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乙酰普卡胺

乙酰普卡胺用途

N-Acetylprocainamide 是第三代抗心律失常剂,能够抑制 K+ 通道。

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乙酰普卡胺名称

[ CAS 号 ]:
32795-44-1

[ 中文名 ]:
N-乙酰普鲁卡因胺

[ 英文名 ]:
N-Acetylprocainamide

[中文别名 ]:

乙酰普卡胺

[英文别名 ]:

NAPA
4-acetamido-N-(2-diethylaminoethyl)benzamide
Acecainide [INN]
MFCD00009052
4-acetamido-N-[2-(diethylamino)ethyl]benzamide
N-Acetyloprokainamid
Acecainidum
Acekainid
N-Acetylnovocainamide
Acekainid [Polish]

乙酰普卡胺生物活性

[ 描述 ]:

N-Acetylprocainamide 是第三代抗心律失常剂,能够抑制 K+ 通道。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[ 靶点 ]

K+ channel[1]

[体外研究]

N-乙酰基过甲酰胺是K +阻断剂。 N-乙酰基过甲酰胺减少由K +和乙酰甲胆碱诱导的张力。 N-乙酰基过硫酰胺对0.3和1μM乙酰甲胆碱诱导的收缩的pIC50值分别为2.80±0.03和2.65±0.02。并且K +通道阻滞剂抑制了N-乙酰基过甲酰胺的这种松弛作用[1]。 N-乙酰基过甲酰胺对Na +吸收或Cl-分泌没有影响[2]。

[参考文献]

[1]. Nakahara T, et al. Role of K+ channels in N-acetylprocainamide-induced relaxation of bovine tracheal smooth muscle. Eur J Pharmacol. 2001 Mar 9;415(1):73-8.

[2]. Plass H, et al. Class I antiarrhythmics inhibit Na+ absorption and Cl- secretion in rabbit descending colon epithelium. Naunyn Schmiedebergs Arch Pharmacol. 2005 Jun;371(6):492-9.

[相关活性小分子]

乙酰普卡胺物理化学性质

[ 密度 ]:
1.097g/cm3

[ 沸点 ]:
500ºC at 760mmHg

[ 熔点 ]:
138-140ºC(lit.)

[ 分子式 ]:
C₁₅H₂₃N₃O₂

[ 分子量 ]:
277.36200

[ 闪点 ]:
256.2ºC

[ 精确质量 ]:
277.17900

[ PSA ]:
61.44000

[ LogP ]:
2.18050

[ 储存条件 ]:
-20°C

[ 水溶解性 ]:
soluble1%, clear, colorless to faintly yellow (1N HCl)

乙酰普卡胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AE1974350

CHEMICAL NAME :: Acetanilide, 4'-((2-(diethylamino)ethyl)carbamoyl)-

CAS REGISTRY NUMBER :: 32795-44-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H23-N3-O2

MOLECULAR WEIGHT :: 277.41

WISWESSER LINE NOTATION :: 2N2&2MVR DMV1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 380 mg/kg

TOXIC EFFECTS :: Cardiac - other changes

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 169,156,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3173 No. of Facilities: 71 (estimated) No. of Industries: 2 No. of Occupations: 2 No. of Employees: 758 (estimated) No. of Female Employees: 361 (estimated)

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乙酰普卡胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
UN 3249

[ WGK德国 ]:
3

[ RTECS号 ]:
AE1974350

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2924299090

乙酰普卡胺合成路线

详细合成路线

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乙酰普卡胺海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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 ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

乙酰普卡胺文献

Drug-herb interaction: effect of St John's wort on bioavailability and metabolism of procainamide in mice.

Arch. Pathol. Lab. Med. 131(7) , 1094-8, (2007)

St John's wort induces the activity of the cytochrome P450 enzyme system causing treatment failure because of increased metabolism of many drugs. Procainamide is metabolized by a different pathway to ...

Application of computer-assisted radiotelemetry in the pharmacokinetic and pharmacodynamic modeling of procainamide and N-acetylprocainamide.

J. Pharm. Sci. 85(6) , 595-9, (1996)

The cardiovascular pharmacodynamics (PD) of procainamide and N-acetylprocainamide have not been well characterized in small rodents without the presence of anesthesia or restraint. This study was unde...

The discordant influences of infarct healing on the electrophysiologic effects of procainamide and N-acetylprocainamide.

J. Pharmacol. Exp. Ther. 273(1) , 315-9, (1995)

Ischemic zone refractoriness and conduction delay respond differently to infarct healing and, hypothetically, may exert discordant influences on the electrophysiologic action of different classes of a...

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