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布西拉明

布西拉明用途

【用途一】
用于慢性关节风湿病的治疗。

布西拉明名称

[ CAS 号 ]:
65002-17-7

[ 中文名 ]:
布溪那明

[ 英文名 ]:
Bucillamine

[中文别名 ]:

[英文别名 ]:

L-Cysteine, N-(2-mercapto-2-methyl-1-oxopropyl)-
Bucillamine
N-(2-Mercapto-2-methylpropionyl)-L-cysteine
N-(2-Mercaptoisobutyryl)-L-cysteine
N-(2-Methyl-2-sulfanylpropanoyl)-L-cysteine
N-(2-Mercapto-2-methyl-1-oxopropyl)-L-cysteine
MFCD00867570
Thiobutarit
N-(2-Mercapto-2-methylpropanoyl)-L-cysteine

布西拉明生物活性

[ 描述 ]:

布西拉明(SA96)是一种口服活性和有效的巯基供体和抗氧化剂。布西拉明也是一种具有抗血管生成特性的抗风湿剂。布西拉明可以保护高危器官移植中的缺血/再灌注损伤。布西拉明抑制VEGF的产生。布西拉明可用于研究脉络膜新生血管(CNV)和类风湿性关节炎(RA)[1][2]。

[ 相关类别 ]:

研究领域 >> 心血管疾病

研究领域 >> 炎症/免疫

信号通路 >> 蛋白酪氨酸激酶 >> VEGFR

[体内研究]

布西拉明显著提高接受肝移植的大鼠的存活率并保护其免受肝损伤[1]。布西拉明(结膜下注射)显著减少大鼠实验性CNV的渗漏和大小[2]。

[参考文献]

[1]. Amersi F, et al. Bucillamine, a thiol antioxidant, prevents transplantation-associated reperfusion injury. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8915-20.

[2]. Yanagi Y, et al. Subconjunctival administration of bucillamine suppresses choroidal neovascularization in rat. Invest Ophthalmol Vis Sci. 2002 Nov;43(11):3495-9.

布西拉明物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
438.0±45.0 °C at 760 mmHg

[ 熔点 ]:
119-123ºC

[ 分子式 ]:
C₇H₁₃NO₃S₂

[ 分子量 ]:
223.313

[ 闪点 ]:
218.7±28.7 °C

[ 精确质量 ]:
223.033676

[ PSA ]:
144.00000

[ LogP ]:
1.28

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.553

[ 储存条件 ]:
Hygroscopic, -20?C Freezer, Under Inert Atmosphere

布西拉明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HA2420000

CHEMICAL NAME :: L-Cysteine, N-(2-mercapto-2-methyl-1-oxopropyl)-

CAS REGISTRY NUMBER :: 65002-17-7

LAST UPDATED :: 199312

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C7-H13-N-O3-S2

MOLECULAR WEIGHT :: 223.33

WISWESSER LINE NOTATION :: SHX1&1&VMYVQ1SH

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 :: 3900 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 353 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1021 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1006 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 420 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1090 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - cyanosis

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: 14,346,1983

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 990 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4305958

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - respiratory stimulation Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,429,1985 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 mg/kg/52W-C

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - changes in metals, not otherwise specified

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,429,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15 gm/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight Blood - other changes

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: 14,346,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 45500 mg/kg/91D-I

TOXIC EFFECTS :: Blood - changes in erythrocyte (RBC) count Kidney, Ureter, Bladder - changes in bladder weight Related to Chronic Data - changes in testicular weight

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: 14,346,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 18 gm/kg/15W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - changes in metals, not otherwise specified

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 29,429,1985 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4800 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

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: 16,626,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1200 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

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: 16,626,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3600 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

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: 16,626,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 840 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

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: 16,665,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3900 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death

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: 16,654,1985

布西拉明安全信息

[ 危害码 (欧洲) ]:
T,N,Xi

[ 风险声明 (欧洲) ]:
R23/24/25:Toxic by inhalation, in contact with skin and if swallowed . R50/53:Very Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment .

[ 安全声明 (欧洲) ]:
S26-S27-S28-S45-S60-S61

[ 危险品运输编码 ]:
UN 3146 6.1/PG 3

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2930909090

布西拉明合成路线

详细合成路线

布西拉明上下游产品

布西拉明上游产品

布西拉明下游产品

布西拉明制备

S-苄基-2-巯基-2-甲基丙酸(63.1g，0.30mo1)和氯化亚砜(39.3g, 0.33mo1)反应，得S-苄基-2-巯基-2-甲基丙酰氯。另外将S-苄基-L-半胱氨酸(73.9g，0.35mo1)溶于lmol/L氢氧化钠溶液(700ml，0.70mo1)，用冰浴冷却，在搅拌下滴入上述得到的丙酰氯衍生物，加毕再搅拌1h。用盐酸酸化后，用乙酸乙酯提取。提取液水洗后，无水硫酸钠干燥，浓缩。剩余物用硅胶柱层析，用苯-乙酸乙酯(1：1)洗脱。洗脱液减压蒸发至于，得89.6g的油状物，收率74%。
将上述得到的油状物(89．6g，0.222mol)溶于500ml液氨，在搅拌下，分批小量加入金属钠(21.2g，0.917mo1)。当反应完全后，加入氯化铵(59.4g，1.11mo1)，蒸出氨。剩余物加水溶解。分出水层，用乙酸乙酯洗，然后在冷却下用盐酸酸化。用乙酸乙酯提取酸化产生的沉淀。提取液用水洗，无水硫酸钠干燥，减压浓缩，乙酸乙酯重结晶，得40.1g布西拉明，收率81%，熔点139～140℃。

布西拉明海关

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%