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1-[4-(4-氟苯基)-4-氧亚基丁基]-[1,4-联哌啶]-4-甲酰胺二盐酸

用途

二氢哌安酮(Floropipamide；McN JR 3345)是5-HT2A受体(pKi=8.2)和D4受体(pKi=8.0)的高亲和力拮抗剂,也是D2受体(pKi=6.7)的低亲和力拮抗剂[1]。

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名称

[ CAS 号 ]:
2448-68-2

[ 中文名 ]:
1-[4-(4-氟苯基)-4-氧亚基丁基]-[1,4-联哌啶]-4-甲酰胺二盐酸

[ 英文名 ]:
Pipamperone Dihydrochloride

[英文别名 ]:

Pipamperone Dihydrochloride
Pipamperone dihydrochloride
PipamperoneDihydrochloride

生物活性

[ 描述 ]:

二氢哌安酮(Floropipamide；McN JR 3345)是5-HT2A受体(pKi=8.2)和D4受体(pKi=8.0)的高亲和力拮抗剂,也是D2受体(pKi=6.7)的低亲和力拮抗剂[1]。

[ 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

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

PAR2, PAR4[6]

[参考文献]

[1]. Erik Buntinx, MD, et al. Selective Serotonergic Properties of Low-Dose Pipamperone May Enhance Antidepressant Effect: Preclinical Evidence.

物理化学性质

[ 沸点 ]:
563.7ºC at 760 mmHg

[ 熔点 ]:
203-218ºC

[ 分子式 ]:
C₂₁H₃₂Cl₂FN₃O₂

[ 分子量 ]:
448.40

[ 闪点 ]:
294.7ºC

[ 精确质量 ]:
447.18600

[ PSA ]:
66.64000

[ LogP ]:
4.77450

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
9.88E-13mmHg at 25°C

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DW1060000

CHEMICAL NAME :: (1,4'-Bipiperidine)-4'-carboxamide, 1'-(3-(p-fluorobenzoyl)propyl)-, dihydrochloride

CAS REGISTRY NUMBER :: 2448-68-2

LAST UPDATED :: 198212

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C21-H30-F-N3-O2.2Cl-H

MOLECULAR WEIGHT :: 448.46

WISWESSER LINE NOTATION :: T6NTJ DVZ A- DT6NTJ A3VR DF &GH 2

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 :: 1120 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,631,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 400 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,631,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 910 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,631,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 312 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,631,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 71 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,631,1982

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安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

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

[ RTECS号 ]:
DW1060000

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