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戊诺酰胺

戊诺酰胺用途

Valnoctamide (Valmethamide) 是一种 Valproate 的衍生物,可用于治疗对苯二氮卓类药物有抗药性的癫痫。Valnoctamide (Valmethamide) 直接作用于 GABAA 受体。

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戊诺酰胺名称

[ CAS 号 ]:
4171-13-5

[ 中文名 ]:
戊诺酰胺

[ 英文名 ]:
Valnoctamide

[英文别名 ]:

2-ethyl-3-methylpentanamide
Valnoctamide

戊诺酰胺生物活性

[ 描述 ]:

Valnoctamide (Valmethamide) 是一种 Valproate 的衍生物,可用于治疗对苯二氮卓类药物有抗药性的癫痫。Valnoctamide (Valmethamide) 直接作用于 GABAA 受体。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[ 靶点 ]

GABAA receptor[1]

[参考文献]

[1]. Spampanato J, et al. Valnoctamide enhances phasic inhibition: a potential target mechanism for the treatment of benzodiazepine-refractory status epilepticus. Epilepsia. 2014 Sep;55(9):e94-8.

戊诺酰胺物理化学性质

[ 密度 ]:
0.883g/cm3

[ 沸点 ]:
274.4ºC at 760mmHg

[ 熔点 ]:
113.5-114ºC

[ 分子式 ]:
C₈H₁₇NO

[ 分子量 ]:
143.22700

[ 闪点 ]:
119.8ºC

[ 精确质量 ]:
143.13100

[ PSA ]:
43.09000

[ LogP ]:
2.24430

[ 折射率 ]:
1.438

戊诺酰胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YV5950000

CHEMICAL NAME :: Valeramide, 2-ethyl-3-methyl-

CAS REGISTRY NUMBER :: 4171-13-5

BEILSTEIN REFERENCE NO. :: 1749434

LAST UPDATED :: 199612

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C8-H17-N-O

MOLECULAR WEIGHT :: 143.26

WISWESSER LINE NOTATION :: ZVY2&Y2&1

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 :: 760 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,429,1972

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 580 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,429,1972

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 999 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 62,404,1966

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 540 mg/kg

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

REFERENCE :: 27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,429,1972 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 700 mg/kg

SEX/DURATION :: female 6-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - abortion

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 159,6,1965

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 600 mg/kg

SEX/DURATION :: female 6-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: CRSBAW Comptes Rendus des Seances de la Societe de Biologie et de Ses Filiales. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1849- Volume(issue)/page/year: 159,6,1965

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戊诺酰胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ RTECS号 ]:
YV5950000

[ 海关编码 ]:
2924199090

戊诺酰胺合成路线

详细合成路线

戊诺酰胺上下游产品

戊诺酰胺上游产品

戊诺酰胺下游产品

戊诺酰胺海关

[ 海关编码 ]: 2924199090

[ 中文概述 ]:
2924199090. 其他无环酰胺（包括无环氨基甲酸酯)(包括其衍生物及盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924199090. other acyclic amides (including acyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

戊诺酰胺文献

Structure activity relationship of human microsomal epoxide hydrolase inhibition by amide and acid analogues of valproic acid.

Pharm. Res. 17(2) , 216-21, (2000)

The purpose of this study was to evaluate the in vitro inhibitory potency of various amide analogues and derivatives of valproic acid toward human microsomal epoxide hydrolase (mEH).mEH inhibition was...

A comparative electrographic analysis of the effect of sec-butyl-propylacetamide on pharmacoresistant status epilepticus.

Neuroscience 231 , 145-56, (2013)

Better treatment of status epilepticus (SE), which typically becomes refractory after about 30 min, will require new pharmacotherapies. The effect of sec-butyl-propylacetamide (SPD), an amide derivati...

Amidic modification of valproic acid reduces skeletal teratogenicity in mice.

Birth Defects Res. B Dev. Reprod. Toxicol. 71(1) , 47-53, (2004)

The antiepileptic drug valproic acid (VPA) is well known to cause neural tube and skeletal defects in both humans and animals. The amidic VPA analogues valpromide (VPD) and valnoctamide (VCD) have muc...

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