972-02-1

972-02-1结构式
972-02-1结构式
  • 常用中文名:地芬尼多
  • 常用英文名:Difenidol
  • CAS号:972-02-1
  • 分子式:C21H27NO
  • 分子量:309.44500
  • 相关类别: 原料药 消化系统用药 止吐催吐药
  • 发布时间:2018-08-31 17:26:30
  • 更新时间:2024-01-08 14:27:36
  • 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]。

化源商城直购

中文名 地芬尼多
英文名 diphenidol
中文别名 1,1-二苯基-4-(1-哌啶基)-1-丁醇
二苯哌丁醇
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
Difenidolum
Avomol
1,1-diphenyl-4-piperidin-1-yl-butan-1-ol
描述 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]。
相关类别
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。
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)

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

海关编码 2933399090

~10%

972-02-1结构式

972-02-1

文献:Schmidt, Andreas; Marchetti, Mauro; Eilbracht, Peter Tetrahedron, 2004 , vol. 60, # 50 p. 11487 - 11492

~%

972-02-1结构式

972-02-1

文献:Helvetica Chimica Acta, , vol. 24, p. 209 E, 220 E Journal of the American Chemical Society, , vol. 74, p. 4085

~%

972-02-1结构式

972-02-1

文献:Journal of Organometallic Chemistry, , vol. 332, p. 9 - 18

~%

972-02-1结构式

972-02-1

文献:GB683950 , ;
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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%