| Identification | Back Directory | [Name]
Vantas | [CAS]
220810-26-4 | [Synonyms]
Vantas
Supprelin la
Vantas USP/EP/BP
Histrelin acetate, >=98%
Histrelin?Acetate impurity
Histrelin Acetate(acetate)
(Des-Gly10,D-His(Bzl)6,Pro-NHEt 9)-LHRH acetate salt Pyr-His-Trp-Ser-Tyr-D-His(Bzl)-Leu-Arg-Pro-NHEt acetate salt | [Molecular Formula]
C66H86N18O12 | [MDL Number]
MFCD00918679 | [MOL File]
220810-26-4.mol | [Molecular Weight]
1323.52 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 0.25 mg/ml; PBS (pH 7.2): 10 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white | [Sequence]
{Pyr}-His-Trp-Ser-Tyr-{d-His(Bzl)}-Leu-Arg-Pro-{NHEt} |
| Hazard Information | Back Directory | [Description]
Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor). It stimulates release of oxytocin and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM. In vivo, the initial dose of histrelin (100 μg) stimulates acute increases in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys. Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty. | [Uses]
Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis[1][2][5]. | [Definition]
ChEBI: An acetate salt obtained by combining histrelin with acetic acid. The amount of acetic acid present can vary and a variable amount of water may be present. Histrelin acetate is used as a subcutaneous hydrogel implant for the treatment of prostate cancer an
for the suppression of gonadal sex hormone production in children with central precocious puberty. | [in vivo]
Histrelin (0.1 mg/kg, subcutaneous injection) acetate rescues the circulating LH concentrations in Csfmop/Csfmop mice[2].
Histrelin (10,30, or 100 μg /day, subcutaneous injection) acetate reduces the number of endometrial glands and atrophied the stroma in rabbits[3].
| [References]
[1] Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30. DOI:10.2165/11204800-000000000-00000
[2] Marlena Juszczak, et al. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res Bull. 2010 Jan 15;81(1):185-90. DOI:10.1016/j.brainresbull.2009.10.012
[3] P E Cohen, et al. Colony-stimulating factor-1 plays a major role in the development of reproductive function in male mice. Mol Endocrinol. 1997 Oct;11(11):1636-50. DOI:10.1210/mend.11.11.0009
[4] D W Hahn, et al. Development of an animal model for quantitatively evaluating effects of drugs on endometriosis. Fertil Steril. 1985 Sep;44(3):410-5. DOI:10.1016/s0015-0282(16)48869-2
[5] E Boczek-Leszczyk, et al. Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J Physiol Pharmacol. 2010 Aug;61(4):459-66. PMID:20814074 |
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