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盐酸罗匹尼罗

盐酸罗匹尼罗用途

Ropinirole(SKF101468)盐酸盐是多巴胺受体D2抑制剂,IC50为29 nM。

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盐酸罗匹尼罗名称

[ CAS 号 ]:
91374-20-8

[ 中文名 ]:
4-(2-二正丙基胺乙基)-1,3-二氯-2H-吲哚-2-酮

[ 英文名 ]:
Ropinirole hydrochloride

[中文别名 ]:

[英文别名 ]:

UNII-D7ZD41RZI9
ropinirole hcl
Adartrel
MFCD01754173
Ropinirole hydrochloride
Requip
Ropinirole (hydrochloride)

盐酸罗匹尼罗生物活性

[ 描述 ]:

Ropinirole(SKF101468)盐酸盐是多巴胺受体D2抑制剂,IC50为29 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[参考文献]

[1]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54.

[2]. Iida, M., et al., Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res, 1999. 838(1-2): p. 51-9.

[3]. Lam, Y.W., Clinical pharmacology of dopamine agonists. Pharmacotherapy, 2000. 20(1 Pt 2): p. 17S-25S.

[4]. Allen, R., et al., Ropinirole decreases periodic leg movements and improves sleep parameters in patients with restless legs syndrome. Sleep, 2004. 27(5): p. 907-14.

[相关活性小分子]

盐酸罗匹尼罗物理化学性质

[ 沸点 ]:
410.5ºC at 760mmHg

[ 熔点 ]:
241-243ºC

[ 分子式 ]:
C₁₆H₂₅ClN₂O

[ 分子量 ]:
296.836

[ 精确质量 ]:
296.165527

[ PSA ]:
32.34000

[ LogP ]:
3.78570

[ 外观性状 ]:
灰白色固体

[ 储存条件 ]:
Room temp

盐酸罗匹尼罗毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NM3288250

CHEMICAL NAME :: 2H-Indol-2-one, 1,3-dihydro-4-(2-(dipropylamino)ethyl)-, monohydrochloride

CAS REGISTRY NUMBER :: 91374-20-8

LAST UPDATED :: 199807

DATA ITEMS CITED :: 9

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 :: 396 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1725,199

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 71 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1725,199 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg/30D-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in adrenal weight Related to Chronic Data - changes in ovarian weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1731,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18250 mg/kg/1Y-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Kidney, Ureter, Bladder - other changes Endocrine - changes in adrenal weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1731,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 450 mg/kg/30D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - excitement Skin and Appendages - hair

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1741,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 5475 mg/kg/1Y-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Related to Chronic Data - changes in ovarian weight Related to Chronic Data - changes in testicular weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1741,199 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3040 mg/kg

SEX/DURATION :: female 2 week(s) pre-mating - 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 280 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 24(Suppl 11),S1747,199

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盐酸罗匹尼罗安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
36-60-61-37/39-26

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ RTECS号 ]:
NM3288250

[ 危险类别 ]:
9.0

[ 海关编码 ]:
2933790090

盐酸罗匹尼罗合成路线

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盐酸罗匹尼罗海关

[ 海关编码 ]: 2933790090

[ 中文概述 ]:
2933790090 其他内酰胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:9.0% 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

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