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法倔唑盐酸盐

法倔唑盐酸盐用途

Fadrozole hydrochloride 是一种有效，选择性和非甾体类的 aromatase 抑制剂，其 IC₅₀ 值为 6.4 nM。

法倔唑盐酸盐名称

[ CAS 号 ]:
102676-31-3

[ 中文名 ]:
法倔唑盐酸盐

[ 英文名 ]:
Fadrozole hydrochloride

[英文别名 ]:

FADROZOLE HCL
Fadrazole
fadrozole hydrochloride
MFCD00866239

法倔唑盐酸盐生物活性

[ 描述 ]:

Fadrozole hydrochloride 是一种有效,选择性和非甾体类的 aromatase 抑制剂,其 IC50 值为 6.4 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 芳香

研究领域 >> 癌症

[ 靶点 ]

IC50: 6.4 nM (aromatase)[1]

[体外研究]

盐酸法倔唑是一种有效的,选择性和非甾体芳香化酶抑制剂,IC50为6.4 nM。在仓鼠卵巢切片中,盐酸法倔唑抑制雌激素的产生,IC50为0.03μM。 IC50为120μM时,黄体酮的产生受到抑制。其他细胞色素P-450依赖类固醇的合成可以用更高剂量的盐酸法倔唑[1]进行不同程度的抑制。

[体内研究]

盐酸法倔唑能够抑制未成熟雌性大鼠中芳香酶介导的雄烯二酮诱导的子宫肥大,口服给药时ED50为0.03mg/kg。在同一模型中,氨基乙酰亚胺引起相同的效果,口服给药时ED50为30 mg/kg [1]。盐酸法倔唑可预防雌性Sprague-Dawley大鼠良性和恶性自发乳腺肿瘤的发生。它还可以减缓雌性大鼠ptuitary pars远端腺瘤的自发发展,降低雄性和雌性大鼠自发性肝细胞肿瘤的发生率[2]。在雄性和雌性小鼠中施用盐酸法倔唑抑制17b-雌二醇的产生,伴随寄生虫负荷减少70％。这种保护作用在雄性小鼠中与特定细胞免疫应答的恢复相关。白细胞介素-6(IL-6)血清水平及其通过脾细胞的产生增加了80％,并且其在感染的雄性小鼠的睾丸中的表达增加了10倍。盐酸法倔唑治疗将这些水平恢复到基线值[3]。

[动物实验]

大鼠：每天通过管饲法用纯化水中的盐酸法倔唑治疗大鼠2年。每组中有60只大鼠，每天给予0,0.05,0.25或1.25mg / kg。对照大鼠仅接受水。每周记录临床症状，并在前9个月每4周检查一次可触及的肿块，然后在研究的其余部分每2周检查一次[2]。小鼠：使用10号针头，在感染前1周开始，以皮下长期释放小丸（20mg / wt kg，三周释放小丸）的形式给予盐酸法苯肼。在研究期间施用三个颗粒。以与抑制剂相同的方式将安慰剂颗粒给予另一组感染的小鼠。 1周后，小鼠被感染并在8周后被杀死[3]。

[参考文献]

[1]. Browne LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991 Feb;34(2):725-36.

[2]. Gunson DE, et al. Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor. Br J Cancer. 1995 Jul;72(1):72-5.

[3]. Morales-Montor J, et al. Inhibition of p-450 aromatase prevents feminisation and induces protection during cysticercosis. Int J Parasitol. 2002 Oct;32(11):1379-87.

[相关活性小分子]

法倔唑 | 依西美坦 | N-去甲基-4-羟基-

法倔唑盐酸盐物理化学性质

[ 沸点 ]:
481.7ºC at 760mmHg

[ 分子式 ]:
C₁₄H₁₄ClN₃

[ 分子量 ]:
259.73400

[ 闪点 ]:
245.1ºC

[ 精确质量 ]:
259.08800

[ PSA ]:
41.61000

[ LogP ]:
3.48248

[ 蒸汽压 ]:
1.95E-09mmHg at 25°C

[ 储存条件 ]:
2-8℃

法倔唑盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DI4952500

CHEMICAL NAME :: Benzonitrile, 4-(5,6,7,8-tetrahydroimidazo(1,5-a)pyridin-5-yl)-, monohydrochloride

CAS REGISTRY NUMBER :: 102676-31-3

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C14-H13-N3.Cl-H

MOLECULAR WEIGHT :: 259.76

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 47200 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 163 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 26,740,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2500 ug/kg

SEX/DURATION :: female 16-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: NISFAY Nippon Sanka Fujinka Gakkai Zasshi. Journal of the Japan Society of Obstetrics and Gynecology. (Nippon Sanka Fujinka Gakkai Zasshi, Hoken Kaikan Bekkan, 1-1 Sadohara-cho, Ichigaya, Shijuku-ku, Tokyo 162, Japan) V.1- 1949- Volume(issue)/page/year: 46,227,1994

法倔唑盐酸盐安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H361

[ 警示性声明 ]:
P281-P301 + P310

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22;R63

[ 安全声明 (欧洲) ]:
S36/S37

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

[ RTECS号 ]:
DI4952500

法倔唑盐酸盐文献

Transdifferentiation of differentiated ovary into functional testis by long-term treatment of aromatase inhibitor in Nile tilapia.

Endocrinology 155(4) , 1476-88, (2014)

Females with differentiated ovary of a gonochoristic fish, Nile tilapia, were masculinized by long-term treatment with an aromatase inhibitor (Fadrozole) in the present study. The reversed gonads deve...

Masculinisation of the zebra finch song system: roles of oestradiol and the Z-chromosome gene tubulin-specific chaperone protein A.

J. Neuroendocrinol. 27(5) , 324-34, (2015)

Robust sex differences in brain and behaviour exist in zebra finches. Only males sing, and forebrain song control regions are more developed in males. The factors driving these differences are not cle...

In vivo response of melatonin, gonadal activity and biochemical changes during CYP19 inhibited sex reversal in common carp Cyprinus carpio (L).

Anim. Reprod. Sci. 136(4) , 317-25, (2013)

CYP19 aromatase is the key enzyme in vertebrate steroidogenesis, catalyzing the conversion of C19 androgens to 17β-estradiol (E(2)). The objective of the present study was to assess the effect of the ...

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