth and significantly increased final adult height. Histrelin has also
been used to treat other disorders including endometriosis, polycystic ovarian disease,
uterine leiomyomas, severe premenstrual syndrome and to prevent acute intermittent
porphyria.
Chemical Properties
[α]D20-33.9°(C=1, acetic acid).
Originator
Johnson & Johnson (U.S.A.)
Uses
[des-Gly10, D-His(Bzl)6]-LH-RH ethylamide has been used:
- for inducing Batrachoseps gravid females to oviposit
- for comparing the effect of LHRH (luteinizing hormone-releasing hormone) agonists and dopamine antagonists in Lithobates pipiens
- for inducing oviposition in females of Taricha granulosa and Ensatina eschscoltzii
- to induce spawning in Spea hammondii adults
Definition
ChEBI: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, 1-benzyl-D-histidyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotro
in-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the diacetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.
Brand name
Supprelin (Roberts Pharmaceutical).
Biochem/physiol Actions
Glp-His-Trp-Ser-Tyr-His(Bzl)-Leu-Arg-Pro-NHEt ([des-Gly10, D-His(Bzl)6]-LH-RH) is a GnRH (gonadotropin-releasing hormone) agonist, histerelin. GnRH (Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2), which is also referred as LHRH (luteinizing hormone-releasing hormone) or gonadorelin, is crucial for mammalian reproduction and is released from hypothalamic neurons. It is responsible for the secretion of gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), from the pituitary glands. Mutations in GnRH are associated with normosmic congenital hypogonadotropic hypogonadism. Histerelin is used for the treatment of central precocious puberty in children. It inhibits actions of sex steroids on the male and female reproductive organs.
