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组氨瑞林

组氨瑞林用途

Histrelin是一种促性腺激素释放激素类似物,是促性腺素释放激素受体激动剂。组氨酸增加血清黄体生成素(LH)、卵泡刺激素(FSH)和睾酮水平。组氨酸可用于前列腺癌、子宫内膜异位症的研究[1][2][5]。
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组氨瑞林名称

[ CAS 号 ]:
76712-82-8

[ 中文名 ]:
组氨瑞林

[ 英文名 ]:
Histrelin

[英文别名 ]:

组氨瑞林生物活性

[ 描述 ]:

Histrelin是一种促性腺激素释放激素类似物,是促性腺素释放激素受体激动剂。组氨酸增加血清黄体生成素(LH)、卵泡刺激素(FSH)和睾酮水平。组氨酸可用于前列腺癌、子宫内膜异位症的研究[1][2][5]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体
研究领域 >> 癌症

[ 靶点 ]

GnRH Receptor[1]


[体外研究]

Histrelin(10-100 nM)刺激离体大鼠下丘脑神经垂体外植体释放加压素(VP)[4]。Histrelin(100 nM)刺激大鼠下丘脑神经垂体系统释放催产素(OT)[5]。

[体内研究]

Histrelin(0.1 mg/kg,皮下注射)可挽救Csfmop/Csfmop小鼠的循环LH浓度[2]。Histrelin(10、30或100μg/天,皮下注射)可减少家兔子宫内膜腺的数量,并使基质萎缩[3]。动物模型：Csfmop/Csfmop小鼠[2]剂量：0.001、0.05和0.1 mg/kg给药：皮下注射结果：血清FSH浓度增加4倍。动物模型：兔子[3]剂量：10、30或100μg/天给药：皮下注射4周结果：导致子宫内膜腺体退化和基质变薄。

[参考文献]

[1]. Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30.

[2]. 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.

[3]. 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.

[4]. 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.

[5]. 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.

组氨瑞林物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
1800.6ºC at 760 mmHg

[ 分子式 ]:
C66H86N18O12

[ 分子量 ]:
1323.502

[ 闪点 ]:
1042.8ºC

[ 精确质量 ]:
1322.667236

[ PSA ]:
446.86000

[ LogP ]:
0.09

[ 外观性状 ]:
白色或近乎于白色冻干的粉末

[ 折射率 ]:
1.701

[ 储存条件 ]:
室温， 干燥

组氨瑞林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
OK6370800
CHEMICAL NAME :
Luteinizing hormone releasing factor (pig), 6-(1-(phenylmethyl)-D-histidine)-9-(N-ethyl-L- prolinamide)-10-deglycinamide-
CAS REGISTRY NUMBER :
76712-82-8
LAST UPDATED :
199612
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C66-H86-N18-O12
MOLECULAR WEIGHT :
1323.70

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
46 ug/kg
SEX/DURATION :
male 2 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male
REFERENCE :
JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
4667 ug/kg
SEX/DURATION :
male 8 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
REFERENCE :
JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
2333 ug/kg
SEX/DURATION :
male 4 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)
REFERENCE :
JOAND3 Journal of Andrology. (Lippincott/Harper, Journal Fulfillment Dept., 2350 Virginia Ave., Hagerstown, MD 21740) V.1- 1980- Volume(issue)/page/year: 7,140,1986
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组氨瑞林安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H360

[ 警示性声明 ]:
P201-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
R60

[ 安全声明 (欧洲) ]:
53-22-36/37/39-45

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
OK6370800

[ 海关编码 ]:
2937190090

组氨瑞林制备

通过固相法合成得到组氨瑞林。
用二（对甲基苯基）甲胺为树脂，并用过量3倍的BOC和二环已基碳化二亚胺（DCC）作为致活剂，在二氯甲烷中反应2h，使BOC保护的甘氨酸和树脂偶合。然后连上下一个氨基酸，洗涤，脱保护。按下列操作连上下一个氨基酸。
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组氨瑞林海关

[ 海关编码 ]: 2937190090

组氨瑞林文献

Stability of peptide drugs in the colon.

Eur. J. Pharm. Sci. 78 , 31-6, (2015)

This study was the first to investigate the colonic stability of 17 peptide molecules (insulin, calcitonin, glucagon, secretin, somatostatin, desmopressin, oxytocin, Arg-vasopressin, octreotide, ciclo...

Toward oral delivery of biopharmaceuticals: an assessment of the gastrointestinal stability of 17 peptide drugs.

Mol. Pharm. 12(3) , 966-73, (2015)

A major barrier to successful oral delivery of peptide and protein molecules is their inherent instability in the lumen of the gastrointestinal tract. The aim of this study was to determine the stabil...

Treatment and outcomes of precocious puberty: an update.

J. Clin. Endocrinol. Metab. 98(6) , 2198-207, (2013)

Precocious puberty is a common problem affecting up to 29 per 100,000 girls per year. The earliest identified neuroendocrine change in early puberty thus far is increased kisspeptin secretion from the...


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