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利多氟嗪

利多氟嗪用途

Lidoflazine 是 HERG K+ 通道的高亲和力阻滞剂。Lidoflazine 也是一种抗心绞痛的钙通道阻滞剂,具有延长 QT 间期和发生室性心律失常的重大风险。

利多氟嗪名称

[ CAS 号 ]:
3416-26-0

[ 中文名 ]:
利多氟嗪

[ 英文名 ]:
Lidoflazine

[中文别名 ]:

立得安

[英文别名 ]:

利多氟嗪生物活性

[ 描述 ]:

Lidoflazine 是 HERG K+ 通道的高亲和力阻滞剂。Lidoflazine 也是一种抗心绞痛的钙通道阻滞剂,具有延长 QT 间期和发生室性心律失常的重大风险。

[ 靶点 ]

Ca2+

[体外研究]

Lidoflazine抑制从稳定表达野生型HERG的HEK 293细胞记录的有效HERG电流(IHERG)(IC50为~16nM)。

[参考文献]

[1]. https://www.ncbi.nlm.nih.gov/pubmed/15135665

利多氟嗪物理化学性质

[ 密度 ]:
1.161g/cm3

[ 沸点 ]:
632.6ºC at 760mmHg

[ 熔点 ]:
158-162ºC

[ 分子式 ]:
C₃₀H₃₅F₂N₃O

[ 分子量 ]:
491.61500

[ 闪点 ]:
336.4ºC

[ 精确质量 ]:
491.27500

[ PSA ]:
35.58000

[ LogP ]:
5.69880

[ 外观性状 ]:
white

[ 折射率 ]:
1.581

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMSO: ≥10mg/mL

利多氟嗪MSDS

详细MSDS(安全技术说明书)

利多氟嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TK7910000

CHEMICAL NAME :: 1-Piperazineaceto-2',6'-xylidide, 4-(4,4-bis(p-fluorophenyl)butyl)-

CAS REGISTRY NUMBER :: 3416-26-0

BEILSTEIN REFERENCE NO. :: 0904339

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C30-H35-F2-N3-O

MOLECULAR WEIGHT :: 491.68

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 20570 ug/kg/8D-I

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,923,1972

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3200 mg/kg

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

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 32,461,1977

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3200 mg/kg

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

REFERENCE :: FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 32,461,1977

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: ARPMAS Archiv der Pharmazie (Weinheim, Germany) (VCH Pub., Inc., 303 NW 12th Ave., Deerfield Beach, FL 33441) V.51-261, 1835-1923; V.305- 1972- Volume(issue)/page/year: 322,359,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 40 mg/kg

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

REFERENCE :: FRXXBL French Demande Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2279383

利多氟嗪安全信息

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

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
36

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

[ RTECS号 ]:
TK7910000

利多氟嗪文献

Protective effects of the lazaroid U74500A and lidoflazine on liver preservation with UW solution.

Transpl. Int. 6(5) , 281-4, (1993)

The effect of adding a 21-aminosteroid, U74500A, and a Ca2+ antagonist, lidoflazine, alone and together to UW solution was assessed in a rat liver preservation model. Following preservation, the liver...

Simpson's paradox and clinical trials: what you find is not necessarily what you prove.

Ann. Emerg. Med. 21(12) , 1480-2, (1992)

Expensive clinical trials have become the gold standard for evaluating the efficacy of promising new therapeutic agents. Full exploration of the collected data is routine to maximize the yield of the ...

1,4-Dihydropyridines bearing a pharmacophoric fragment of lidoflazine.

Bioorg. Med. Chem. 4(10) , 1629-35, (1996)

A series of 1,4-dihydropyridines bearing a pharmacophoric fragment of lidoflazine was synthesized. The compounds were evaluated for inotropic, chronotropic, and calcium antagonist activities. All comp...

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