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GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2: GLP-DF-WSY-DA-LRPG-NH2

用途

[D-Phe2,D-Ala6]-LH-RH是一种有效的LH-RH拮抗剂。[D-Phe2,D-Ala6]-LH-RH具有抗LH/FSH-RH和抗排卵活性[1]。

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名称

[ CAS 号 ]:
54784-44-0

[ 中文名 ]:
GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2: GLP-DF-WSY-DA-LRPG-NH2

[ 英文名 ]:
a d lh-rh

[英文别名 ]:

GLP-DPHE-TRP-SER-TYR-DALA-LEU-ARG-PRO-GLY-NH2
[D-PHE2,D-ALA6]-LH-RH (HUMAN)
PYR-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2
[D-PHE2,D-ALA6]-LH-RH
PGLU-D-PHE-TRP-SER-TYR-D-ALA-LEU-ARG-PRO-GLY-NH2
D-phe2,D-ala6-luteinizing hormone*releasing hormo
wy-18,185
LHRH,Phe(2)-Ala(6)
(d-phe(sup2))-(d-ala(sup6))-lhrh

生物活性

[ 描述 ]:

[D-Phe2,D-Ala6]-LH-RH是一种有效的LH-RH拮抗剂。[D-Phe2,D-Ala6]-LH-RH具有抗LH/FSH-RH和抗排卵活性[1]。

[ 相关类别 ]:

研究领域 >> 内分泌

信号通路 >> 其他 >> 其他

[体内研究]

[D-Phe2,D-Ala6]-LH-RH抑制未成年雄性大鼠中LH-RH诱导的LH和FSH释放[1]。[D-Phe2,D-Ala6]-LH-RH(1 mg/大鼠,SC)显示出显著的抗排卵和避孕活性[2]。[D-Phe2,D-Ala6]-LH-RH(0.625,1.25,2.5 mg/kg；皮下注射；单剂量；处死30分钟)导致25日龄垂体切除(低氧)大鼠的茎秆中隆起(SME)-LHRH活性呈剂量依赖性增加,并降低血浆LHRH活性[3]。[D-Phe2,D-Ala6]-LH-RH(25 mg/kg；皮下注射；单剂量)可有效阻断LRH单独诱导的排卵[4]。动物模型：成年雌性Sprague-Dawley大鼠(200-250 g)[2]剂量：1 mg/大鼠给药：SC注射,发情前12:00至14:30小时结果：显示出显著的抗排卵和避孕活性,排卵抑制率为96%。

[参考文献]

[1]. Vilchez-Martinez JA, et al. Comparison of the anti-LH/FSH-RH and anti-ovulatory activities of (D-Phe2, D-Leu6)-LH-RH and (D-Phe2, D-Ala6)-LH-RH. Endocr Res Commun. 1976;3(3-4):231-41.

[2]. Beattie CW, et al. Luteinizing hormone-releasing hormone. Antiovulatory activity of analogs substituted in positions 2 and 6. J Med Chem. 1975 Dec;18(12):1247-50.

[3]. Corbin A, et al. Effect of luteinizing hormone releasing hormone (LHRH) and an LHRH antagonist of hypothalamic and plasma LHRH of hypophysectomized rats. Endocrinology. 1976 Jan;98(1):247-50.

[4]. Corbin A, et al. Ihibition of the pre-ovulatory proestrous gonadotropin surge, ovulation and pregnancy with a peptide analogue of luteinizing hormone releasing hormone. Endocr Res Commun. 1975;2(1):1-23.

物理化学性质

[ 密度 ]:
1.46g/cm3

[ 分子式 ]:
C₅₉H₇₉N₁₅O₁₃

[ 分子量 ]:
1206.35000

[ 精确质量 ]:
1205.60000

[ PSA ]:
443.45000

[ LogP ]:
2.77280

[ 折射率 ]:
1.687

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OK6600000

CHEMICAL NAME :: Luteinizing hormone-releasing hormone, (D-phe(sup 2))-(D-ala(sup 6))-

CAS REGISTRY NUMBER :: 54784-44-0

LAST UPDATED :: 198910

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C59-H79-N15-O13

MOLECULAR WEIGHT :: 1206.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 3750 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 18,1247,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: IJGOAL International Journal of Gynaecology & Obstetrics. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.7- 1969- Volume(issue)/page/year: 16,359,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 30 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 12500 ug/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: EDRCAM Endocrine Research Communcations. (New York, NY) V.1-9, 1974-83. Volume(issue)/page/year: 2,1,1975

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安全信息

[ 风险声明 (欧洲) ]:
60

[ 安全声明 (欧洲) ]:
53-22-36/37/39-45