盐酸奥布卡因

盐酸奥布卡因用途

Oxybuprocaine hydrochloride (Benoxinate hydrochloride) 可逆地阻断钠通道 (sodium channels),并防止角膜,结膜和巩膜中疼痛神经的冲动传播。Oxybuprocaine hydrochloride 专用于眼科和耳鼻喉科。

盐酸奥布卡因名称

[ CAS 号 ]:
5987-82-6

[ 中文名 ]:
奥布卡因盐酸盐

[ 英文名 ]:
benoxinate hydrochloride

[中文别名 ]:

[英文别名 ]:

Oxybuprocaine HCL
Benoxinate hydrochloride
MFCD00012512
EINECS 227-808-8
oxybuprocaine hydrochloride

盐酸奥布卡因生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 神经疾病

[体内研究]

盐酸氧丁普鲁卡因(盐酸苯诺辛酯；27.6,51.7,103.5,413.9μg；s.c.)对大鼠针刺有剂量依赖性阻滞作用[1]。盐酸氧丁普鲁卡因(27.6μg)可产生100%的感觉/伤害性阻滞[1]。动物模型：雄性Sprague-Dawley大鼠(203-253 g)[1]剂量：27.6、51.7、103.5、413.9μg给药：SC结果：对针刺提供剂量依赖性阻滞。

[参考文献]

[1]. Chen YW, et al. The Addition of Epinephrine to Proxymetacaine or Oxybuprocaine Solution Increases the Depth and Duration of Cutaneous Analgesia in Rats. Reg Anesth Pain Med. 2016 Sep-Oct;41(5):601-6.

[2]. Chen YW, et al. Adding Dopamine to Proxymetacaine or Oxybuprocaine Solutions Potentiates and Prolongs the Cutaneous Antinociception in Rats. Anesth Analg. 2018 May;126(5):1721-1728.

[3]. Page M, et al. Safety, efficacy, and patient acceptability of lidocaine hydrochloride ophthalmic gel as a topicalocular anesthetic for use in ophthalmic procedures. Clin Ophthalmol. 2009;3:601-9. Epub 2009 Nov 2.

盐酸奥布卡因物理化学性质

[ 沸点 ]:
446.9ºC at 760 mmHg

[ 熔点 ]:
158 - 162ºC

[ 分子式 ]:
C₁₇H₂₉ClN₂O₃

[ 分子量 ]:
344.877

[ 闪点 ]:
224.1ºC

[ 精确质量 ]:
344.186676

[ PSA ]:
64.79000

[ LogP ]:
4.32950

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
室温

盐酸奥布卡因毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DG1502900

CHEMICAL NAME :: Benzoic acid, 4-amino-3-butoxy-, 2-(diethylamino)ethyl ester, monohydrochloride

CAS REGISTRY NUMBER :: 5987-82-6

LAST UPDATED :: 199509

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C17-H28-N2-O3.Cl-H

MOLECULAR WEIGHT :: 344.93

WISWESSER LINE NOTATION :: 4OR BZ EVO2N2&2 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,154,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >5600 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,232,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42500 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,154,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >6800 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,232,1990

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 30 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,232,1990

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

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 5600 ug/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,1957,1974

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 21 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,232,1990

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 4200 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,232,1990

盐酸奥布卡因安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S22-S26-S36

[ 危险品运输编码 ]:
UN 1544PSN2 6.1 / PGIII

[ RTECS号 ]:
DG15029

[ 海关编码 ]:
29225000

盐酸奥布卡因制备

【方法一】
将3-氧-4-硝基苯甲酸与乙醇酯化得到的乙酯，与丁基溴反应，获得丁氧基硝基苯甲酸乙酯，加苛性碱皂化，生成3-丁氧基-4-硝基苯甲酸。然后，将其与亚硫酰氯反应得到酰基氯中间体，再与二乙氨基乙醇酯化，得到3-丁氧基-4-硝基苯甲酸二乙氨基乙酯，经还原成盐即制成盐酸丁氧普鲁卡因。

盐酸奥布卡因海关

[ 海关编码 ]: 29225000

盐酸奥布卡因文献

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To investigate whether the Sonic hedgehog (Shh) signaling induces myopic development by increasing the expression of matrix metalloproteinase (MMP)-2 in guinea pigs.A translucent diffuser was glued on...

Corneal thickness differences between sexes after oxybuprocaine eye drops.

Optom. Vis. Sci. 92(1) , 89-94, (2015)

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