<生产厂家价格>

地芬尼多

地芬尼多用途

迪芬尼多是一种口服活性止吐药。地芬尼多减轻慢性压迫损伤后大鼠的异常神经性疼痛和TNF-α过表达。迪芬尼多还具有局部麻醉活性并抑制钠电流。迪芬尼多可用于梅尼埃病、抗眩晕、止吐和镇痛的研究[1][2]。

地芬尼多名称

[ CAS 号 ]:
972-02-1

[ 中文名 ]:
地芬尼多

[ 英文名 ]:
Difenidol

[中文别名 ]:

[英文别名 ]:

Difenidol
1,1-diphenyl-4-piperidylbutanol
Vontrol
Nometic
1,1-diphenyl-4-piperidin-1-ylbutan-1-ol
DIPHENIDOL
defenidol
Difenidolo [DCIT]
Difenidolo
Cephadol

地芬尼多生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体外研究]

地芬尼多(0.1-100µM)在N2A细胞中阻断Na+电流,IC50为0.77µM,希尔系数为1.15[1]。

[体内研究]

地芬尼多(0.77 mg/大鼠；鞘内注射；单次)阻断大鼠的运动功能、本体感受和伤害感受[1]。迪芬尼多(0.62,3.09 mg/kg；i.p.；每日一次,持续7天)有效逆转或完全阻断大鼠CCI诱发的机械性异常疼痛[2]。动物模型：雄性SpragueeDawley大鼠(275-325g)[1]。剂量：0.77 mg/大鼠(2.50µmol/大鼠)给药：鞘内注射；仅有一个的结果：造成100%的运动功能、本体感觉和伤害感觉阻滞,作用持续时间分别为51、77和123分钟。动物模型：雄性成年Sprague-Dawley大鼠(200-250 g；CCI大鼠模型)[2]。剂量：0.62,3.09 mg/kg(2,10µmol/kg)给药：腹膜内注射；每天一次,持续7天。结果：给药后1h阻断CCI诱导的低机械戒断阈值。在CCI后第7天降低TNF-α水平并减轻大鼠神经性触觉异常疼痛。

地芬尼多物理化学性质

[ 密度 ]:
1.066 g/cm3

[ 沸点 ]:
473.3ºC at 760 mmHg

[ 熔点 ]:
105ºC

[ 分子式 ]:
C₂₁H₂₇NO

[ 分子量 ]:
309.44500

[ 闪点 ]:
233.5ºC

[ 精确质量 ]:
309.20900

[ PSA ]:
23.47000

[ LogP ]:
4.12650

[ 折射率 ]:
1.5614 (estimate)

地芬尼多毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM4970000

CHEMICAL NAME :: 1-Piperidinebutanol, alpha,alpha-diphenyl-

CAS REGISTRY NUMBER :: 972-02-1

BEILSTEIN REFERENCE NO. :: 0265884

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C21-H27-N-O

MOLECULAR WEIGHT :: 309.49

WISWESSER LINE NOTATION :: T6NTJ A3XQR&R

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 :: 815 mg/kg

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

REFERENCE :: PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959- Volume(issue)/page/year: 5,265,1963

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 304 mg/kg

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

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 450 mg/kg

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

REFERENCE :: PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959- Volume(issue)/page/year: 5,265,1963

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 103 mg/kg

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

REFERENCE :: LACHDL Liebigs Annalen der Chemie. (Verlag Chemie International, Inc., VCH Pub., Inc., 303 N.W. 12th Ave., Deerfield Beach, FL 33441) No. 1- 1979- Volume(issue)/page/year: (10),1554,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 32 mg/kg

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

REFERENCE :: MPHEAE Medicina et Pharmacologia Experimentalis. (Basel, Switzerland) V.12-17, 1965-67. For publisher information, see PHMGBN. Volume(issue)/page/year: 13,325,1965

地芬尼多安全信息

[ 海关编码 ]:
2933399090

地芬尼多合成路线

详细合成路线

地芬尼多上下游产品

地芬尼多上游产品

地芬尼多下游产品

地芬尼多海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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: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 ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%