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尼普地洛

尼普地洛用途

β-阻断作用和血管扩张作用,无内源性拟交感作用,可降低心搏数,减少心肌耗氧量和冠脉血流量,还有抗心律不齐作用。用于轻至中度原发性高血压。

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尼普地洛名称

[ CAS 号 ]:
81486-22-8

[ 中文名 ]:
尼普地洛

[ 英文名 ]:
Nipradilol

[英文别名 ]:

尼普地洛生物活性

[ 描述 ]:

尼普拉洛尔(KT-210;K-351)是一种强效的α-1-肾上腺素能受体阻断剂。尼泊洛尔抑制了苯肾上腺素(HY-B0769)诱导的白化兔模型中的眼内压(IOP)升高。尼普拉多抑制去甲肾上腺素(NA)诱导的肌肉收缩,同时对狗冠状动脉也表现出血管舒张作用[1][2]。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[ 靶点 ]

α1-adrenergic receptor


[体外研究]

尼普拉洛尔(1μM;10分钟) 抑制钾诱导的犬肌肉收缩,第50页值为 0.8μM[1]尼普拉洛尔(1μM;10分钟) 降低静息张力,抑制近端区钠诱导的收缩[1]。

[体内研究]

尼普拉洛尔(0.125%、0.25%、0.5%;静脉注射; 单剂量) 以浓度依赖的方式抑制兔眼眼压的增加[2]。

[参考文献]

[1]. 3,4-dihydro-8-(2-hydroxy-3-isopropylaminopropoxy)-3-nitroxy-2H-1-benzopyran (K-351) and its denitrated derivative on smooth muscle cells of the dog coronary artery. Br J Pharmacol. 1983 May;79(1):285-95.  

[2]. Nishio K. Alpha-1-adrenoceptor blocking activity of KT-210 (nipradilol ophthalmic solution) on intraocular pressure in the rabbit eye[J]. Nihon Ganka Kiyo (Folia Ophthalmol Jpn), 1999, 50: 655-660.

尼普地洛物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
500.0±45.0 °C at 760 mmHg

[ 熔点 ]:
110-122ºC

[ 分子式 ]:
C15H22N2O6

[ 分子量 ]:
326.345

[ 闪点 ]:
256.2±28.7 °C

[ 精确质量 ]:
326.147797

[ PSA ]:
105.77000

[ LogP ]:
1.97

[ 外观性状 ]:
无色针状晶体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.561

尼普地洛毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DJ2887000
CHEMICAL NAME :
2H-1-Benzopyran-3-ol, 3,4-dihydro-8-(2-hydroxy-3-((1-methylethyl)amino)prop oxy)-, 3-nitrate
CAS REGISTRY NUMBER :
81486-22-8
LAST UPDATED :
199612
DATA ITEMS CITED :
20
MOLECULAR FORMULA :
C15-H22-N2-O6
MOLECULAR WEIGHT :
326.39

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 :
1040 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
144 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
850 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
78 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
461 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
147 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
416 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
68 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>400 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
300 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,725,1985
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 20,228,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
5250 mg/kg/5W-C
TOXIC EFFECTS :
Liver - changes in liver weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,733,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
93600 mg/kg/52W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Blood - normocytic anemia Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,221,1985 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
5400 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,1,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
4400 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,747,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2200 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,747,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
550 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,747,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
2700 mg/kg
SEX/DURATION :
female 17-22 day(s) after conception lactating female 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - physical
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 30,1,1985
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
260 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,747,1985
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尼普地洛合成路线

尼普地洛上下游产品

尼普地洛制备

消旋体的制备。1.82g2-烯丙基-6-甲氧基苯基乙酸酯溶于20ml二氯甲烷,加入3.0ml40%(W/V)过氧乙酸溶液和0.18g乙酸钾,在室温下搅拌48h。将反应液加到100ml氯仿和50ml5%亚硫酸钠水溶液中。分出有机层,水洗,无水硫酸钠干燥。减压浓缩得1.74g淡黄色粘稠液体的化合物(Ⅰ),收率88.7%。

1.74g化合物(Ⅰ)溶于10ml乙醚,在0℃加入5.0ml20%(W/V)氯化氢的乙醚溶液,在室温下搅拌12h。加入100ml乙醚,用饱和碳酸氢钠溶液中和。分出醚层,水洗,无水硫酸钠干燥。减压浓缩得1.83g淡黄色粘稠液体的化合物(Ⅱ),收率90.4%。

1.82g化合物(Ⅱ)溶于10ml二甲基甲酰胺,加入1.26g碳酸钾,在室温下搅拌2h后,加入50ml水和100ml苯。分出有机层,水洗,无水硫酸钠干燥。减压浓缩得1.53g淡黄色粘稠液体的化合物(Ⅲ)。

1.53g化合物(Ⅲ)溶于30ml甲醇,加入10ml1mol/L氢氧化钠溶液。在室温下搅拌1h后,加入12ml1mol/L盐酸。减压浓缩,剩余物用30ml苯提取。提取液水洗,无水硫酸钠干燥。减压浓缩得到的棕色粘稠油用苯-己烷重结晶,得0.66g无色棱状结晶的化合物c,收率52.1%,熔点79~82℃。

1.50g化合物1mol/L加到8.60g47%氢溴酸中,在90℃下搅拌9h。冷至室温,用氢氧化钠水溶液调至弱酸性后,用30ml乙酸乙酯提取。提取液用饱和盐水洗,无水硫酸钠干燥。减压浓缩,丙酮结晶得棕色固体。再用乙酮和己烷重结晶,得1.23g无色针状结晶的化合物(Ⅴ),收率88.9%,熔点126~129℃。

20mmol化合物(Ⅴ)和23mmol三乙胺溶于20ml四氢呋喃,在0~5℃加入23mmol氯甲酸乙酯(或三氯乙酰氯)溶于35ml四氢呋喃的溶液,再搅拌0.5h。过滤,滤液减压浓缩。剩余物(4.85g)溶于80ml乙腈,冷至-8~-10℃,加入乙酰硝酸酯(从2.22g乙酸酐和1.36g发烟硝酸制得),在此温度再搅拌0.5h。再在-8℃加入另一份乙酰硝酸酯(从1.36g乙酸酐和0.85g发烟硝酸制得),继续搅拌0.5h。加入碳酸氢钠以终止反应,用180ml乙酸乙酯提取。提取液用碳酸氢钠溶液和饱和盐水洗,干燥,浓缩至干。剩余物棕色油溶于10ml甲醇和0.93g氢氧化钠溶于5ml水的混合溶液,在室温下搅拌0.5h。用浓盐酸酸化后,减压蒸去甲醇,用60ml乙酸乙酯提取。提取液用饱和盐水洗,干燥,浓缩至干。剩余的深棕色油用硅胶柱层析,用苯洗脱。得到的固体再用苯和己烷结晶,得无色结晶的化合物(Ⅵ),收率65%,熔点101~103℃。

4mmol化合物(Ⅵ)溶于15ml1mol/L氢氧化钠,加入16mmol环氧氯丙烷,在50℃下搅拌2h。加入30ml乙酸乙酯。分出有机层,用10ml1mol/L氢氧化钠溶液和10ml饱和盐水洗,干燥,浓缩至干。得到的油状物无需提纯,可直接用于下列反应。取4mmol该油溶于30ml甲醇,加入20mmol异丙胺,在70℃下加热1h。浓缩至干,剩余油状物用三氧化二铝柱层析,氯仿洗脱。得到的固体用乙酸乙酯和己烷结晶,得尼普地洛,收率61%,熔点110~122℃。

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推荐生产厂家/供应商:

公司名:上海化源世纪贸易有限公司

区域:上海市普陀区

价格:

联系人:徐经理

产品详情:Nipradolol


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